Showing 4801–4816 of 5741 results

Momelotinib (CYT387)

Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Phase 3.

Torkinib (PP242)

Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM in cell-free assays targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively.

Mubritinib (TAK 165)

Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM in BT-474 cell no activity to EGFR, FGFR, PDGFR, JAK1, Src and Blk in BT-474 cell line. Phase 1.

DAPT (GSI-IX)

DAPT (GSI-IX) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells.

AZ 960

AZ 960 is a novel ATP competitive JAK2 inhibitor with IC50 and Ki of <3 nM and 0.45 nM, 3-fold selectivity of AZ960 for JAK2 over JAK3.

Formestane

Formestane is a second generation selective aromatase inhibitor with an IC50 of 80 nM.

PIK-293

PIK-293 is a PI3K inhibitor, mostly for PI3Kδ with IC50 of 0.24 μM, 500-, 100- and 50-fold less potent to PI3Kα/β/γ, respectively.

R788 (Fostamatinib) Disodium

R788 (Fostamatinib) disodium, a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM in a cell-free assay, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 3.

OSI-420

OSI-420 is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).

NVP-BHG712

NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.

BMS-794833

BMS-794833 is a potent ATP competitive inhibitor of Met/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nM a prodrug of BMS-817378. Phase 1.

SGI-1776 Free Base

SGI-1776 free base is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM in a cell-free assay, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. Phase 1.

A-966492

A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.

Dabigatran (BIBR 953)

Dabigatran (BIBR 953) is a potent nonpeptide thrombin inhibitor with an IC50 of 9.3 nM in a cell-free assay.