BLU-285

BLU-285
  • Name: BLU-285
  • Catalog No.: CPD1212
  • CAS No.: 1703793-34-3
  • Molecular Weight: 498.56
  • Chemical Formula: C26H27FN10
  • For scientific research only, not for patients.

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    Pack Size Availability Price (USD)
    10mg In stock 300
    50mg In stock 500
    100mg In stock 800
    More Sizes Get Quotes Get Quotes

    Chemical Name:

    (S)-1-(4-fluorophenyl)-1-(2-(4-(6-(1-methyl-1H-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl)piperazin-1-yl)pyrimidin-5-yl)ethan-1-amine

    SMILES Code: 

    CN1N=CC(C2=CN3C(C(N4CCN(C5=NC=C([C@@](C)(N)C6=CC=C(F)C=C6)C=N5)CC4)=NC=N3)=C2)=C1

    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

    Keyword:

    BLU-285, BLU 285, BLU285, Avapritinib

    Solubility: Soluble in DMSO

    Storage: 0 - 4°C for short term (days to weeks), or -20°C for long term (months).

    Description: 

    Avapritinib (BLU-285) has demonstrated biochemical in vitro activity on the KIT exon 17 mutant enzyme, KIT D816V (IC50=0.27 nM). Cellular activity of Avapritinib on KIT D816 mutants is measured by autophosphorylation in the human mast cell leukemia cell line HMC1.2, and the P815 mouse mastocytoma cell line with IC50=4 and 22 nM, respectively. In Kasumi-1 cells, a t(8;21)-positive AML cell line with a KIT exon 17 N822K mutation, Avapritinib potently inhibits KIT N822K mutant autophosphorylation (IC50=40 nM), downstream signaling, as well as cellular proliferation (IC50=75 nM)[1].

    Target: KIT




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