[CAS NO. 1703793-34-3] Avapritinib (BLU-285)
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PRODUCTS SPECIFICATIONS [1703793-34-3]
Store
Catalog
SLK-S8553
Brand
Selleck
CAS
1703793-34-3
DESCRIPTION [1703793-34-3]
Overview
| MDL | MFCD31544325 |
|---|---|
| Molecular Weight | 498.56 |
| Molecular Formula | C26H27FN10 |
| SMILES | N[C@@](C)(C1=CC=C(F)C=C1)C2=CN=C(N3CCN(C4=NC=NN5C4=CC(C6=CN(C)N=C6)=C5)CC3)N=C2 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Description
Avapritinib (BLU-285) is a small molecule kinase inhibitor that potently inhibits mutant activity in vitro (IC50 = 0.5 nM) and PDGFRα D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogous mutation, D816V in Kit (c-Kit) Exon 17 (IC50 = 0.5 nM).
In vitro
BLU-285 is a selective oral inhibitor that targets KIT Exon 17 and PDGFRα D842 activation loop mutants. Cellular assays measuring inhibition of KIT mutant autophosphorylation confirm the activity of BLU-285 against the KIT D816 mutants D816V (HMC1.2 cells, IC50 = 3 nM) and D816Y (P815 cells, IC50 = 22 nM) as well as other KIT Exon 17 mutants such as N822K (Kasumi cells, IC50 = 40 nM) found in treatment-refractory GIST.
References
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