2408934-57-4
Chemical Structure
Avapritinib-d3
Synonym(s): BLU-285-d3
- CAS No.: 2408934-57-4
- Formula:C26H24D3FN10
- Molecular Weight:501.58
InChIKey: DWYRIWUZIJHQKQ-SVJJMHFFSA-N
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
Biological Activity: 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].
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Avapritinib-d3 | 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. | |||||||||||||||||||||
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Avapritinib (Standard) | ≥98% | 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. | ||||||||||||||||||||
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Avapritinib | 99.75% | 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. | ||||||||||||||||||||
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- [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [Content Brief]
- [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. [Content Brief]
