src/abl tyrosine kinase inhibitor

Bosutinib (SKI-606) is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl (IC50: 1 nM) and Src (IC50: 1.2 nM) kinases.

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.

Bosutinib hydrate (SKI-606 hydrate) is an orally active and potent dual kinase inhibitor of BCR-ABL and Src tyrosine kinases for the study of Philadelphia Chromosome Positive Chronic Granulocytic Leukemia.

PD173955 is src family-selective tyrosine kinase inhibitor with IC50 of ~22 nM for Src, Yes and Abl kinase; less potent for FGFRα and no activity on InsR and PKC.

Dasatinib D8 is deuterium-labeled dasatinib. Dasatinib is a dual Bcr-Abl and Src family tyrosine kinase inhibitor.

XL228 is an inhibitor of multi-targeted tyrosine kinase (IC50s: 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src, and Lyn, respectively).

KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 (IC50: 6.6 nM), modestly effective to Bcr-Abl, FGFR1, and Aurora A; little inhibitory on PDGFRβ, IGF-1R, EGFR.

PD173952 is a tyrosine (Src) kinase and Myt1 inhibitor with antitumor activity, inhibits Lyn, Abl and Csk, and induces Bcr-Abl-dependent hematopoietic cell apoptosis.

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.

HG-7-85-01 is a novel ATP-competitive and type II tyrosine kinase inhibitor targeting both wild-type and watchman mutant BCR-ABL, PDGFRα, Kit, and Src kinases, with inhibitory effects on the proliferation of a variety of cancer cell lines, leading to G0/G1-phase blockade and apoptosis induction in BCR-ABL-expressing cells.

Debio 0617B is a multi-kinase inhibitor that reduces maintenance and self-renewal of primary human AML CD34+ stem/progenitor cells. debio 0617B targets key kinases upstream of STAT3/STAT5 signalling, such as JAK, ABL, SRC and class III/V receptor tyrosine kinases. debio 0617B can be used to study STAT3 driven solid tumours.

AP23464 represents a highly specialized ATP-based small molecule tyrosine kinase inhibitor specifically engineered to target the catalytic domain of Abl and Src kinases along with the Kit receptor with exceptional inhibitory potency and selectivity, effectively facilitating the measurable blockade of phosphorylation-mediated signaling across various preclinical experimental models to evaluate the suppression of oncogenic driver activities during strictly monitored laboratory observation periods and biochemical investigations to ensure high experimental sensitivity.

Dasatinib (Standard) is a reference standard for research and analysis in studies involving Dasatinib. Dasatinib (BMS-354825) is a tyrosine kinase inhibitor that inhibits Src and Bcr-Abl (Ki=16/30 pM) and is orally active and ATP-competitive. Dasatinib has antitumor activity and is used in the treatment of leukemia and lymphoma.