solo para uso en investigación
Cat. No.: S1159
| Líneas celulares | Tipo de ensayo | Concentración | Tiempo de incubación | Formulación | Descripción de la actividad | PMID |
|---|---|---|---|---|---|---|
| NCI-H1975 | Growth Inhibition Assay | 72 h | IC50=8 nM | 22144665 | ||
| NCI-H1975 | Growth Inhibition Assay | 48 h | IC50=16 nM | 22144665 | ||
| Calu-6 | Growth Inhibition Assay | IC50=64 nM | 23012248 | |||
| Calu-1 | Growth Inhibition Assay | IC50=58 nM | 23012248 | |||
| H2122 | Growth Inhibition Assay | IC50=53 nM | 23012248 | |||
| A549 | Growth Inhibition Assay | IC50=43 nM | 23012248 | |||
| H358 | Growth Inhibition Assay | IC50=29 nM | 23012248 | |||
| H1734 | Growth Inhibition Assay | IC50=28 nM | 23012248 | |||
| H727 | Growth Inhibition Assay | IC50=28 nM | 23012248 | |||
| COR-L23 | Growth Inhibition Assay | IC50=22 nM | 23012248 | |||
| H1792 | Growth Inhibition Assay | IC50=20 nM | 23012248 | |||
| H2009 | Growth Inhibition Assay | IC50=19 nM | 23012248 | |||
| SK-LU-1 | Growth Inhibition Assay | IC50=18 nM | 23012248 | |||
| H2212 | Growth Inhibition Assay | IC50=17 nM | 23012248 | |||
| H441 | Growth Inhibition Assay | IC50=14 nM | 23012248 | |||
| H2030 | Growth Inhibition Assay | IC50=12 nM | 23012248 | |||
| H23 | Growth Inhibition Assay | IC50=11 nM | 23012248 | |||
| HOP-62 | Growth Inhibition Assay | IC50=11 nM | 23012248 | |||
| IA-LM | Growth Inhibition Assay | IC50=10 nM | 23012248 | |||
| H460 | Growth Inhibition Assay | IC50=8 nM | 23012248 | |||
| H157 | Growth Inhibition Assay | IC50=7 nM | 23012248 | |||
| H1355 | Growth Inhibition Assay | IC50=5 nM | 23012248 | |||
| VCaP | Growth Inhibition Assay | IC50=7 nM | 23152004 | |||
| LNCaP | Growth Inhibition Assay | IC50=8 nM | 23152004 | |||
| Ramos-RA1 | Growth Inhibition Assay | IC50=7.4 nM | 23303741 | |||
| Karpas-299 | Growth Inhibition Assay | IC50=9.6 nM | 23303741 | |||
| Kasumi-1 | Growth Inhibition Assay | IC50=5.8 nM | 23303741 | |||
| CCRF-CEM (2) | Growth Inhibition Assay | IC50=7.2 nM | 23303741 | |||
| CCRF-CEM (1) | Growth Inhibition Assay | IC50=12.5 nM | 23303741 | |||
| MOLT-4 | Growth Inhibition Assay | IC50=10.6 nM | 23303741 | |||
| RS4;11 | Growth Inhibition Assay | IC50=13.5 nM | 23303741 | |||
| COG-LL-317 | Growth Inhibition Assay | IC50=4.4 nM | 23303741 | |||
| NALM-6 | Growth Inhibition Assay | IC50=11.7 nM | 23303741 | |||
| CHLA-136 | Growth Inhibition Assay | IC50=23.2 nM | 23303741 | |||
| CHLA-90 | Growth Inhibition Assay | IC50=22.3 nM | 23303741 | |||
| NB-EBc1 | Growth Inhibition Assay | IC50=16.8 nM | 23303741 | |||
| NB-1643 | Growth Inhibition Assay | IC50=7.4 nM | 23303741 | |||
| SJ-GBM2 | Growth Inhibition Assay | IC50=12.9 nM | 23303741 | |||
| CHLA-258 | Growth Inhibition Assay | IC50=6.4 nM | 23303741 | |||
| CHLA-10 | Growth Inhibition Assay | IC50=5.7 nM | 23303741 | |||
| CHLA-9 | Growth Inhibition Assay | IC50=4.6 nM | 23303741 | |||
| TC-71 | Growth Inhibition Assay | IC50=4.5 nM | 23303741 | |||
| CHLA-266 | Growth Inhibition Assay | IC50=27.1 nM | 23303741 | |||
| BT-12 | Growth Inhibition Assay | IC50=14.3 nM | 23303741 | |||
| Rh30 | Growth Inhibition Assay | IC50=5.6 nM | 23303741 | |||
| Rh18 | Growth Inhibition Assay | IC50=6.2 nM | 23303741 | |||
| Rh41 | Growth Inhibition Assay | IC50=10.4 nM | 23303741 | |||
| RD | Growth Inhibition Assay | IC50=8 nM | 23303741 | |||
| K033 | Apoptosis Assay | 100 nM | 72 h | significantly induces apoptosis | 23418523 | |
| M23 | Apoptosis Assay | 100 nM | 72 h | significantly induces apoptosis | 23418523 | |
| K029 | Apoptosis Assay | 100 nM | 72 h | significantly induces apoptosis | 23418523 | |
| K028 | Apoptosis Assay | 100 nM | 72 h | significantly induces apoptosis | 23418523 | |
| K008 | Apoptosis Assay | 100 nM | 72 h | significantly induces apoptosis | 23418523 | |
| K033 | Function Assay | 250 nM | 24 h | induces a modest increase in G1 population | 23418523 | |
| M23 | Function Assay | 250 nM | 24 h | induces G1 and G2/M arrest | 23418523 | |
| K029 | Function Assay | 250 nM | 24 h | induces G1 arrest | 23418523 | |
| K028 | Function Assay | 250 nM | 24 h | induces G2 arrest | 23418523 | |
| K008 | Function Assay | 250 nM | 24 h | induces G2 arrest | 23418523 | |
| K033 | Cell Viability Assay | IC50=75.5 nM | 23418523 | |||
| M23 | Cell Viability Assay | IC50=37.5 nM | 23418523 | |||
| K029 | Cell Viability Assay | IC50=46 nM | 23418523 | |||
| K028 | Cell Viability Assay | IC50=84 nM | 23418523 | |||
| K008 | Cell Viability Assay | IC50=60 nM | 23418523 | |||
| H3122 | Cell Viability Assay | 0-1000 nM | 72 h | IC50=10 nM | 23533265 | |
| H2228 | Cell Viability Assay | 0-1000 nM | 72 h | IC50=13 nM | 23533265 | |
| A1847 | Apoptosis Assay | 10-100 nM | 24/48/72 h | induces apoptosis time and dose dependently | 23900136 | |
| OVCAR-8 | Apoptosis Assay | 10-100 nM | 24/48/72 h | induces apoptosis time and dose dependently | 23900136 | |
| OVCAR-5 | Apoptosis Assay | 10-100 nM | 24/48/72 h | induces apoptosis time and dose dependently | 23900136 | |
| SKOV-3 | Cell Viability Assay | 0-1000 nM | 72 h | inhibits cell viability dose dependently | 23900136 | |
| A1847 | Cell Viability Assay | 0-1000 nM | 72 h | inhibits cell viability dose dependently | 23900136 | |
| OVCAR-8 | Cell Viability Assay | 0-1000 nM | 72 h | inhibits cell viability dose dependently | 23900136 | |
| OVCAR-5 | Cell Viability Assay | 0-1000 nM | 72 h | inhibits cell viability dose dependently | 23900136 | |
| H146 | Function Assay | 30 nM | 72 h | induces persistent G2/M phase arrest | 24166505 | |
| GLC4 | Function Assay | 30 nM | 72 h | induces persistent G2/M phase arrest | 24166505 | |
| H82 | Function Assay | 30 nM | 72 h | induces persistent G2/M phase arrest | 24166505 | |
| AC3 | Growth Inhibition Assay | IC50=25.9 nM | 24166505 | |||
| H1173 | Growth Inhibition Assay | IC50=12.62 nM | 24166505 | |||
| H792 | Growth Inhibition Assay | IC50=45.07 nM | 24166505 | |||
| H620 | Growth Inhibition Assay | IC50=32.67 nM | 24166505 | |||
| N592 | Growth Inhibition Assay | IC50=14.12 nM | 24166505 | |||
| H526 | Growth Inhibition Assay | IC50=21.64 nM | 24166505 | |||
| H187 | Growth Inhibition Assay | IC50=24.99 nM | 24166505 | |||
| H146 | Growth Inhibition Assay | IC50=28.51 nM | 24166505 | |||
| H128 | Growth Inhibition Assay | IC50=69.55 nM | 24166505 | |||
| H69 | Growth Inhibition Assay | IC50=83.36 nM | 24166505 | |||
| GLC4 | Growth Inhibition Assay | IC50=20.47 nM | 24166505 | |||
| H82 | Growth Inhibition Assay | IC50=30.27 nM | 24166505 | |||
| MDA-MB-231 | Function Assay | 100 nM | 24 h | inhibits the migratory and invasive capacity | 24173541 | |
| BT-20 | Function Assay | 100/250 nM | 24 h | resulted in a dose-dependent destabilization of EGFR, IGF-IR, MET, and CRAF | 24173541 | |
| MDA-MB-435 | Function Assay | 100 nM | 30 min | inhibits accumulation of HIF-1α | 24248265 | |
| MDA-MB-231 | Function Assay | 100 nM | 30 min | inhibits accumulation of HIF-1α | 24248265 | |
| HCC2998 | Growth Inhibition Assay | IC50=128 nM | 24682747 | |||
| SK-CO-1 | Growth Inhibition Assay | IC50=81 nM | 24682747 | |||
| LS-123 | Growth Inhibition Assay | IC50=73 nM | 24682747 | |||
| SNU-C2B | Growth Inhibition Assay | IC50=45 nM | 24682747 | |||
| LS-1034 | Growth Inhibition Assay | IC50=31 nM | 24682747 | |||
| LoVo | Growth Inhibition Assay | IC50=22 nM | 24682747 | |||
| COLO-678 | Growth Inhibition Assay | IC50=21 nM | 24682747 | |||
| NCI-H747 | Growth Inhibition Assay | IC50=17 nM | 24682747 | |||
| COLO-205 | Growth Inhibition Assay | IC50=14 nM | 24682747 | |||
| HCT 116 | Growth Inhibition Assay | IC50=14 nM | 24682747 | |||
| HuTu-80 | Growth Inhibition Assay | IC50=13 nM | 24682747 | |||
| HCT-15 | Growth Inhibition Assay | IC50=8 nM | 24682747 | |||
| SW620 | Growth Inhibition Assay | IC50=8 nM | 24682747 | |||
| LS-411 N | Growth Inhibition Assay | IC50=5 nM | 24682747 | |||
| RKO | Growth Inhibition Assay | IC50=4 nM | 24682747 | |||
| SW780 | Growth Inhibition Assay | IC50=3451 nM | 24784839 | |||
| RT4 | Growth Inhibition Assay | IC50=1733 nM | 24784839 | |||
| TCCSUP | Growth Inhibition Assay | IC50=142 nM | 24784839 | |||
| MGH-U3 | Growth Inhibition Assay | IC50=53 nM | 24784839 | |||
| HT-1197 | Growth Inhibition Assay | IC50=53 nM | 24784839 | |||
| 5637 | Growth Inhibition Assay | IC50=44 nM | 24784839 | |||
| 35612 | Growth Inhibition Assay | IC50=38 nM | 24784839 | |||
| KU-19-19 | Growth Inhibition Assay | IC50=36 nM | 24784839 | |||
| LB831-BLC | Growth Inhibition Assay | IC50=34 nM | 24784839 | |||
| UM-UC3 | Growth Inhibition Assay | IC50=33 nM | 24784839 | |||
| 647-V | Growth Inhibition Assay | IC50=27 nM | 24784839 | |||
| HT-1376 | Growth Inhibition Assay | IC50=21 nM | 24784839 | |||
| J82 | Growth Inhibition Assay | IC50=18 nM | 24784839 | |||
| BFTC | Growth Inhibition Assay | IC50=17 nM | 24784839 | |||
| SCaBER | Growth Inhibition Assay | IC50=10 nM | 24784839 | |||
| 639-V | Growth Inhibition Assay | IC50=10 nM | 24784839 | |||
| RT112 | Growth Inhibition Assay | IC50=9 nM | 24784839 | |||
| T24 | Growth Inhibition Assay | IC50=7 nM | 24784839 | |||
| SW-1710 | Growth Inhibition Assay | IC50=6 nM | 24784839 | |||
| DSH1 | Growth Inhibition Assay | IC50=6 nM | 24784839 | |||
| CAL27 | Cytoxicity Assay | 10/50 nM | 24 h | decreases cell proliferation dose dependently | 25205430 | |
| Detroit562 | Cytoxicity Assay | 10/50 nM | 24 h | decreases cell proliferation dose dependently | 25205430 | |
| FUDA | Cytoxicity Assay | 10/50 nM | 24 h | decreases cell proliferation dose dependently | 25205430 | |
| SCC25 | Cytoxicity Assay | 10/50 nM | 24 h | decreases cell proliferation dose dependently | 25205430 | |
| HT-29 | Function Assay | 50nM | 24 h | DMSO | induced G0/G1 arrest | 25210794 |
| HCT-116 | Function Assay | 50nM | 24 h | DMSO | induced G0/G1 arrest | 25210794 |
| MGC-803 | Function Assay | 0.1-1000 nM | 24 h | induces G2/M cell-cycle arrest | 25590805 | |
| MKN-28 | Cell Viability Assay | 0.1-1000 nM | 72 h | inhibits cell viability dose dependently | 25590805 | |
| SGC-7901 | Cell Viability Assay | 0.1-1000 nM | 72 h | inhibits cell viability dose dependently | 25590805 | |
| MGC-803 | Cell Viability Assay | 0.1-1000 nM | 72 h | inhibits cell viability dose dependently | 25590805 | |
| MV411 | Apoptosis Assay | 30/80/150/250 nM | 24/48/72 h | induces dose dependant induction of apoptosis | 25882550 | |
| HL60 | Apoptosis Assay | 30/80/150/250 nM | 24/48/72 h | induces dose dependant induction of apoptosis | 25882550 | |
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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 | |||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | |||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | |||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | |||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 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 | |||
| 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 | |||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 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 | |||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | |||
| Haga clic para ver más datos experimentales de líneas celulares | ||||||
| Peso molecular | 364.4 | Fórmula | C20H20N4O3 |
Almacenamiento (Desde la fecha de recepción) | |
|---|---|---|---|---|---|
| Nº CAS | 888216-25-9 | Descargar SDF | Almacenamiento de soluciones madre |
|
|
| Sinónimos | N/A | Smiles | CC(C)C1=C(C=C(C(=C1)C2=NNC(=O)N2C3=CC4=C(C=C3)N(C=C4)C)O)O | ||
|
In vitro |
DMSO
: 40 mg/mL
(109.76 mM)
Ethanol : 9 mg/mL Water : Insoluble |
|
In vivo |
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Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)
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.)
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.
| Targets/IC50/Ki |
HSP90
(OSA 8 cells) 4 nM
|
|---|---|
| In vitro |
Las concentraciones inhibitorias al 50% (IC50) para Ganetespib (STA-9090) contra líneas celulares de mastocitos malignos son 10-50 veces menores que las de 17-AAG, lo que indica que la clase de triazolona de inhibidores de HSP90 probablemente exhibe una mayor potencia que los inhibidores basados en geldanamicina. Este compuesto inhibe las líneas celulares MG63 con una IC50 de 43 nM. Se une al dominio de unión a ATP en el N-terminal de Hsp90 y sirve como un potente inhibidor de Hsp90 al causar la degradación de múltiples proteínas cliente oncogénicas de Hsp90, incluyendo HER2/neu, EGFR mutado, Akt, c-Kit, IGF-1R, PDGFRα, Jak1, Jak2, STAT3, STAT5, HIF-1α, CDC2 y c-Met, así como el tumor de Wilms 1. A bajas concentraciones nanomolares, detiene potentemente la proliferación celular e induce la apoptosis en una amplia variedad de líneas celulares de cáncer humano, incluidas muchas líneas celulares resistentes a inhibidores de tirosina quinasa y a tanespimicina. Exhibe una potente citotoxicidad en una variedad de líneas celulares tumorales sólidas y hematológicas, incluidas aquellas que expresan quinasas mutadas que confieren resistencia a inhibidores de tirosina quinasa de moléculas pequeñas. Su tratamiento causó rápidamente la degradación de proteínas cliente de Hsp90 conocidas, exhibe una potencia superior al inhibidor de ansamicina 17-AAG y muestra actividad sostenida incluso con tiempos de exposición cortos. En otro estudio, induce la apoptosis de líneas celulares de mastocitos malignos caninos. Es activo a concentraciones significativamente más bajas para mastocitos malignos caninos C2 y BR con IC50 de 19 y 4 nM, respectivamente, mientras que 17-AAG inhibe mastocitos malignos caninos C2 y BR con IC50 de 958 y 44 nM, respectivamente. Tanto la expresión de Kit WT como mutante se regulan a la baja por 100 nM de este compuesto después de 24 horas en todas las líneas tratadas, incluidas las células C2 y BMCMCs. Sin embargo, no se observan efectos sobre la expresión de PI3K o HSP90 después del tratamiento.
|
| In vivo |
La administración de Ganetespib (STA-9090) conduce a una reducción significativa del tamaño del tumor en varios modelos de xenoinjertos tumorales en ratones y parece ser menos tóxica. Además, este compuesto demostró una mejor penetración tumoral en comparación con tanespimicina. Inhibe el crecimiento tumoral in vivo tanto en modelos de xenoinjertos de mastocitos malignos como de OSA. Ganetespib inhibe significativamente el crecimiento tumoral cuando se dosifica con dos ciclos repetidos de 25 mg/kg/día durante 3 días, con un valor de %T/C de 18. Es bien tolerado, con los grupos vehículo y Ganetespib presentando cambios de peso corporal promedio con respecto al inicio del estudio de +0.3% y -8.1% en el día 17, respectivamente.
|
Referencias |
|
| Métodos | Biomarcadores | Imágenes | PMID |
|---|---|---|---|
| Western blot | EGFR / c-Met / IGF-1Rβ/ Akt / p-Akt / ERK / p-ERK |