BLU-285

Lub npe tshuaj:

(S)-1-(4-fluorophenyl)-1-(2-(4-(6-(1-methyl-1H-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4] [1] 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

Lo lus tseem ceeb:

BLU-285, BLU 285, BLU285, Avapritinib

Solubility:Soluble hauv DMSO

Cia:0 - 4 ° C rau lub sijhawm luv (hnub mus rau lub lis piam), lossis -20 ° C rau lub sijhawm ntev (hli).

Nqe lus piav qhia:

Avapritinib (BLU-285) tau qhia txog biochemical hauv vitro ua haujlwm ntawm KIT exon 17 mutant enzyme, KIT D816V (IC50 = 0.27 nM). Cellular kev ua ntawm Avapritinib ntawm KIT D816 mutants yog ntsuas los ntawm autophosphorylation nyob rau hauv tib neeg mast cell leukemia cell kab HMC1.2, thiab P815 nastocytoma cell kab nrog IC50 = 4 thiab 22 nM, feem. Hauv Kasumi-1 hlwb, ntawm (8; 21)-zoo AML kab ntawm tes nrog KIT exon 17 N822K kev hloov pauv, Avapritinib potently inhibits KIT N822K mutant autophosphorylation (IC50 = 40 nM), downstream signaling, as well as cellular proliferation (IC50 = 75 nM)[1].

Hom phiaj: KIT