A dual inhibitor of KIT and PDGFRα mutant kinases
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BLU-285

Item No. 22985

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(αS)-(4-fluorophenyl)-α-methyl-2-[4-[6-(1-methyl-1H-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]-1-piperazinyl]-5-pyrimidinemethanamine
CAS Number
1703793-34-3
Synonyms
  • Avapritinib
Molecular Formula
C26H27FN10
Formula Weight
498.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 66 mg/mlEthanol: 3 mg/ml
λmax
254, 309 nm
SMILES
C[C@@](C1=CC=C(F)C=C1)(N)C(C=N2)=CN=C2N3CCN(C4=NC=NN5C4=CC(C6=CN(C)N=C6)=C5)CC3
InChi Code
InChI=1S/C26H27FN10/c1-26(28,20-3-5-22(27)6-4-20)21-13-29-25(30-14-21)36-9-7-35(8-10-36)24-23-11-18(16-37(23)33-17-31-24)19-12-32-34(2)15-19/h3-6,11-17H,7-10,28H2,1-2H3/t26-/m0/s1
InChi Key
DWYRIWUZIJHQKQ-SANMLTNESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    BLU-285 is a dual inhibitor of KIT receptor and platelet-derived growth factor receptor α (PDGFRα) tyrosine kinases with activating loop mutations (IC50s = 0.27 and 0.24 nM for KITD816V and PDGFRαD842V, respectively).1 It is >150-fold selective for KITD816V and PDGFRαD842V over a kinase panel at a concentration of 3 μM. BLU-285 also has activity against a panel of KIT and PDGFRα loop mutants identified in patients with gastrointestinal stromal tumors (GISTs; IC50s = <100 nM). It inhibits growth of cancer cell lines containing wild-type and mutant KIT and PDGFRα, demonstrating increased potency in cell lines expressing KIT and PDGFRα with activating loop mutations. BLU-285 (0.3-30 mg/kg) reduces tumor volume in a P815 KITD814Y mastocytoma allograft mouse model and a GIST patient-derived mouse xenograft model in a dose-dependent manner. Formulations containing BLU-285 have been used to treat KIT- and PDGFRα-driven malignancies.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Evans, E.K., Gardino, A.K., Kim, J.L., et al. A precision therapy against cancers driven by KIT/PDGFRA mutations. Sci. Transl. Med. 9(414), eaao1690 (2017).