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Bcr-Abl

Bcr-Abl

Most patients with chronic myelogenous leukemia (CML) are treated in the first instance with Bcr-Abl tyrosine-kinase inhibitors (TKI). A chromosomal abnormality that results in the formation of a so-called Philadelphia chromosome is the root cause of more than 90% of CML cases. This abnormality results from the fusion of the break point cluster (Bcr) gene at chromosome 22 with the Abelson (Abl) tyrosine kinase gene at chromosome 9, creating a chimeric oncogene (Bcr-Abl) and a constitutively active Bcr-Abl tyrosine kinase that has been linked to the pathogenesis of CML. The tyrosine kinase has been selectively inhibited by substances.

Bcr-Abl related products

Structure Cat No. Product Name CAS No. Product Description
AP 24149 V69652 AP 24149 926922-29-4 AP 24149 is a potent Src-Abl dual (bifunctional) inhibitor (antagonist) with IC50s of 9.1 and 3.6 nM for Src and Abl respectively.
BCR-ABL-IN-10 V94424 BCR-ABL-IN-10 BCR-ABL-IN-10 (Compound B4) is a covalent aryl vinyl sulfate (AVS) inhibitor of BCR-ABL with IC50 of 43.1 nM for ABL kinase.
BCR-ABL-IN-3 V69651 BCR-ABL-IN-3 2240191-12-0 BCR-ABL-IN-3 is a potent and irreversible Bcr-Abl inhibitor (antagonist) with IC50 of ≤100 nM for Ba/F3Bcr-AblT3151.
BCR-ABL-IN-7 V69653 BCR-ABL-IN-7 688050-42-2 BCR-ABL-IN-7 (compound 4) is an inhibitor (blocker/antagonist) of WT and T315I mutant ABL kinase.
BCR-ABL-IN-8 V69650 BCR-ABL-IN-8 1808288-49-4 BCR-ABL-IN-8 (compound 26f) is a BCR-ABL inhibitor containing trimethoxy group.
cSRC/BCR-ABL1-IN-1 V94434 cSRC/BCR-ABL1-IN-1 cSRC/BCR-ABL1-IN-1 (Compound 16a) is a dual-target cSRC/BCR-ABL1 kinase inhibitor.
PDGFRα kinase inhibitor 2 V87986 PDGFRα kinase inhibitor 2 404844-11-7 PDGFRα kinase inhibitor 2 (compound 1) is an imatinib analogue and a covalent irreversible kinase inhibitor with IC50 values of 6.95 μM, 2.45 μM, and 1.39 μM for ABL1 wt, KIT wt, and PDGFRR wt, respectively.
PROTAC BCR-ABL1 ligand 1 V69654 PROTAC BCR-ABL1 ligand 1 2489876-34-6 PROTAC BCR-ABL1 ligand 1, compound GMB-475, is a ligand of a proteolysis-targeting chimera (PROTAC) that allosterically targets the BCR-ABL1 protein and recruits the E3 ligase Von Hippel-Lindau, resulting in Ubiquitination and subsequent degradation of BCR-ABL1 protein.
Tyrosine kinase-IN-8 V87987 Tyrosine kinase-IN-8 Tyrosine kinase-IN-8 (compound 4e) is a BCR-ABL1 tyrosine kinase inhibitor (TKI).
达沙替尼 V0629 Dasatinib (BMS354825; Sprycel) 302962-49-8 Dasatinib (formerly known as BMS-354825; sold under the brand name Sprycel), is a novel, potent and multi-targeted, orally bioavailable synthetic small molecule inhibitor that targets Abl, Src and c-Kitwith potential antitumor activity.
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