[CAS NO. 1073154-85-4] Defactinib (VS-6063)
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PRODUCTS SPECIFICATIONS [1073154-85-4]
Store
Catalog
SLK-S7654
Brand
Selleck
CAS
1073154-85-4
DESCRIPTION [1073154-85-4]
Overview
| MDL | MFCD25977806 |
|---|---|
| Molecular Weight | 510.49 |
| Molecular Formula | C20H21F3N8O3S |
| SMILES | O=C(NC)C1=CC=C(NC2=NC=C(C(F)(F)F)C(NCC3=NC=CN=C3N(C)S(=O)(C)=O)=N2)C=C1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9589 mL | 9.7945 mL | 19.5890 mL |
| 5 mM | 0.3918 mL | 1.9589 mL | 3.9178 mL |
| 10 mM | 0.1959 mL | 0.9795 mL | 1.9589 mL |
| 50 mM | 0.0392 mL | 0.1959 mL | 0.3918 mL |
Description
Defactinib (VS-6063, PF-04554878) is a selective, and orally active inhibitor. Phase 2.
Targets
| FAK [1] |
In vitro
In taxane-sensitive (SKOV3ip1) and taxane-resistant (SKOV3-TR) cell lines, VS-6063 significantly inhibits pFAK (Tyr397) expression. The combination of VS-6063 and paclitaxel synergistically decreases proliferation and increases apoptosis in SKOV3ip1, SKOV3-TR, HeyA8 and HeyA8-MDR cells. The combination of VS-6063 and Y15 synergistically decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines.
In vivo
In both PTX-sensitive and PTX-resistant models, VS-6063 (50 mg/kg p.o.) enhances tumor growth inhibition by paclitaxel.
References
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