réservé à la recherche
N° Cat.S2775
| Cibles apparentées | Akt Wnt/beta-catenin PKC HSP ROCK Integrin Bcr-Abl Actin FAK Kinesin |
|---|---|
| Autre Microtubule Associated Inhibiteurs | MMAF Patupilone (Epothilone B) Lexibulin (CYT997) CW069 Combretastatin A4 Epothilone A ABT-751 (E7010) TAI-1 Cucurbitacin B INH1 |
| Lignées cellulaires | Type dessai | Concentration | Temps dincubation | Formulation | Description de lactivité | PMID |
|---|---|---|---|---|---|---|
| L1210 murine leukemia cell | Growth inhibition assay | In vitro for its inhibitory activity against L1210 murine leukemia cell growth, IC50=38 nM | 1738146 | |||
| LT12 | Antiproliferative assay | 48 hrs | Antiproliferative activity against rat LT12 cells after 48 hrs by XTT assay, IC50 = 0.006 μM. | 19220018 | ||
| HepG2 | Function assay | 0.1 to 10 uM | 1 hr | Inhibition of TNFalpha-induced NFkappaB (unknown origin)-dependent transcriptional activity expressed in human HepG2 cells at 0.1 to 10 uM incubated for 1 hr prior to TNFalpha induction measured after 6 hrs by dual-luciferase reporter gene assay | 25827522 | |
| PANC1 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human PANC1 cells after 48 hrs by SRB assay, GI50 = 0.01 μM. | 27688193 | ||
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay, GI50 = 0.01 μM. | 27688193 | ||
| MDA-MB-231 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by SRB assay, GI50 = 0.01 μM. | 27688193 | ||
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by SRB cell proliferation assay, GI50 = 0.01 μM. | 29089233 | ||
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells after 48 hrs by SRB cell proliferation assay, GI50 = 0.01 μM. | 29089233 | ||
| MDA-MB-231 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by SRB cell proliferation assay, GI50 = 0.01 μM. | 29089233 | ||
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay, GI50 = 0.015 μM. | 25827522 | ||
| MDA-MB-231 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by SRB assay, GI50 = 0.017 μM. | 25827522 | ||
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by SRB assay, GI50 = 0.02 μM. | 25827522 | ||
| L1210 | Function assay | 48 hrs | Inhibitory concentration against proliferation of cultured lymphoid leukemia L1210 cells during 48 hrs, ID50 = 0.027 μM. | 7131483 | ||
| PANC1 | Anticancer assay | 48 hrs | Anticancer activity against human PANC1 cells after 48 hrs by SRB assay, GI50 = 0.029 μM. | 27130357 | ||
| A549 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human A549 cells after 24 hrs by MTT assay, IC50 = 0.0366 μM. | 20110137 | ||
| NCI60 | Growth inhibition assay | 48 hrs | Growth inhibition of human NCI60 cells incubated for 48 hrs by sulforhodamine B assay, GI50 = 0.0389 μM. | 27956038 | ||
| P388 | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse P388 cells after 48 hrs by XTT assay, IC50 = 0.04 μM. | 19220018 | ||
| LT12 | Antiproliferative assay | 48 hrs | Antiproliferative activity against LT12 cells by XTT assay after 48 hrs, IC50 = 0.04 μM. | 17181164 | ||
| LT12 | Antiproliferative assay | 48 hrs | Antiproliferative activity against rat LT12 cells after 48 hrs by XTT assay, IC50 = 0.04 μM. | 20537765 | ||
| LT12 | Antiproliferative assay | 48 hrs | Antiproliferative activity against rat LT12 cells after 48 hrs by XTT assay, IC50 = 0.04 μM. | 21705223 | ||
| MDA-MB-231 | Anticancer assay | 48 hrs | Anticancer activity against human MDA-MB-231 cells after 48 hrs by SRB assay, GI50 = 0.042 μM. | 27130357 | ||
| L1210 | Antiproliferative assay | 48 hrs | Antiproliferative activity against L1210 cells by XTT assay after 48 hrs, IC50 = 0.05 μM. | 17181164 | ||
| P388 | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse adriamycin-resistant P388 cells after 48 hrs by XTT assay, IC50 = 0.05 μM. | 17973361 | ||
| L12 | Antiproliferative assay | 48 hrs | Antiproliferative activity against rat multidrug-resistant L12 cells after 48 hrs by XTT assay, IC50 = 0.05 μM. | 17973361 | ||
| L1210 | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse L1210 cells after 48 hrs by XTT assay, IC50 = 0.05 μM. | 20537765 | ||
| P388 | Antiproliferative assay | 48 hrs | Antiproliferative activity against ADR-resistant mouse P388 cells after 48 hrs by XTT assay, IC50 = 0.05 μM. | 21705223 | ||
| U2OS | Function assay | 72 hrs | Induction of mitotic arrest in human U2OS cells assessed as mitotic index after 72 hrs by microscopic analysis, EC50 = 0.05 μM. | 24900887 | ||
| L1210 | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse L1210 cells after 48 hrs by XTT assay, IC50 = 0.06 μM. | 17973361 | ||
| L1210 | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse L1210 cells after 48 hrs by XTT assay, IC50 = 0.06 μM. | 19220018 | ||
| L1210 | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse L1210 cells after 48 hrs by XTT assay, IC50 = 0.06 μM. | 21705223 | ||
| HeLa | Anticancer assay | 48 hrs | Anticancer activity against human HeLa cells after 48 hrs by SRB assay, GI50 = 0.063 μM. | 27130357 | ||
| MDA-MB-231 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 0.065 μM. | 28117204 | ||
| NCI-H460 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human NCI-H460 cells after 48 hrs by alamar blue assay, IC50 = 0.068 μM. | 21563750 | ||
| BT549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human BT549 cells after 48 hrs by alamar blue assay, IC50 = 0.069 μM. | 21563750 | ||
| LT12 MDR | Antiproliferative assay | 48 hrs | Antiproliferative activity against LT12 MDR cells by XTT assay after 48 hrs, IC50 = 0.07 μM. | 17181164 | ||
| L1210 | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse vincristine-resistant L1210 cells after 48 hrs by XTT assay, IC50 = 0.07 μM. | 17973361 | ||
| P388 | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse P388 cells after 48 hrs by XTT assay, IC50 = 0.07 μM. | 17973361 | ||
| LT12 | Antiproliferative assay | 48 hrs | Antiproliferative activity against multi drug-resistant rat LT12 cells after 48 hrs by XTT assay, IC50 = 0.07 μM. | 20537765 | ||
| P388 | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse P388 cells after 48 hrs by XTT proliferation assay, IC50 = 0.07 μM. | 21705223 | ||
| LT12 | Antiproliferative assay | 48 hrs | Antiproliferative activity against rat multiple drug-resistant LT12 cells after 48 hrs by XTT assay, IC50 = 0.07 μM. | 21705223 | ||
| L1210 | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse VCR-resistant L1210 cells after 48 hrs by XTT assay, IC50 = 0.07 μM. | 21705223 | ||
| 451LU | Antiproliferative assay | 48 hrs | Antiproliferative activity against human 451LU cells after 48 hrs by alamar blue assay, IC50 = 0.072 μM. | 21563750 | ||
| P388 | Antiproliferative assay | 48 hrs | Antiproliferative activity against P388 cells by XTT assay after 48 hrs, IC50 = 0.08 μM. | 17181164 | ||
| P388 | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse P388 cells after 48 hrs by XTT assay, IC50 = 0.08 μM. | 20537765 | ||
| SKOV3 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human SKOV3 cells after 48 hrs by alamar blue assay, IC50 = 0.08 μM. | 21563750 | ||
| SGC7901 | Growth inhibition assay | 72 hrs | Growth inhibition of human SGC7901 cells after 72 hrs by MTT assay, IC50 = 0.08 μM. | 25262051 | ||
| A549 | Anticancer assay | 48 hrs | Anticancer activity against human A549 cells after 48 hrs by SRB assay, GI50 = 0.08 μM. | 27130357 | ||
| K562 | Function assay | Effective concentration required to arrest propidium iodide stained K562 cells in G2/M phase, EC50 = 0.082 μM. | 12852768 | |||
| SKBR3 | Growth inhibition assay | 48 hrs | Growth inhibition of human SKBR3 cells after 48 hrs by MTT assay, IC50 = 0.084 μM. | 22850214 | ||
| HeLa | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HeLa cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 0.086 μM. | 28117204 | ||
| A549 | Cytotoxicity assay | Cytotoxicity against human A549 cells by MTT assay, IC50 = 0.087 μM. | 21954851 | |||
| COLO205 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human COLO205 cells after 48 hrs by alamar blue assay, IC50 = 0.088 μM. | 21563750 | ||
| L1210 VCR | Antiproliferative assay | 48 hrs | Antiproliferative activity against L1210 VCR cells by XTT assay after 48 hrs, IC50 = 0.09 μM. | 17181164 | ||
| L1210 | Antiproliferative assay | 48 hrs | Antiproliferative activity against vincristine-resistant mouse L1210 cells after 48 hrs by XTT assay, IC50 = 0.09 μM. | 20537765 | ||
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 0.09 μM. | 28117204 | ||
| KB/HeLa | Cell cycle assay | Cell cycle arrest in KB/HeLa cells by accumulation at G2/M phase, EC50 = 0.091 μM. | 17181164 | |||
| KB/HeLa | Cell cycle assay | 24 hrs | Cell cycle arrest in KB/HeLa cells assessed as accumulation at G2/M phase after 24 hrs by flow cytometric analysis, EC50 = 0.091 μM. | 17973361 | ||
| KB/HeLa | Cell cycle assay | 24 hrs | Cell cycle arrest in human KB/HeLa cells assessed as G2/M phase accumulation after 24 hrs by FACS analysis, EC50 = 0.091 μM. | 19220018 | ||
| KB/HeLa | Cell cycle assay | 24 hrs | Cell cycle arrest in human KB/HeLa cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide staining by FACS analysis, EC50 = 0.091 μM. | 20537765 | ||
| KB/HeLa | Cell cycle assay | 24 hrs | Cell cycle arrest in human KB/HeLa cells assessed as accumulation of cells at G2/M phase after 24 hrs by flow cytometry, EC50 = 0.091 μM. | 21705223 | ||
| MiaPaCa | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MiaPaCa cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 0.091 μM. | 28117204 | ||
| MCF7 | Growth inhibition assay | Growth inhibition of human MCF7 cells by Sulforhodamine B assay, GI50 = 0.1 μM. | 21106458 | |||
| MCF7 | Growth inhibition assay | Growth inhibition of human MCF7 cells by Sulforhodamine B assay, LC50 = 0.1 μM. | 21106458 | |||
| A549 | Growth inhibition assay | Growth inhibition of human A549 cells by Sulforhodamine B assay, GI50 = 0.1 μM. | 21106458 | |||
| A549 | Growth inhibition assay | Growth inhibition of human A549 cells by Sulforhodamine B assay, LC50 = 0.1 μM. | 21106458 | |||
| A549 | Cell cycle assay | 24 hrs | Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide staining by flow cytometry, EC50 = 0.1065 μM. | 20110137 | ||
| RKO | Cytotoxicity assay | Cytotoxic activity against human colon adenocarcinoma RKO cells without ectopic inducible expression of cyclin-dependent kinase inhibitor p27kip1, IC50 = 0.11 μM. | 12852768 | |||
| RKO | Antiproliferative assay | 48 hrs | Antiproliferative activity against RKO cells by XTT assay after 48 hrs, IC50 = 0.11 μM. | 17181164 | ||
| RKO | Cytotoxicity assay | 48 hrs | Cytotoxicity against human RKO cells after 48 hrs by XTT assay, IC50 = 0.11 μM. | 17973361 | ||
| RKO | Antiproliferative assay | Antiproliferative activity against human RKO cells by XTT assay, IC50 = 0.11 μM. | 19220018 | |||
| RKO | Antiproliferative assay | 48 hrs | Antiproliferative activity against human RKO cells after 48 hrs by XTT assay, IC50 = 0.11 μM. | 20537765 | ||
| RKOp27 | Cytotoxicity assay | 48 hrs | Cytotoxicity against non induced human RKOp27 cells after 48 hrs by XTT assay, IC50 = 0.11 μM. | 21705223 | ||
| SW480 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human SW480 cells after 48 hrs by alamar blue assay, IC50 = 0.12 μM. | 21563750 | ||
| A549 | Growth inhibition assay | 72 hrs | Growth inhibition of human A549 cells after 72 hrs by MTT assay, IC50 = 0.12 μM. | 25262051 | ||
| KB/HeLa | Antiproliferative assay | Antiproliferative activity against human KB/HeLa cells by XTT assay, IC50 = 0.14 μM. | 19220018 | |||
| KB/HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against KB/HeLa cells by XTT assay after 48 hrs, IC50 = 0.14 μM. | 17181164 | ||
| KB/HeLa | Cytotoxicity assay | 48 hrs | Cytotoxicity against human KB/HeLa cells after 48 hrs by XTT assay, IC50 = 0.14 μM. | 17973361 | ||
| KB/HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human KB/HeLa cells after 48 hrs by XTT assay, IC50 = 0.14 μM. | 20537765 | ||
| KB/HeLa | Cytotoxicity assay | 48 hrs | Cytotoxicity against human KB/HeLa cells after 48 hrs by XTT assay, IC50 = 0.14 μM. | 21705223 | ||
| HT1080 | Growth inhibition assay | 72 hrs | Growth inhibition of human HT1080 cells after 72 hrs by MTT assay, IC50 = 0.14 μM. | 25262051 | ||
| NCI-H460 | Antiproliferative assay | 48 hrs | Antiproliferative activity against NCI-H460 cells by XTT assay after 48 hrs, IC50 = 0.15 μM. | 17181164 | ||
| NCI-H460 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human NCI-H460 cells after 48 hrs by XTT assay, IC50 = 0.15 μM. | 17973361 | ||
| NCI-H460 | Antiproliferative assay | Antiproliferative activity against human NCI-H460 cells by XTT assay, IC50 = 0.15 μM. | 19220018 | |||
| NCI-H460 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human NCI-H460 cells after 48 hrs by XTT assay, IC50 = 0.15 μM. | 20537765 | ||
| NCI-H460 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human NCI-H460 cells after 48 hrs by XTT assay, IC50 = 0.15 μM. | 21705223 | ||
| SKOV3 | Antiproliferative assay | 48 hrs | Antiproliferative activity against SKOV3 cells by XTT assay after 48 hrs, IC50 = 0.17 μM. | 17181164 | ||
| P388 ADR | Antiproliferative assay | 48 hrs | Antiproliferative activity against P388 ADR cells by XTT assay after 48 hrs, IC50 = 0.17 μM. | 17181164 | ||
| SKOV3 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human SKOV3 cells after 48 hrs by XTT assay, IC50 = 0.17 μM. | 17973361 | ||
| SKOV3 | Antiproliferative assay | Antiproliferative activity against human SKOV3 cells by XTT assay, IC50 = 0.17 μM. | 19220018 | |||
| SKOV3 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human SKOV3 cells after 48 hrs by XTT assay, IC50 = 0.17 μM. | 20537765 | ||
| P388 | Antiproliferative assay | 48 hrs | Antiproliferative activity against adriamycin-resistant mouse P388 cells after 48 hrs by XTT assay, IC50 = 0.17 μM. | 20537765 | ||
| SKOV3 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human SKOV3 cells after 48 hrs by XTT assay, IC50 = 0.17 μM. | 21705223 | ||
| HCT116 | Cytotoxicity assay | Cytotoxicity against human HCT116 cells by SRB assay, IC50 = 0.173 μM. | 21954851 | |||
| HeLa | Cytotoxicity assay | 24 to 48 hrs | Cytotoxicity against human HeLa cells after 24 to 48 hrs by trypan blue assay, IC50 = 0.178 μM. | 23445405 | ||
| L1210 | Function assay | 0.3 uM | 24 hrs | Fraction of cell population of cultured lymphoid leukemia L1210 cells in mitosis at a dose of 0.3 uM after 24 hr, Mitotic index = 0.19 μM. | 7131483 | |
| DLD1 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human DLD1 cells after 48 hrs by alamar blue assay, IC50 = 0.19 μM. | 21563750 | ||
| SF268 | Antiproliferative assay | 48 hrs | Antiproliferative activity against SF268 cells by XTT assay after 48 hrs, IC50 = 0.3 μM. | 17181164 | ||
| SF268 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human SF268 cells after 48 hrs by XTT assay, IC50 = 0.3 μM. | 17973361 | ||
| SF268 | Antiproliferative assay | Antiproliferative activity against human SF268 cells by XTT assay, IC50 = 0.3 μM. | 19220018 | |||
| L12 | Antiproliferative assay | 48 hrs | Antiproliferative activity against rat L12 cells after 48 hrs by XTT assay, IC50 = 0.3 μM. | 17973361 | ||
| SF268 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human SF268 cells after 48 hrs by XTT assay, IC50 = 0.3 μM. | 20537765 | ||
| SF268 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human SF268 cells after 48 hrs by XTT assay, IC50 = 0.3 μM. | 21705223 | ||
| LT12 | Antiproliferative assay | 48 hrs | Antiproliferative activity against rat LT12 cells ectopic expression of human MDR1 after 48 hrs by XTT assay, IC50 = 0.4 μM. | 19220018 | ||
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells after 48 hrs by SRB assay, GI50 = 0.5 μM. | 20529689 | ||
| SK-N-SH | Cytotoxicity assay | 48 hrs | Cytotoxicity against human SK-N-SH cells after 48 hrs by SRB assay, GI50 = 0.65 μM. | 20529689 | ||
| SK-N-SH | Growth inhibition assay | Growth inhibition of human SK-N-SH cells by Sulforhodamine B assay, GI50 = 0.66 μM. | 21106458 | |||
| HeLa | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.71 μM. | 23748152 | ||
| HeLa | Growth inhibition assay | Growth inhibition of human HeLa cells by Sulforhodamine B assay, GI50 = 0.75 μM. | 21106458 | |||
| SK-N-SH | Growth inhibition assay | Growth inhibition of human SK-N-SH cells by Sulforhodamine B assay, LC50 = 0.75 μM. | 21106458 | |||
| K562 | Function assay | Inhibition of tubulin polymerization in human K562 cells, IC50 = 0.76 μM. | 20546980 | |||
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 0.81 μM. | 25131956 | ||
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay, GI50 = 0.81 μM. | 27344493 | ||
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.89 μM. | 25599948 | ||
| HeLa | Growth inhibition assay | Growth inhibition of human HeLa cells by Sulforhodamine B assay, LC50 = 0.9 μM. | 21106458 | |||
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by SRB assay, IC50 = 0.9 μM. | 28988624 | ||
| MDA-MB-453 | Cytotoxicity assay | 48 hrs | Cytotoxicity in human MDA-MB-453 cells incubated for 48 hrs by MTT assay, IC50 = 0.91 μM. | 28923381 | ||
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 0.94 μM. | 25131956 | ||
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay, GI50 = 0.94 μM. | 27344493 | ||
| MIAPaCa2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MIAPaCa2 cells assessed as growth inhibition after 48 hrs by SRB assay, GI50 = 0.95 μM. | 25131956 | ||
| MIAPaCa2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MIAPaCa2 cells after 48 hrs by SRB assay, GI50 = 0.95 μM. | 27344493 | ||
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells after 48 hrs by SRB assay, LC50 = 1 μM. | 20529689 | ||
| HCT116 | Cytotoxicity assay | 48 hrs | Cytotoxicity in human HCT116 cells incubated for 48 hrs by MTT assay, IC50 = 1.06 μM. | 28923381 | ||
| HeLa | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HeLa cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 1.1 μM. | 25599948 | ||
| DU145 | Cytotoxicity assay | 48 hrs | Cytotoxicity in human DU145 cells incubated for 48 hrs by MTT assay, IC50 = 1.14 μM. | 28923381 | ||
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay, IC50 = 1.2 μM. | 28988624 | ||
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay, IC50 = 1.25 μM. | 28988624 | ||
| HCT116 | Anticancer assay | 48 hrs | Anticancer activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 1.262 μM. | 28789894 | ||
| IMR32 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human IMR32 cells after 48 hrs by SRB assay, IC50 = 1.3 μM. | 28988624 | ||
| A549 | Anticancer assay | 48 hrs | Anticancer activity against human A549 cells after 48 hrs by MTT assay, IC50 = 1.513 μM. | 28789894 | ||
| MCF7 | Anticancer assay | 48 hrs | Anticancer activity against human MCF7 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay, IC50 = 1.6 μM. | 26231080 | ||
| DU145 | Anticancer assay | 48 hrs | Anticancer activity against human DU145 cells after 48 hrs by MTT assay, IC50 = 1.698 μM. | 28789894 | ||
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 1.7 μM. | 25599948 | ||
| PC3 | Cytotoxicity assay | 48 hrs | Cytotoxicity in human PC3 cells incubated for 48 hrs by MTT assay, IC50 = 1.84 μM. | 28923381 | ||
| MDA-MB-231 | Anticancer assay | 48 hrs | Anticancer activity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 1.862 μM. | 28789894 | ||
| A549 | Anticancer assay | 48 hrs | Anticancer activity against human A549 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay, IC50 = 1.87 μM. | 26231080 | ||
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 1.87 μM. | 28668476 | ||
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50 = 2.31 μM. | 23748152 | ||
| SK-N-SH | Cytotoxicity assay | 48 hrs | Cytotoxicity against human SK-N-SH cells after 48 hrs by SRB assay, LC50 = 2.8 μM. | 20529689 | ||
| DU145 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human DU145 cells after 48 hrs by MTT assay, IC50 = 2.8 μM. | 23748152 | ||
| HeLa | Anticancer assay | 48 hrs | Anticancer activity against human HeLa cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay, IC50 = 2.83 μM. | 26231080 | ||
| HeLa | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 2.83 μM. | 28668476 | ||
| DU145 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human DU145 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 3.2 μM. | 25599948 | ||
| HaCaT | Cytotoxicity assay | 48 hrs | Cytotoxic activity against human HaCaT cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay, IC50 = 8.9 μM. | 26231080 | ||
| NIH3T3 | Apoptosis assay | 0.5 ug/ml | 24 hrs | Induction of apoptosis in mouse NIH3T3 cells assessed as accumulation at subG1 phase at 0.5 ug/ml after 24 hrs by flow cytometry | 18247573 | |
| PC3M | Apoptosis assay | 0.5 ug/ml | 24 hrs | Induction of apoptosis in human PC3M cells assessed as accumulation at subG1 phase at 0.5 ug/ml after 24 hrs by flow cytometry | 18247573 | |
| NRK | Function assay | 30 uM | 60 mins | Golgi-disturbing activity in golgi apparatus of rat NRK cells assessed as microtubule depolymerization-associated golgi fragmentation at 30 uM after 60 mins by Hoechst 3342 staining-based immunofluorescence microscopy | 20189813 | |
| Vero | Function assay | 5 ug/ml | 30 mins | Effect on disruption of microtubules in african green monkey Vero cells at 5 ug/ml after 30 mins by immunofluorescence method | 19182783 | |
| MCF7 | Apoptosis assay | 2.5 uM | 48 hrs | Induction of apoptosis in human MCF7 cells assessed as nuclear fragmentation at 2.5 uM after 48 hrs by DAPI staining | 21194809 | |
| MCF7 | Function assay | 2.5 uM | 48 hrs | Inhibition of tubulin polymerization in human MCF7 cells assessed as disrupted microtubule organization at 2.5 uM after 48 hrs by microscopic analysis | 21194809 | |
| A549 | Cell cycle assay | 24 hrs | Cell cycle arrest in human A549 cells assessed as accumulation of cells in G2 phase after 24 hrs measured using propidium iodide staining by FACS analysis | 21863853 | ||
| A549 | Apoptosis assay | 10 to 100 nM | 48 hrs | Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 10 to 100 nM after 48 hrs by annexin-V FITC/7-ADD staining-based flow cytometric analysis | 21916509 | |
| A549 | Apoptosis assay | 10 to 100 nM | 48 hrs | Induction of apoptosis in human A549 cells assessed as necrotic cells at 10 to 100 nM after 48 hrs by annexin-V FITC/7-ADD staining-based flow cytometric analysis | 21916509 | |
| A549 | Cell cycle assay | 1 uM | 48 hrs | Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 1 uM after 48 hrs by propidium iodide staining-based flow cytometric analysis relative to control | 22361684 | |
| SKBR3 | Function assay | 50 to 100 nM | 24 hrs | Induction of Hsp27 phosphorylation in human SKBR3 cells at 50 to 100 nM after 24 hrs by SDS-PAGE analysis | 22435708 | |
| SKBR3 | Function assay | 0.2 to 1 uM | 24 hrs | Induction of Hsp27 phosphorylation in human SKBR3 cells at 0.2 to 1 uM after 24 hrs by SDS-PAGE analysis | 22435708 | |
| MCF7 | Function assay | 4 uM | 24 hrs | Inhibition of microtubule organization in human MCF7 cells at 4 uM after 24 hrs by immunofluorescence analysis | 22982122 | |
| Jurkat T | Function assay | 36 hrs | Induction of microtubule damage in human Jurkat T cells overexpressing Bcl2 after 36 hrs by immunostaining method | 22197393 | ||
| Jurkat T | Function assay | 36 hrs | Induction of microtubule damage in human Jurkat T cells overexpressing Neo after 36 hrs by immunostaining method | 22197393 | ||
| Jurkat T | Apoptosis assay | 36 hrs | Induction of apoptosis in human Jurkat T cells overexpressing Bcl2 assessed as cellular protrusions after 36 hrs by light microscopy | 22197393 | ||
| Jurkat T | Apoptosis assay | 36 hrs | Induction of apoptosis in human Jurkat T cells overexpressing Neo after 36 hrs by flow cytometry | 22197393 | ||
| Jurkat T | Apoptosis assay | 36 hrs | Induction of apoptosis in human Jurkat T cells overexpressing Neo assessed as cellular protrusions after 36 hrs by light microscopy | 22197393 | ||
| HeLa | Function assay | 1 uM | 24 hrs | Inhibition of tubulin polymerization in human HeLa cells assessed as tubulin soluble fraction at 1 uM after 24 hrs by immunohistochemistry analysis | 23313639 | |
| HeLa | Function assay | 1 uM | 24 hrs | Mitotic arrest in human HeLa cells assessed as increase in accumulation at G2/M phase at 1 uM for 24 hrs by PI staining/FACS analysis | 24530033 | |
| HeLa | Cell cycle assay | 2 uM | 24 hrs | Cell cycle arrest at G2/M phase in human HeLa cells assessed as increase in cyclin B1 expression at 2 uM after 24 hrs by immunoblot analysis relative to control | 25499929 | |
| HeLa | Cell cycle assay | 2 uM | 24 hrs | Cell cycle arrest at G2/M phase in human HeLa cells assessed as soluble form of tubulin at 2 uM after 24 hrs by immunoblot analysis relative to control | 25499929 | |
| DU145 | Function assay | 50 uM | 48 hrs | Disruption of microtubule network in human DU145 cells at 50 uM after 48 hrs by immunohistochemistry analysis | 25615796 | |
| HeLa | Function assay | 25 uM | 24 hrs | Effect on PCM1 protein in human HeLa cells assessed as accumulation of pericentriolar material at 25 uM after 24 hrs by immunofluorescence microscopy | 25050880 | |
| SGC7901 | Function assay | 48 hrs | Induction of distortions in tubulin assembly in human SGC7901 cells assessed as abnormal mitotic spindle formation at 2 fold IC50 level incubated for 48 hrs by immunofluorescence staining based fluorescence microscopy | 25262051 | ||
| HT1080 | Function assay | 48 hrs | Induction of distortions in tubulin assembly in human HT1080 cells assessed as abnormal mitotic spindle formation at 2 fold IC50 level incubated for 48 hrs by immunofluorescence staining based fluorescence microscopy | 25262051 | ||
| MCF7 | Function assay | 1 uM | 4 hrs | Induction of tubulin depolymerization in human MCF7 cells at 1 uM after 4 hrs by sedimentation assay and Western blotting method | 25369367 | |
| DU145 | Function assay | 1.5 uM | 48 hrs | Reduction in mitochondrial membrane potential in human DU145 cells at 1.5 uM incubated for 48 hrs by JC1 dye staining based flow cytometry | 26330077 | |
| SKBR3 | Function assay | 2.5 uM | 24 hrs | Induction of microtubule destabilization in human SKBR3 cells assessed as soluble fraction of protein at 2.5 uM after 24 hrs by Western blot analysis | 26599530 | |
| HeLa | Function assay | 100 nM | 4 hrs | Inhibition of tubulin polymerization in human HeLa cells assessed as microtubule disruption in mitotic phase at 100 nM after 4 hrs by indirect immunofluorescence analysis | 26641132 | |
| HeLa | Function assay | 100 nM | 4 hrs | Inhibition of tubulin polymerization in human HeLa cells assessed as microtubule disruption in interphase at 100 nM after 4 hrs by indirect immunofluorescence analysis | 26641132 | |
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | |||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | |||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | |||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | |||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | |||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | |||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | |||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | |||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | |||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 29435139 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 29435139 | |||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 29435139 | |||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | |||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | |||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 29435139 | |||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | |||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 29435139 | |||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 29435139 | |||
| HeLa | Function assay | 24 hrs | Inhibition of tubulin polymerization in human HeLa cells assessed as increase in soluble tubulin fraction after 24 hrs by Western blot analysis | 28818768 | ||
| HeLa | Function assay | 0.1 uM | 24 hrs | Inhibition of tubulin polymerization in human HeLa cells assessed as shift of tubulin protein to soluble fraction at 0.1 uM after 24 hrs by Western blot analysis | 29501940 | |
| PC3MLN4 | Function assay | 1 uM | 24 hrs | Upregulation of Cyclin-B1 protein expression in human PC3MLN4 cells at 1 uM after 24 hrs by Western blot method | 29288939 | |
| PC3MLN4 | Function assay | 1 uM | 48 hrs | Disruption of microtubule dynamics in human PC3MLN4 cells at 1 uM after 48 hrs by immunofluorescence microscopic method | 29288939 | |
| MCF7 | Function assay | 1 uM | 4 hrs | Induction of tubulin depolymerization in human MCF7 cells at 1 uM after 4 hrs by Western blot method | 27689728 | |
| Jurkat | Function assay | 1 uM | 4 hrs | Induction of tubulin depolymerization in human Jurkat cells at 1 uM after 4 hrs by Western blot method | 27689728 | |
| Cliquez pour voir plus de données expérimentales sur les lignées cellulaires | ||||||
| Poids moléculaire | 301.32 | Formule | C14H11N3O3S |
Stockage (À partir de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 31430-18-9 | Télécharger le SDF | Stockage des solutions mères |
|
|
| Synonymes | R17934, Oncodazole, NSC238159 | Smiles | COC(=O)NC1=NC2=C(N1)C=C(C=C2)C(=O)C3=CC=CS3 | ||
|
In vitro |
DMSO
: 7.5 mg/mL
(24.89 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
|||||
Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)
Étape 2 : Entrez la formulation in vivo (Ceci nest que le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)
Résultats du calcul :
Concentration de travail : mg/ml;
Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH2O, mélanger et clarifier.
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuite μL Huile de maïs, mélanger et clarifier.
Remarque : 1. Assurez-vous que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue lors de lajout précédent est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie peuvent être utilisées pour faciliter la dissolution.
| Targets/IC50/Ki |
Microtubules
(Cell-free assay) Abl
(Cell-free assay) 0.21 μM
Abl (E255K)
(Cell-free assay) 0.53 μM
Abl (T315I)
(Cell-free assay) 0.64 μM
|
|---|---|
| In vitro |
Nocodazole est un ligand de haute affinité pour les kinases liées au cancer, y compris Abl phosphorylée, c-Kit, BRAF et MEK avec un Kd de 0,091 μM, 1,6 μM, 1,8 μM et 1,6 μM, respectivement. De plus, le Kd de ce composé pour Abl(E255K) phosphorylée, Abl(T315I) phosphorylée, BRAF(V600E) et PI3Kγ est de 0,12 μM, 0,17 μM, 1,1 μM et 1,5 μM, respectivement. Il induit l'apoptosis dans les cellules de leucémie lymphoïde chronique. Cette substance chimique inhibe le transport du glucose stimulé par l'insuline. Elle diminue l'apoptosis dans certaines cellules de carcinome du côlon humain. Elle altère la morphologie et la directionnalité des cellules de l'éminence ganglionnaire médiale migrantes. À des concentrations élevées, ce composé dépolymérise rapidement les microtubules dans les cellules, tandis que de faibles concentrations de celui-ci inhibent l'instabilité dynamique des microtubules. Les cellules mitotiques incubées avec différentes concentrations sont inhibées de progresser en phase G1 6 heures après la libération du bloc de Nocodazole, avec une concentration inhibitrice médiane de 4 nM. Les cellules prétraitées au Nocodazole exposées en l'absence de cette substance chimique ne forment que des microtubules flottants libres, tandis que les cellules prétraitées exposées en sa présence organisent des microtubules assemblés au centrosome. Il perturbe les microtubules en se liant à la β-tubuline. Ce composé empêche la formation de l'une des deux liaisons disulfures inter-chaînes. Il altère le transport des vésicules. Il supprime la mort cellulaire et la dysfonction lysosomale induites par le METH. La mort cellulaire induite par le METH est significativement diminuée par le prétraitement avec ce composé par rapport au METH seul. Il double l'efficacité HDR jusqu'à 30% dans les iPSCs. Il améliore l'efficacité HDR médiée par CRISPR et a un effet additif sur l'amélioration de l'édition précise du génome. |
| In vivo |
Le volume et le poids tumoraux des souris traitées avec Nocodazole sont significativement réduits par rapport à ceux traités avec ce composé seul. Le traitement combiné avec cette substance chimique améliore fortement l'apoptosis des xénogreffes tumorales COLO 205 traitées avec celle-ci seule. |
Références |
|
| Méthodes | Biomarqueurs | Images | PMID |
|---|---|---|---|
| Western blot | Cdc2 / cyclin B1 / MAD2 / Cdc20 |
|
21918689 |
| Immunofluorescence | Tubulin / LC8 Brd4 / α-tubulin |
|
23038268 |
| Growth inhibition assay | Cell viability |
|
21918689 |
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