PX-478 2HCl

Defactinib (VS-6063) ^New

Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.

SU6656 ^New

SU 6656 is a selective Src family kinase inhibitor with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.

Dasatinib Monohydrate ^New

Dasatinib Monohydrate is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.

2-Methoxyestradiol (2-MeOE2)

2-Methoxyestradiol (2-MeOE2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. Phase 2.

Roxadustat (FG-4592)

Roxadustat (FG-4592) is an HIF-α prolyl hydroxylase inhibitor in a cell-free assay, stabilizes HIF-2 and induces EPO production. Phase 3.

IOX2

IOX2 is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM in a cell-free assay, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH.

BAY 87-2243

BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. Phase 1.

Ibrutinib (PCI-32765)

Ibrutinib (PCI-32765) is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.

Dasatinib

Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively.

Saracatinib (AZD0530)

Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Phase 2/3.

Features:The 1st Src inhibitor to show inhibition of the Src pathway in human tumor tissue.