BLU-285

Orukọ Kemikali:

(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

KỌỌDỌ SMILES:

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

Koodu InChi:

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)2 4-23-11-18 (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

Bọtini InChi:

DWYRIWUZIJHQKQ-SANMLTNESA-N

Koko-ọrọ:

BLU-285, BLU 285, BLU285, Avapritinib

Solubility:Tiotuka ni DMSO

Ibi ipamọ:0 - 4°C fun igba kukuru (ọjọ si awọn ọsẹ), tabi -20°C fun igba pipẹ (osu).

Apejuwe:

Avapritinib (BLU-285) ti ṣe afihan iṣẹ ṣiṣe biochemical in vitro lori KIT exon 17 mutant enzyme, KIT D816V (IC50=0.27 nM). Iṣẹ ṣiṣe sẹẹli ti Avapritinib lori awọn ẹda KIT D816 jẹ iwọn nipasẹ autophosphorylation ninu laini sẹẹli mast cell leukemia cell HMC1.2, ati laini sẹẹli mastocytoma mouse P815 pẹlu IC50 = 4 ati 22 nM, lẹsẹsẹ. Ninu awọn sẹẹli Kasumi-1, ni (8; 21) laini sẹẹli AML rere pẹlu iyipada KIT exon 17 N822K, Avapritinib ni agbara ṣe idiwọ KIT N822K mutant autophosphorylation (IC50=40 nM), ifihan agbara isalẹ, bakanna bi ilọsiwaju cellular (IC50= 75 nM) [1].

Àfojúsùn: KIT