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.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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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. |
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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. |
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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. |
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V69650 | BCR-ABL-IN-8 | 1808288-49-4 | BCR-ABL-IN-8 (compound 26f) is a BCR-ABL inhibitor containing trimethoxy group. |
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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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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. |
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