Cas No.: | 1672665-49-4 |
Chemical Name: | PT 2385,PT-2385 |
Synonyms: | PT 2385,PT-2385 |
SMILES: | CS(=O)(=O)C1=C2[C@@H](C(CC2=C(C=C1)OC3=CC(=CC(=C3)C#N)F)(F)F)O |
Formula: | C17H12F3NO4S |
M.Wt: | 383.34 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | PT-2385 is a selective HIF-2α antagonist with a Ki of less than 50 nM. |
In Vivo: | PT-2385 (PT2385) inhibits expression of HIF-2α regulated genes in a dose dependent manner in vivo. Tumor is regressed with PT-2385 (3 and 10 mg/kg, p.o., b.i.d. dose) in 786-O xenograft. PT-2385 (1,3 and 10 mg/kg) also inhibits tumor-derived VEGFA protein levels. PT-2385 (10 mg/kg) treatment reduces proliferation (Ki67) and angiogenesis (CD-31)[1]. |
In Vitro: | PT-2385 (PT2385) is a selective antagonist of HIF-2 over HIF-1. PT-2385 is inactive for HIF-1α[1]. |