Avapritinib - CAS 1703793-34-3
Catalog number: B0084-007732
Category: Inhibitor
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BLU-285 is a potent and selective inhibitor of exon 17 mutant KIT (IC50= 0.27 nM for KIT D816V). BLU-285 showed dose-dependent, robust anti-tumor efficacy in a TKI- resistant KIT exon 11/17 mutant GIST PDX model through inhibition of tumor growth, proliferation, KIT signaling and induction of apoptosis.
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B0084-007732 10 mg $199 In stock
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Brife Description:
inhibitor of exon 17 mutant KIT
(1S)-1-(4-fluorophenyl)-1-[2-[4-[6-(1-methylpyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]piperazin-1-yl]pyrimidin-5-yl]ethanamine; BLU-285; BLU 285; BLU285; UNII-513P80B4YJ; SCHEMBL16652297
DMSO:≥ 83.33 mg/mL
1.42±0.1 g/cm3
Canonical SMILES:
1.Structural and clinical consequences of activation loop mutations in class III receptor tyrosine kinases.
Klug LR;Kent JD;Heinrich MC Pharmacol Ther. 2018 Jun 28. pii: S0163-7258(18)30118-9. doi: 10.1016/j.pharmthera.2018.06.016. [Epub ahead of print]
Mutations within the activation loop of members of the class III receptor tyrosine kinase (RTK) subfamily, which includes KIT, PDGFRA, and FLT3, have been observed in multiple human tumor types. These mutations confer constitutive activation as well as resistance to the type II tyrosine kinase inhibitors (TKI) that are currently clinically available, such as imatinib and sunitinib. It is now understood that activation loop mutations in class III RTKs shift the activation state equilibrium away from inactive states, to which type II TKIs bind, to the active state by destabilizing the inactive conformation. Recently, type I TKIs, which can bind to active kinase conformations, have been developed with specificity for class III RTK members. Some type I TKIs, such as crenolanib and avapritinib (BLU-285), have entered clinical studies for patients with activation loop mutations in KIT, PDGFRA, or FLT3. Preliminary results suggest that these type I TKIs show activity in these patient populations that previously lacked effective treatments. This article reviews the inactive and active structures of KIT, PDGFRA, and FLT3, how the mutations seen in human cancers affect kinase structure, and the clinical implications of these mutations in terms of type I vs.
2.Kit Mutations: New Insights and Diagnostic Value.
Falchi L;Verstovsek S Immunol Allergy Clin North Am. 2018 Aug;38(3):411-428. doi: 10.1016/j.iac.2018.04.005. Epub 2018 Jun 9.
Mastocytosis is a World Health Organization-defined clonal mast cell disorder characterized by significant clinicopathologic heterogeneity. Despite this diversity, a mutation of the KIT gene, most commonly D816V, is found in almost all cases and believed a driver lesion. Peripheral blood allele-specific oligonucleotide polymerase chain reaction can reliably detect KIT D816V and is used for the initial screening of adults with suspected systemic mastocytosis. The discovery of KIT mutations as central to the pathobiology of mastocytosis has prompted development of KIT-targeted agents, including imatinib and midostaurin (approved medications for patients with advanced systemic mastocytosis), and drugs in development, like KIT D816V-specific inhibitor avapritinib.
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CAS 1703793-34-3 Avapritinib

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