solo para uso en investigación
Romidepsin (FK228) HDAC inhibidor
Cat. No.S3020
Estructura química
Peso molecular: 540.7
Saltar a
Control de calidad
Lote:
Pureza:
99.95%
99.95
Cultivo celular, tratamiento y concentración de trabajo
| Líneas celulares | Tipo de ensayo | Concentración | Tiempo de incubación | Formulación | Descripción de la actividad | PMID |
|---|---|---|---|---|---|---|
| SU-DHL4 | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 | |
| U2932 | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 | |
| OCI-LY7 | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 | |
| Farage | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 | |
| LY7/EBV | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 | |
| U2932/EBV | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 | |
| HCT116 | Growth Inhibition Assay | 5-5000 nM | 24 h | DMSO | induces cell death in a concentration-dependent manner | 25492515 |
| ACH-2 | Function Assay | 1-9 nM | 24 h | induces HIV-1 Env expression | 25149467 | |
| MCF-10A | Growth Inhibition Assay | IC50=0.17±0.01 nM | 24954856 | |||
| MCF-7 | Growth Inhibition Assay | IC50=1.10±0.20 nM | 24954856 | |||
| SK-BR-3 | Growth Inhibition Assay | IC50=1.00±0.35 nM | 24954856 | |||
| MDA-MB-231 | Growth Inhibition Assay | IC50=0.68±0.14 nM | 24954856 | |||
| PC3 | Growth Inhibition Assay | IC50=1.65±0.35 nM | 24954856 | |||
| HCT116 | Growth Inhibition Assay | IC50=1.00±0.00 nM | 24954856 | |||
| HCT116-p21-/- | Growth Inhibition Assay | IC50=1.26±0.37 nM | 24954856 | |||
| S1 | Growth Inhibition Assay | IC50=7.67±0.29 nM | 24954856 | |||
| SW620 | Growth Inhibition Assay | IC50=0.93±0.29 nM | 24954856 | |||
| LOX-IMVI | Growth Inhibition Assay | IC50=0.87±0.03 nM | 24954856 | |||
| UACC-62 | Growth Inhibition Assay | IC50=0.56±0.16 nM | 24954856 | |||
| MDA-MB-435 | Growth Inhibition Assay | IC50=0.90±0.06 nM | 24954856 | |||
| SF-295 | Growth Inhibition Assay | IC50=0.88±0.15 nM | 24954856 | |||
| A549 | Growth Inhibition Assay | IC50=1.26±0.24 nM | 24954856 | |||
| H460 | Growth Inhibition Assay | IC50=2.58±0.80 nM | 24954856 | |||
| EKVX | Growth Inhibition Assay | IC50=1.33±0.34 nM | 24954856 | |||
| H146 | Growth Inhibition Assay | IC50=0.22±0.07 nM | 24954856 | |||
| H526 | Growth Inhibition Assay | IC50=0.15±0.03 nM | 24954856 | |||
| HuT-78 | Growth Inhibition Assay | IC50=1.73±0.44 nM | 24954856 | |||
| HA | Growth Inhibition Assay | 0.625-10nM | 48 h | induces a significantly stronger inhibition of cell proliferation co-treated with bortezomib | 24771510 | |
| MS-275 | Growth Inhibition Assay | 0.625-10nM | 48 h | induces a significantly stronger inhibition of cell proliferation co-treated with bortezomib | 24771510 | |
| CD4 T | Growth Inhibition Assay | 48 h | EC50=4.5±1.0 nM | 24722454 | ||
| CD4 T | Growth Inhibition Assay | 48 h | CC50=107±126 nM | 24722454 | ||
| CD4+ T | Growth Inhibition Assay | EC50=3 nM | 24495105 | |||
| A549 | Growth Inhibition Assay | 10–100 nM | 24/36/48 h | inhibits cell growth in both concentration- and time-dependent manner | 24485799 | |
| JJN3 | Growth Inhibition Assay | 24/48 h | EC50<1 nM; 48 h | 24030150 | ||
| OPM-2 | Growth Inhibition Assay | 24/48 h | EC50s=1 nM; 48 h | 24030150 | ||
| RPMI-8226 | Growth Inhibition Assay | 24/48 h | EC50s=1.8 nM; 48 h | 24030150 | ||
| U266 | Growth Inhibition Assay | 24/48 h | EC50s=10 nM; 48 h | 24030150 | ||
| CA46 | Apoptosis Assay | 6 h | induces blunt apoptosis | 23966164 | ||
| DG75 | Apoptosis Assay | 6 h | induces no apoptosis | 23966164 | ||
| Ramos | Apoptosis Assay | 6 h | induces extensive apoptosis | 23966164 | ||
| ST486 | Apoptosis Assay | 6 h | induces extensive apoptosis | 23966164 | ||
| HuT78 | Apoptosis Assay | 1/10/100 nM | 48 h | induces apoptosis at 1 nM | 23532732 | |
| DpVp35 | Apoptosis Assay | 1/10/100 nM | 48 h | induces blunt apoptosis | 23532732 | |
| DpVp50 | Apoptosis Assay | 1/10/100 nM | 48 h | induces blunt apoptosis | 23532732 | |
| DpP75 | Apoptosis Assay | 1/10/100 nM | 48 h | induces blunt apoptosis | 23532732 | |
| SKOV-3 | Growth Inhibition Assay | 1–20nM | 72 h | DMSO | reduces cell viability alone and combined with cisplatin | 23010348 |
| Brca1 WT | Growth Inhibition Assay | 1–20nM | 72 h | DMSO | reduces cell viability alone and combined with cisplatin | 23010348 |
| Brca1 Null | Growth Inhibition Assay | 1–20nM | 72 h | DMSO | reduces cell viability alone and combined with cisplatin | 23010348 |
| OVCAR-8 | Growth Inhibition Assay | 1–20nM | 72 h | DMSO | reduces cell viability alone and combined with cisplatin | 23010348 |
| NCI/ADR-RES | Growth Inhibition Assay | 1–20nM | 72 h | DMSO | reduces cell viability alone and combined with cisplatin | 23010348 |
| HCT116 | Growth Inhibition Assay | 5 nM-50 μM | 24 h | DMSO | inhibits cell growth in a concentration-dependent manner | 22924958 |
| RKO | Growth Inhibition Assay | 5 nM-50 μM | 24 h | DMSO | inhibits cell growth in a concentration-dependent manner | 22924958 |
| CO115 | Growth Inhibition Assay | 5 nM-50 μM | 24 h | DMSO | inhibits cell growth in a concentration-dependent manner | 22924958 |
| HFS | Growth Inhibition Assay | 5 nM | 24/48/72 h | inhibits cell growth time-dependently | 22106282 | |
| LNCaP | Growth Inhibition Assay | 5 nM | 24/48/72 h | inhibits cell growth time-dependently | 22106282 | |
| A549 | Growth Inhibition Assay | 5 nM | 24/48/72 h | inhibits cell growth time-dependently | 22106282 | |
| 697 | Growth Inhibition Assay | IC50 = 2.5 nM | 21538216 | |||
| 697-R | Growth Inhibition Assay | IC50 = 8.6 nM | 21538216 | |||
| HUT78 | Growth Inhibition Assay | IC50=1 nM | 21198545 | |||
| THJ-16T | Growth Inhibition Assay | 1 nM | 24 h | inhibits cell growth | 20810568 | |
| HCT116 | Function Assay | 20 nM | 8 h | modulates transcript levels for hundreds of genes in either direction | 20739454 | |
| B104 | Function Assay | 2 nM | 24/48/72 h | increases the surface expression of CD20 | 20686505 | |
| HL-60 | Cytotoxicity Assay | 1-500 nM | 24 h | induces cytotoxicity in a concentration-dependent manner | 20624163 | |
| HP100 | Cytotoxicity Assay | 1-500 nM | 24 h | induces cytotoxicity in a concentration-dependent manner | 20624163 | |
| HL-60 | Function Assay | 10 nM | 4/6/16 h | induces the generation of hydrogen peroxide from 4h | 20624163 | |
| HP100 | Function Assay | 10 nM | 4/6/16 h | induces the generation of hydrogen peroxide from 4h | 20624163 | |
| HL-60 | Function Assay | 10-500 nM | 4 h | decreases the histone deacetylase (HDAC) activity | 20624163 | |
| HP100 | Function Assay | 10-500 nM | 4 h | decreases the histone deacetylase (HDAC) activity | 20624163 | |
| 11z | Kinase Assay | 3-100 nM | reduces HDAC enzymatic activity (IC50 = 6.5 ± 0.6 nmol/L) | 20605144 | ||
| SKOV-3 | Growth Inhibition Assay | 4/8/16 nM | 48 h | inhibits cell growth in a concentration-dependent manner | 20404564 | |
| OVCAR-3 | Growth Inhibition Assay | 4/8/16 nM | 48 h | inhibits cell growth in a concentration-dependent manner | 20404564 | |
| HBL-2 | Growth Inhibition Assay | 2-10 nM | 24 h | IC50=4.3 nM | 20068080 | |
| Jeko-1 | Growth Inhibition Assay | 2-50 nM | 24 h | IC50=11 nM | 20068080 | |
| Granta-519 | Growth Inhibition Assay | 5-40 nM | 24 h | IC50=58.5 nM | 20068080 | |
| L1236 | Cytotoxicity Assay | 1 nM-100 μM | 48 h | EC50=0.07 μM | 19233470 | |
| L428 | Cytotoxicity Assay | 1 nM-100 μM | 48 h | EC50=0.43 μM | 19233470 | |
| KM-H2 | Cytotoxicity Assay | 1 nM-100 μM | 48 h | EC50=0.58 μM | 19233470 | |
| L540Cy | Cytotoxicity Assay | 1 nM-100 μM | 48 h | EC50=0.16 μM | 19233470 | |
| G401 | Function Assay | 10 nM | 24/48/72 h | DMSO | increases CDKN1C expression | 19221586 |
| STM91-01 | Function Assay | 10 nM | 24/48/72 h | DMSO | increases CDKN1C expression | 19221586 |
| SJSC | Function Assay | 10 nM | 24/48/72 h | DMSO | increases CDKN1C expression | 19221586 |
| BT16 | Function Assay | 10 nM | 24/48/72 h | DMSO | increases CDKN1C expression | 19221586 |
| NCI-H1299 | Growth Inhibition Assay | IC50=4.6±0.2 ng/ml | 19179890 | |||
| NCI-2882 | Growth Inhibition Assay | IC50=1.6±0.04 ng/ml | 19179890 | |||
| HCC95 | Growth Inhibition Assay | IC50=2.5±0.05 ng/ml | 19179890 | |||
| NCI-H23 | Growth Inhibition Assay | IC50=2.9±0.2 ng/ml | 19179890 | |||
| NCI-H157 | Growth Inhibition Assay | IC50=1.6±0.02 ng/ml | 19179890 | |||
| NCI-H460 | Growth Inhibition Assay | IC50=2.1±0.07 ng/ml | 19179890 | |||
| NCI-H1975 | Growth Inhibition Assay | IC50=1.3±0.04 ng/ml | 19179890 | |||
| NCI-H820 | Growth Inhibition Assay | IC50=2.4±0.1 ng/ml | 19179890 | |||
| NCI-H1650 | Growth Inhibition Assay | IC50=4.9±0.3 ng/ml | 19179890 | |||
| DTC1 | Growth Inhibition Assay | IC50=0.51 nM | 18566246 | |||
| KAO | Growth Inhibition Assay | IC50=0.91 nM | 18566246 | |||
| SU-CCS-1 | Growth Inhibition Assay | IC50=0.89 nM | 18566246 | |||
| SYO-1 | Growth Inhibition Assay | IC50=0.67 nM | 18566246 | |||
| FUJI | Growth Inhibition Assay | IC50=1.31 nM | 18566246 | |||
| SKNMC | Growth Inhibition Assay | IC50=1.17 nM | 18566246 | |||
| 402-91 | Growth Inhibition Assay | IC50=1.26 nM | 18566246 | |||
| 1765-92 | Growth Inhibition Assay | IC50=1.77 nM | 18566246 | |||
| JN-DSRCT-1 | Growth Inhibition Assay | IC50=1.25 nM | 18566246 | |||
| NMS-2PC | Growth Inhibition Assay | IC50=0.81 nM | 18566246 | |||
| HL60 | Growth Inhibition Assay | IC50=1.86 nM | 18566246 | |||
| A549 | Growth Inhibition Assay | IC50=3.24 nM | 18566246 | |||
| SW480 | Growth Inhibition Assay | IC50=2.69 nM | 18566246 | |||
| MCF7 | Growth Inhibition Assay | IC50=3.55 nM | 18566246 | |||
| PC-3 | Growth Inhibition Assay | IC50=2.51 nM | 18566246 | |||
| MMRU | Growth Inhibition Assay | IC50=2.57 nM | 18566246 | |||
| Hs68 | Growth Inhibition Assay | IC50=>10 nM | 18566246 | |||
| hMSC-001F | Growth Inhibition Assay | IC50=>10 nM | 18566246 | |||
| mammalian cells | Function assay | Inhibition of Histone deacetylase 4 in mammalian cells, IC50 = 0.51 μM. | 14584932 | |||
| mammalian cells | Function assay | Inhibition of Histone deacetylase 1 induced acetylated histone in mammalian cells., EC50 = 36 μM. | 14584932 | |||
| MCF7 | Growth inhibition assay | Growth inhibition of MCF7 cells, IC50 = 0.00075 μM. | 17958342 | |||
| A498 | Cytotoxicity assay | 6 days | Cytotoxicity against human A498 cells after 6 days by MTT assay, TGI = 0.028 μM. | 21967146 | ||
| COLO205 | Cytotoxicity assay | 6 days | Cytotoxicity against human COLO205 cells after 6 days by MTT assay, TGI = 0.031 μM. | 21967146 | ||
| U251 | Cytotoxicity assay | 6 days | Cytotoxicity against human U251 cells after 6 days by MTT assay, TGI = 0.031 μM. | 21967146 | ||
| RXF393 | Cytotoxicity assay | 6 days | Cytotoxicity against human RXF393 cells after 6 days by MTT assay, TGI = 0.062 μM. | 21967146 | ||
| MDA-MB-468 | Cytotoxicity assay | 6 days | Cytotoxicity against human MDA-MB-468 cells after 6 days by MTT assay, TGI = 0.09 μM. | 21967146 | ||
| COLO205 | Cytotoxicity assay | 6 days | Cytotoxicity against human COLO205 cells after 6 days by MTT assay, LC50 = 0.092 μM. | 21967146 | ||
| UACC257 | Cytotoxicity assay | 6 days | Cytotoxicity against human UACC257 cells after 6 days by MTT assay, TGI = 0.095 μM. | 21967146 | ||
| U251 | Cytotoxicity assay | 6 days | Cytotoxicity against human U251 cells after 6 days by MTT assay, LC50 = 0.13 μM. | 21967146 | ||
| A498 | Cytotoxicity assay | 6 days | Cytotoxicity against human A498 cells after 6 days by MTT assay, LC50 = 0.2 μM. | 21967146 | ||
| NCI-H322M | Cytotoxicity assay | 6 days | Cytotoxicity against human NCI-H322M cells after 6 days by MTT assay, TGI = 0.23 μM. | 21967146 | ||
| SF295 | Cytotoxicity assay | 6 days | Cytotoxicity against human SF295 cells after 6 days by MTT assay, TGI = 0.25 μM. | 21967146 | ||
| RXF393 | Cytotoxicity assay | 6 days | Cytotoxicity against human RXF393 cells after 6 days by MTT assay, LC50 = 0.3 μM. | 21967146 | ||
| NCI60 | Cytotoxicity assay | 6 days | Cytotoxicity against human NCI60 cells after 6 days by MTT assay, TGI = 0.33 μM. | 21967146 | ||
| SN12C | Cytotoxicity assay | 6 days | Cytotoxicity against human SN12C cells after 6 days by MTT assay, TGI = 0.34 μM. | 21967146 | ||
| MDA-MB-231 | Cytotoxicity assay | 6 days | Cytotoxicity against human MDA-MB-231 cells after 6 days by MTT assay, TGI = 0.35 μM. | 21967146 | ||
| ACHN | Cytotoxicity assay | 6 days | Cytotoxicity against human ACHN cells after 6 days by MTT assay, TGI = 0.73 μM. | 21967146 | ||
| SN12C | Cytotoxicity assay | 6 days | Cytotoxicity against human SN12C cells after 6 days by MTT assay, LC50 = 1.5 μM. | 21967146 | ||
| UO31 | Cytotoxicity assay | 6 days | Cytotoxicity against human UO31 cells after 6 days by MTT assay, TGI = 1.55 μM. | 21967146 | ||
| Caki1 | Cytotoxicity assay | 6 days | Cytotoxicity against human Caki1 cells after 6 days by MTT assay, TGI = 1.89 μM. | 21967146 | ||
| NCI60 | Cytotoxicity assay | 6 days | Cytotoxicity against human NCI60 cells after 6 days by MTT assay, LC50 = 3.5 μM. | 21967146 | ||
| MDA-MB-231 | Cytotoxicity assay | 6 days | Cytotoxicity against human MDA-MB-231 cells after 6 days by MTT assay, LC50 = 4.08 μM. | 21967146 | ||
| MDA-MB-468 | Cytotoxicity assay | 6 days | Cytotoxicity against human MDA-MB-468 cells after 6 days by MTT assay, LC50 = 4.14 μM. | 21967146 | ||
| ACHN | Cytotoxicity assay | 6 days | Cytotoxicity against human ACHN cells after 6 days by MTT assay, LC50 = 5.37 μM. | 21967146 | ||
| UACC257 | Cytotoxicity assay | 6 days | Cytotoxicity against human UACC257 cells after 6 days by MTT assay, LC50 = 5.46 μM. | 21967146 | ||
| NCI-H322M | Cytotoxicity assay | 6 days | Cytotoxicity against human NCI-H322M cells after 6 days by MTT assay, LC50 = 9.02 μM. | 21967146 | ||
| SF295 | Cytotoxicity assay | 6 days | Cytotoxicity against human SF295 cells after 6 days by MTT assay, LC50 = 10.2 μM. | 21967146 | ||
| Caki1 | Cytotoxicity assay | 6 days | Cytotoxicity against human Caki1 cells after 6 days by MTT assay, LC50 = 20.9 μM. | 21967146 | ||
| NCI-H23 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human NCI-H23 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| NCI-H522 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human NCI-H522 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| OVCAR5 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human OVCAR5 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| SW620 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human SW620 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| MDA-MB-435 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human MDA-MB-435 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| COLO205 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human COLO205 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| LOXIMVI | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human LOXIMVI cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| UACC62 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human UACC62 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| MDA-MB-231 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human MDA-MB-231 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| SF295 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human SF295 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| U251 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human U251 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| OVRAC3 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human OVRAC3 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| LLC | Function assay | Inhibition of HDAC-mediated HIF-1alpha activity in mouse LLC cells, IC50 = 2 μM. | 22305612 | |||
| NCI-H522 | Growth inhibition assay | Growth inhibition of human NCI-H522 cells by sulforhodamine B colorimetric method, GI50 = 0.0018 μM. | 23313638 | |||
| LOXIMVI | Growth inhibition assay | Growth inhibition of human LOXIMVI cells by sulforhodamine B colorimetric method, GI50 = 0.0025 μM. | 23313638 | |||
| A549 | Growth inhibition assay | Growth inhibition of human A549 cells by sulforhodamine B colorimetric method, GI50 = 0.0026 μM. | 23313638 | |||
| OVCAR5 | Growth inhibition assay | Growth inhibition of human OVCAR5 cells by sulforhodamine B colorimetric method, GI50 = 0.0028 μM. | 23313638 | |||
| MKN74 | Growth inhibition assay | Growth inhibition of human MKN74 cells by sulforhodamine B colorimetric method, GI50 = 0.003 μM. | 23313638 | |||
| NCI-H460 | Growth inhibition assay | Growth inhibition of human NCI-H460 cells by sulforhodamine B colorimetric method, GI50 = 0.003 μM. | 23313638 | |||
| HCT116 | Growth inhibition assay | Growth inhibition of human HCT116 cells by sulforhodamine B colorimetric method, GI50 = 0.0031 μM. | 23313638 | |||
| HCC2998 | Growth inhibition assay | Growth inhibition of human HCC2998 cells by sulforhodamine B colorimetric method, GI50 = 0.0031 μM. | 23313638 | |||
| MKN1 | Growth inhibition assay | Growth inhibition of human MKN1 cells by sulforhodamine B colorimetric method, GI50 = 0.0032 μM. | 23313638 | |||
| SKOV3 | Growth inhibition assay | Growth inhibition of human SKOV3 cells by sulforhodamine B colorimetric method, GI50 = 0.0033 μM. | 23313638 | |||
| HT-29 | Growth inhibition assay | Growth inhibition of human HT-29 cells by sulforhodamine B colorimetric method, GI50 = 0.0033 μM. | 23313638 | |||
| KM12 | Growth inhibition assay | Growth inhibition of human KM12 cells by sulforhodamine B colorimetric method, GI50 = 0.0034 μM. | 23313638 | |||
| DMS114 | Growth inhibition assay | Growth inhibition of human DMS114 cells by sulforhodamine B colorimetric method, GI50 = 0.0036 μM. | 23313638 | |||
| SF539 | Growth inhibition assay | Growth inhibition of human SF539 cells by sulforhodamine B colorimetric method, GI50 = 0.0036 μM. | 23313638 | |||
| U251 | Growth inhibition assay | Growth inhibition of human U251 cells by sulforhodamine B colorimetric method, GI50 = 0.0039 μM. | 23313638 | |||
| SF295 | Growth inhibition assay | Growth inhibition of human SF295 cells by sulforhodamine B colorimetric method, GI50 = 0.004 μM. | 23313638 | |||
| MCF7 | Growth inhibition assay | Growth inhibition of human MCF7 cells by sulforhodamine B colorimetric method, GI50 = 0.0042 μM. | 23313638 | |||
| NCI-H23 | Growth inhibition assay | Growth inhibition of human NCI-H23 cells by sulforhodamine B colorimetric method, GI50 = 0.0046 μM. | 23313638 | |||
| OVCAR3 | Growth inhibition assay | Growth inhibition of human OVCAR3 cells by sulforhodamine B colorimetric method, GI50 = 0.0046 μM. | 23313638 | |||
| MKN7 | Growth inhibition assay | Growth inhibition of human MKN7 cells by sulforhodamine B colorimetric method, GI50 = 0.0049 μM. | 23313638 | |||
| SF268 | Growth inhibition assay | Growth inhibition of human SF268 cells by sulforhodamine B colorimetric method, GI50 = 0.0049 μM. | 23313638 | |||
| MDA-MB-231 | Growth inhibition assay | Growth inhibition of human MDA-MB-231 cells by sulforhodamine B colorimetric method, GI50 = 0.0055 μM. | 23313638 | |||
| OVCAR8 | Growth inhibition assay | Growth inhibition of human OVCAR8 cells by sulforhodamine B colorimetric method, GI50 = 0.0055 μM. | 23313638 | |||
| DMS273 | Growth inhibition assay | Growth inhibition of human DMS273 cells by sulforhodamine B colorimetric method, GI50 = 0.0058 μM. | 23313638 | |||
| DU145 | Growth inhibition assay | Growth inhibition of human DU145 cells by sulforhodamine B colorimetric method, GI50 = 0.006 μM. | 23313638 | |||
| RXF631L | Growth inhibition assay | Growth inhibition of human RXF631L cells by sulforhodamine B colorimetric method, GI50 = 0.0066 μM. | 23313638 | |||
| HBC4 | Growth inhibition assay | Growth inhibition of human HBC4 cells by sulforhodamine B colorimetric method, GI50 = 0.0069 μM. | 23313638 | |||
| SNB75 | Growth inhibition assay | Growth inhibition of human SNB75 cells by sulforhodamine B colorimetric method, GI50 = 0.0072 μM. | 23313638 | |||
| BSY1 | Growth inhibition assay | Growth inhibition of human BSY1 cells by sulforhodamine B colorimetric method, GI50 = 0.0085 μM. | 23313638 | |||
| NCI-H226 | Growth inhibition assay | Growth inhibition of human NCI-H226 cells by sulforhodamine B colorimetric method, GI50 = 0.0089 μM. | 23313638 | |||
| SNB78 | Growth inhibition assay | Growth inhibition of human SNB78 cells by sulforhodamine B colorimetric method, GI50 = 0.0096 μM. | 23313638 | |||
| HBC5 | Growth inhibition assay | Growth inhibition of human HBC5 cells by sulforhodamine B colorimetric method, GI50 = 0.013 μM. | 23313638 | |||
| MKN45 | Growth inhibition assay | Growth inhibition of human MKN45 cells by sulforhodamine B colorimetric method, GI50 = 0.014 μM. | 23313638 | |||
| MKN28 | Growth inhibition assay | Growth inhibition of human MKN28 cells by sulforhodamine B colorimetric method, GI50 = 0.017 μM. | 23313638 | |||
| PC3 | Growth inhibition assay | Growth inhibition of human PC3 cells by sulforhodamine B colorimetric method, GI50 = 0.018 μM. | 23313638 | |||
| ACHN | Growth inhibition assay | Growth inhibition of human ACHN cells by sulforhodamine B colorimetric method, GI50 = 0.02 μM. | 23313638 | |||
| OVCAR4 | Growth inhibition assay | Growth inhibition of human OVCAR4 cells by sulforhodamine B colorimetric method, GI50 = 0.02 μM. | 23313638 | |||
| St-4 | Growth inhibition assay | Growth inhibition of human St-4 cells by sulforhodamine B colorimetric method, GI50 = 0.022 μM. | 23313638 | |||
| HCT15 | Growth inhibition assay | Growth inhibition of human HCT15 cells by sulforhodamine B colorimetric method, GI50 = 0.45 μM. | 23313638 | |||
| CD4+ T | Function assay | 7 days | Reactivation of latent HIV1 NL4-3-Luc expression in human naive CD4+ T cells treated 7 days post-infection measured after 48 hrs by luminescence plate reader analysis, EC50 = 0.003 μM. | 24495105 | ||
| NCI-H522 | Cytotoxicity assay | Cytotoxicity against human NCI-H522 cells by SRB assay, GI50 = 0.0018 μM. | 24589486 | |||
| LOXIMVI | Cytotoxicity assay | Cytotoxicity against human LOXIMVI cells by SRB assay, GI50 = 0.0025 μM. | 24589486 | |||
| A549 | Cytotoxicity assay | Cytotoxicity against human A549 cells by SRB assay, GI50 = 0.0026 μM. | 24589486 | |||
| OVCAR5 | Cytotoxicity assay | Cytotoxicity against human OVCAR5 cells by SRB assay, GI50 = 0.0028 μM. | 24589486 | |||
| NCI-H460 | Cytotoxicity assay | Cytotoxicity against human NCI-H460 cells by SRB assay, GI50 = 0.003 μM. | 24589486 | |||
| MKN74 | Cytotoxicity assay | Cytotoxicity against human MKN74 cells by SRB assay, GI50 = 0.003 μM. | 24589486 | |||
| HCC2998 | Cytotoxicity assay | Cytotoxicity against human HCC2998 cells by SRB assay, GI50 = 0.0031 μM. | 24589486 | |||
| HCT116 | Cytotoxicity assay | Cytotoxicity against human HCT116 cells by SRB assay, GI50 = 0.0031 μM. | 24589486 | |||
| MKN1 | Cytotoxicity assay | Cytotoxicity against human MKN1 cells by SRB assay, GI50 = 0.0032 μM. | 24589486 | |||
| HT-29 | Cytotoxicity assay | Cytotoxicity against human HT-29 cells by SRB assay, GI50 = 0.0033 μM. | 24589486 | |||
| SKOV3 | Cytotoxicity assay | Cytotoxicity against human SKOV3 cells by SRB assay, GI50 = 0.0033 μM. | 24589486 | |||
| KM12 | Cytotoxicity assay | Cytotoxicity against human KM12 cells by SRB assay, GI50 = 0.0034 μM. | 24589486 | |||
| SF539 | Cytotoxicity assay | Cytotoxicity against human SF539 cells by SRB assay, GI50 = 0.0036 μM. | 24589486 | |||
| 293T | Function assay | 30 mins | Inhibition of human HDAC1 expressed in human 293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay, IC50 = 0.0036 μM. | 24589486 | ||
| DMS114 | Cytotoxicity assay | Cytotoxicity against human DMS114 cells by SRB assay, GI50 = 0.0036 μM. | 24589486 | |||
| U251 | Cytotoxicity assay | Cytotoxicity against human U251 cells by SRB assay, GI50 = 0.0039 μM. | 24589486 | |||
| SF295 | Cytotoxicity assay | Cytotoxicity against human SF295 cells by SRB assay, GI50 = 0.004 μM. | 24589486 | |||
| MCF7 | Cytotoxicity assay | Cytotoxicity against human MCF7 cells by SRB assay, GI50 = 0.0042 μM. | 24589486 | |||
| OVCAR3 | Cytotoxicity assay | Cytotoxicity against human OVCAR3 cells by SRB assay, GI50 = 0.0046 μM. | 24589486 | |||
| NCI-H23 | Cytotoxicity assay | Cytotoxicity against human NCI-H23 cells by SRB assay, GI50 = 0.0046 μM. | 24589486 | |||
| SF268 | Cytotoxicity assay | Cytotoxicity against human SF268 cells by SRB assay, GI50 = 0.0049 μM. | 24589486 | |||
| MKN7 | Cytotoxicity assay | Cytotoxicity against human MKN7 cells by SRB assay, GI50 = 0.0049 μM. | 24589486 | |||
| OVCAR8 | Cytotoxicity assay | Cytotoxicity against human OVCAR8 cells by SRB assay, GI50 = 0.0055 μM. | 24589486 | |||
| MDA-MB-231 | Cytotoxicity assay | Cytotoxicity against human MDA-MB-231 cells by SRB assay, GI50 = 0.0055 μM. | 24589486 | |||
| DMS273 | Cytotoxicity assay | Cytotoxicity against human DMS273 cells by SRB assay, GI50 = 0.0058 μM. | 24589486 | |||
| DU145 | Cytotoxicity assay | Cytotoxicity against human DU145 cells by SRB assay, GI50 = 0.006 μM. | 24589486 | |||
| RXF631L | Cytotoxicity assay | Cytotoxicity against human RXF631L cells by SRB assay, GI50 = 0.0066 μM. | 24589486 | |||
| HBC4 | Cytotoxicity assay | Cytotoxicity against human HBC4 cells by SRB assay, GI50 = 0.0069 μM. | 24589486 | |||
| SNB75 | Cytotoxicity assay | Cytotoxicity against human SNB75 cells by SRB assay, GI50 = 0.0072 μM. | 24589486 | |||
| BSY1 | Cytotoxicity assay | Cytotoxicity against human BSY1 cells by SRB assay, GI50 = 0.0085 μM. | 24589486 | |||
| NCI-H226 | Cytotoxicity assay | Cytotoxicity against human NCI-H226 cells by SRB assay, GI50 = 0.0089 μM. | 24589486 | |||
| SNB78 | Cytotoxicity assay | Cytotoxicity against human SNB78 cells by SRB assay, GI50 = 0.0096 μM. | 24589486 | |||
| HBC5 | Cytotoxicity assay | Cytotoxicity against human HBC5 cells by SRB assay, GI50 = 0.013 μM. | 24589486 | |||
| MKN45 | Cytotoxicity assay | Cytotoxicity against human MKN45 cells by SRB assay, GI50 = 0.014 μM. | 24589486 | |||
| MKN28 | Cytotoxicity assay | Cytotoxicity against human MKN28 cells by SRB assay, GI50 = 0.017 μM. | 24589486 | |||
| PC3 | Cytotoxicity assay | Cytotoxicity against human PC3 cells by SRB assay, GI50 = 0.018 μM. | 24589486 | |||
| ACHN | Cytotoxicity assay | Cytotoxicity against human ACHN cells by SRB assay, GI50 = 0.02 μM. | 24589486 | |||
| OVCAR4 | Cytotoxicity assay | Cytotoxicity against human OVCAR4 cells by SRB assay, GI50 = 0.02 μM. | 24589486 | |||
| St-4 | Cytotoxicity assay | Cytotoxicity against human St-4 cells by SRB assay, GI50 = 0.022 μM. | 24589486 | |||
| 293T | Function assay | 30 mins | Inhibition of mouse HDAC6 expressed in human 293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay, IC50 = 0.39 μM. | 24589486 | ||
| HCT15 | Cytotoxicity assay | Cytotoxicity against human HCT15 cells by SRB assay, GI50 = 0.45 μM. | 24589486 | |||
| mink Mv1Lu | Function assay | 24 hrs | Increase in human wild type p21 protein expression in mink Mv1Lu cells after 24 hrs by p21 promoter assay in presence of 0.1 mM dithiothreitol, EC1000 = 0.0157 μM. | 24997578 | ||
| HCT116 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HCT116 cells after 48 hrs in presence of DTT by MTT assay, IC50 = 0.003 μM. | 25147612 | ||
| MOLT4 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay, GI50 = 0.00206 μM. | 26331334 | ||
| DU145 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay, GI50 = 0.00255 μM. | 26331334 | ||
| U937 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay, GI50 = 0.00341 μM. | 26331334 | ||
| HLF | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HLF cells after 72 hrs by CCK8 assay, GI50 = 0.00489 μM. | 26331334 | ||
| WI38 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human WI38 cells after 72 hrs by CCK8 assay, GI50 = 0.00539 μM. | 26331334 | ||
| U937 | Function assay | 24 hrs | Inhibition of HDAC6 in human U937 cells assessed as reduction of alpha-tubilin acetylation at 5 nM to 5 uM after 24 hrs by Western blot analysis | 26331334 | ||
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.028 μM. | 26481659 | ||
| IGROV1/Pt1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human IGROV1/Pt1 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.08 μM. | 26481659 | ||
| IGROV1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human IGROV1 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.22 μM. | 26481659 | ||
| Haga clic para ver más datos experimentales de líneas celulares | ||||||
Información química, almacenamiento y estabilidad
| Peso molecular | 540.7 | Fórmula | C24H36N4O6S2 |
Almacenamiento (Desde la fecha de recepción) | |
|---|---|---|---|---|---|
| Nº CAS | 128517-07-7 | -- | Almacenamiento de soluciones madre |
|
|
| Sinónimos | FK228, Depsipeptide, FR 901228, NSC 630176, | Smiles | CC=C1C(=O)NC(C(=O)OC2CC(=O)NC(C(=O)NC(CSSCCC=C2)C(=O)N1)C(C)C)C(C)C | ||
Solubilidad
|
In vitro |
DMSO
: 10 mg/mL
(18.49 mM)
Water : Insoluble Ethanol : Insoluble |
Calculadora de Molaridad
Calculadora de Dilución
Calculadora de Peso Molecular
|
In vivo |
|||||
Calculadora de formulación in vivo (Solución clara)
Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)
mg/kg
g
μL
Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Resultados del cálculo:
Concentración de trabajo: mg/ml;
Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )
Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH2O, mezclar y clarificar.
Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.
Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.
Mecanismo de acción
| Características |
More effective than other classical HDAC inhibitors such as TSA, TPX, and butyrate.
|
|---|---|
| Targets/IC50/Ki |
HDAC1
(Cell-free assay) 36 nM
HDAC2
(Cell-free assay) 47 nM
|
| In vitro |
A diferencia de TSA, la forma activa redFK de Romidepsin inhibe fuertemente HDAC1 y HDAC2 con IC50 de 1,6 nM y 3,9 nM, respectivamente, pero es relativamente débil para inhibir HDAC4 y HDAC6 con IC50 de 25 nM y 790 nM, respectivamente. Este compuesto es 17-23 veces más débil que redFK en la inhibición de estas HDACs con IC50 de 36 nM, 47 nM, 510 nM y 14 μM, respectivamente. El tratamiento con este químico en células HeLa induce la acetilación de histonas y la expresión de p21 con EC50 de 3,0 nM, más fuertemente que redFK con EC50 de 11 nM debido a la inestabilidad de redFK. Además de la detención en G2/M, este compuesto causa la regulación a la baja de la ciclina D1 y una inducción de p21 independiente de p53, lo que lleva a la inhibición de CDK y la desfosforilación de Rb, lo que resulta en la detención del crecimiento en la fase G1 temprana. Es 100 veces más potente que TSA y 1.000.000 de veces más potente que el butirato en la inhibición de la proliferación de las células A549. Este agente inhibe el crecimiento de las células U-937, K562 y CCRF-CEM con IC50 de 5,92 nM, 8,36 nM y 6,95 nM, respectivamente. Promueve la apoptosis en células de leucemia linfocítica crónica (LLC) a una concentración correspondiente a aquella en la que ocurre la acetilación de H3 y H4 y la inhibición de HDAC, involucrando selectivamente la activación de la caspasa 8 y la caspasa efectora 3, así como la regulación a la baja de la proteína c-FLIP. En 11 de 13 (85%) líneas celulares de carcinoma de células renales y en 16 de 37 (43%) otras líneas celulares cancerosas, este compuesto regula al alza los receptores de muerte tumoral y potencia la destrucción tumoral mediada por células asesinas naturales (NK). Exhibe citotoxicidad dependiente de la concentración contra un panel de líneas celulares de linfoma de células del manto (LCM).
|
| Ensayo de quinasa |
Actividad inhibidora de HDAC
|
|
Para el ensayo enzimático, se añaden 10 μL de histonas marcadas con [3H]acetilo (25.000 cpm/10 μg) a 90 μL de la fracción enzimática HDAC extraída de células 293T que sobreexpresan HDAC1 o HDAC2 en presencia de concentraciones crecientes de Romidepsin, y la mezcla se incuba a 37 °C durante 15 minutos. La reacción enzimática es lineal durante al menos 1 hora. La reacción se detiene añadiendo 10 μL de HCl concentrado. El ácido [3H]acético liberado se extrae con 1 mL de acetato de etilo, y 0,9 mL de la capa de disolvente se transfieren a 5 mL de solución de centelleador acuoso II para la determinación de la radioactividad. Los valores de IC50 se determinan a partir de al menos tres curvas dosis-respuesta independientes.
|
|
| In vivo |
El tratamiento con Romidepsin inhibe potentemente la neovascularización del embrión de pollo y la de ratones adultos en el ensayo de tapón de Matrigel. La administración de este compuesto a 0,1-1 mg/kg dos veces por semana prolonga significativamente la supervivencia de ratones portadores de linfoma U-937, con tiempos de supervivencia medianos de 30,5 (0,56 mg/kg) y 33 días (0,32 mg/kg), respectivamente (frente a 20 días en ratones control).
|
Referencias |
|
Aplicaciones
| Métodos | Biomarcadores | Imágenes | PMID |
|---|---|---|---|
| Western blot | p21 / Cyclin D1 AcH3(K9) / Ac-α-Tubulin(K40) / Ac-NFκB2(K310) p65 / 3MeH3(K27) HDAC3 / HDAC4 / HDAC6 / HDAC2 γH2AX / PARP1 / Cleaved caspase3 / BAK / p21(waf1/cip1) / XIAP Cyclin E1 / BRCA1 / E2F1 / Cleaved PARP / H3Ac pAKT(S473) / pAKT(T308) / AKT |
|
19682393 |
| Growth inhibition assay | Cell viability |
|
27444036 |
| Immunofluorescence | SS18/TLE1 Cleaved caspase-3 |
|
27120803 |
Información del ensayo clínico
(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)
| Número NCT | Reclutamiento | Condiciones | Patrocinador/Colaboradores | Fecha de inicio | Fases |
|---|---|---|---|---|---|
| NCT03770000 | Completed | T Cell Lymphoma |
Rhizen Pharmaceuticals SA |
March 12 2019 | Phase 1|Phase 2 |
| NCT02616965 | Active not recruiting | Cutaneous T-cell Lymphoma (CTCL) |
Fox Chase Cancer Center|Seagen Inc.|Celgene Corporation |
February 22 2017 | Phase 1 |
| NCT02616874 | Completed | HIV |
IrsiCaixa|Germans Trias i Pujol Hospital|Fundación FLS de Lucha Contra el Sida las Enfermedades Infecciosas y la Promoción de la Salud y la Ciencia|Hospital Clinic of Barcelona|Hospital de Sant Pau|HIVACAT|University of Oxford|BCN Checkpoint |
February 2016 | Phase 1 |
Soporte técnico
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