Avapritinib (Standard)

Avapritinib (Standard) is the analytical standard of Avapritinib. This product is intended for research and analytical applications. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2[1][2].

Product Specifications

CAS Number

[1703793-34-3]

Product Name Alternative

BLU-285 (Standard)

UNSPSC

12352005

Target

C-Kit; PDGFR; Reference Standards

Type

Reference Standards

Related Pathways

Others; Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/avapritinib-standard.html

Smiles

CN1N=CC(C2=CN3C(C(N4CCN(C5=NC=C([C@@](C)(N)C6=CC=C(F)C=C6)C=N5)CC4)=NC=N3)=C2)=C1

Molecular Formula

C26H27FN10

Molecular Weight

498.56

References & Citations

[1]Wu CP, et al. Avapritinib: A Selective Inhibitor of KIT and PDGFRα that Reverses ABCB1 and ABCG2-MediatedMultidrug Resistance in Cancer Cell Lines. Mol Pharm. 2019 Jul 1;16 (7) :3040-3052.|[2]Evans EK, et al. A precision therapy against cancers driven by KIT/PDGFRA mutations. Sci Transl Med. 2017 Nov 1;9 (414) . pii: eaao1690.|[3]Erica Evans, et al. Blu-285, a Potent and Selective Inhibitor for Hematologic Malignancies with KIT Exon 17 Mutations.Blood 2015 126:568.