Avapritinib-d3

• Description:

  Avapritinib-d3 (BLU-285-d3) is deuterium labeled Avapritinib. 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 Name Alternative:

  BLU-285-d3

• UNSPSC:

  12352005

• Target:

  C-Kit; Isotope-Labeled Compounds; PDGFR

• Related Pathways:

  Others; Protein Tyrosine Kinase/RTK

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Smiles:

  C[C@] (N) (C1=CC=C (C=C1) F) C2=CN=C (N=C2) N (CC3) CCN3C4=NC=NN5C4=CC (C (C=N6) =CN6C ([2H]) ([2H]) [2H]) =C5

• Molecular Formula:

  C26H24D3FN10

• Molecular Weight:

  501.58

• References & Citations:

  [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]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.|[3]Evans EK, et al. A precision therapy against cancers driven by KIT/PDGFRA mutations. Sci Transl Med. 2017 Nov 1;9 (414) . pii: eaao1690.|[4]Erica Evans, et al. Blu-285, a Potent and Selective Inhibitor for Hematologic Malignancies with KIT Exon 17 Mutations.Blood 2015 126:568.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Isotope-Labeled Compounds

• Clinical Information:

  No Development Reported

• CAS Number:

  2408934-57-4