c-kit (wt)

Dasatinib (BMS-354825) is an orally active, ATP-competitive tyrosine kinase inhibitor that targets Src and Bcr-Abl (Ki=16 30 pM), with antitumor activity, used in the treatment of leukemia and lymphoma.

Dasatinib monohydrate (BMS-354825 Monohydrate) is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib monohydrate binds to and inhibits the growth-promoting activities of these kinases. Apparently, because of its less stringent binding affinity for the BCR-ABL kinase, Dasatinib monohydrate has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations.

Dasatinib hydrochloride (BMS-354825 HCl) (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib hydrochloride hydrochloride also induces Apoptosis and Autophagy.

c-Kit-IN-3 is a selective inhibitor of c-KIT kinase with IC50s of 4 nM and 8 nM for c-Kit (wt) and c-Kit (T670I).

JI6 (JAK3 Inhibitor VI) is a potent, selective and orally active FLT3 inhibitor. JI6 exhibits IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits c-Kit and JAK3, with IC50s of ∼500 and ∼250 nM, respectively. JI6 has research value in acute myeloid leukemia.

DCC-2036 (Rebastinib (DCC-2036)) is a conformational control Bcr-Abl inhibitor for Abl1(WT, IC50: 0.8 nM) and Abl1(T315I, IC50: 4 nM), also inhibits LYN, SRC, HCK, FGR, FLT3, KDR, and Tie-2, and low activity to c-Kit. Rebastinib aimed at the Angiopoietin2-Tie2 pathway.

c-Kit-IN-3 D-tartrate is a potent and selective c-KIT kinase inhibitor (IC50s: 4 nM, 8 nM for c-KIT wt, and c-KIT T670I).

c-Kit-IN-3 hydrochloride is a potent and selective c-KIT kinase inhibitor (IC50s: 4 nM, 8 nM for c-KIT wt, and c-KIT T670I).

c-Kit-IN-3 L-tartrate is a potent and selective c-KIT kinase inhibitor (IC50s: 4 nM, 8 nM for c-KIT wt, and c-KIT T670I).

c-Kit-IN-3 maleate is a potent and selective c-KIT kinase inhibitor (IC50s: 4 nM, 8 nM for c-KIT wt, and c-KIT T670I).

c-Kit-IN-3 tartrate is a potent and selective c-KIT kinase inhibitor (IC50s: 4 nM, 8 nM for c-KIT wt, and c-KIT T670I).

FLT3-IN-12 is a selective, potent, orally active FLT3 kinase inhibitor that acts on FLT3-WT (IC50: 1.48 nM) and FLT3-D835Y (IC50: 2.87 nM). FLT3-IN-12 is more selective than c-KIT (>1000-fold). FLT3-IN-12 showed significant anti-AML effects, with an IC50 value of 0.75 nM for MV4-11 cells.

Imatinib impurities3 is a protein kinases inhibitor with IC50 values of 6.95uM, 0.245uM, 0.139uM for ABL1 wt, KIT wt, PDGFRR wt, respectively.