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Avapritinib-d3

CAT: 0804-HY-W754911Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-W754911Size:1 Each
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
CAS Number
2408934-57-4
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

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