Name | PND-1186 |
Synonyms | SR2516 SR 2516 SR-2516 PND1186 VS-4718 PND 1186 PND-1186 PND-1186 (VS-4718) |
CAS | 1061353-68-1 |
Molecular Formula | C25H26F3N5O3 |
Molar Mass | 501.5 |
Density | 1.334±0.06 g/cm3(Predicted) |
Boling Point | 654.0±55.0 °C(Predicted) |
pKa | 14.58±0.46(Predicted) |
Storage Condition | -20℃ |
In vitro study | In vitro, PND-1186 inhibited 4T1 breast cancer motility, promoted 4T1 apoptosis under suspension conditions, and reduced 4T1 soft agar colony number and size. In Hcy and OVCAR8 cells, VS-4718 promoted G0-G1 cell cycle arrest leading to cell death. |
In vivo study | In mice bearing 4T1 tumors, PND-1186(100 mg/kg s.c.) inhibited 4T1 subcutaneous tumor growth by inducing apoptosis. In mice bearing ID8 tumors, PND-1186 (0.5 mg/mL ,p.o.) also resulted in growth inhibition of ovarian cancer tumors. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.994 ml | 9.97 ml | 19.94 ml |
5 mM | 0.399 ml | 1.994 ml | 3.988 ml |
10 mM | 0.199 ml | 0.997 ml | 1.994 ml |
5 mM | 0.04 ml | 0.199 ml | 0.399 ml |
biological activity | PND-1186 (VS-4718, SR-2156) is a reversible and selective inhibitor of FAK, the IC50 was 1.5 nM. PND-1186 can selectively promote the apoptosis of tumor cells. Phase 1. |
Target | TargetValue FAK (Cell-free assay) 1.5 nM |
Target | Value |
FAK (Cell-free assay) | 1.5 nM |
in vitro study | in vitro, PND-1186 inhibits 4T1 breast cancer motility and promotes 4T1 apoptosis in suspension, and reduce the number and size of 4T1 soft agar colonies. In Hcy and OVCAR8 cells, VS-4718 promoted G0-G1 cell cycle arrest leading to cell death. |
in vivo study | in mice bearing 4T1 tumors, PND-1186(100 mg/kg s.c.) induced apoptosis, inhibition of 4T1 subcutaneous tumor growth. In mice bearing ID8 tumors, PND-1186 (0.5 mg/mL ,p.o.) also resulted in growth inhibition of ovarian cancer tumors. |