BLU-285

Izina ryimiti:

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

Kode ya 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

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 Urufunguzo:

DWYRIWUZIJHQKQ-SANMLTNESA-N

Ijambo ryibanze:

BLU-285, BLU 285, BLU285, Avapritinib

Gukemura:Gukemura muri DMSO

Ububiko:0 - 4 ° C mugihe gito (iminsi kugeza ibyumweru), cyangwa -20 ° C mugihe kirekire (amezi).

Ibisobanuro:

Avapritinib (BLU-285) yerekanye biohimiki mubikorwa bya vitro kuri KIT exon 17 mutant enzyme, KIT D816V (IC50 = 0.27 nM). Ibikorwa bya selile ya Avapritinib kuri mutant ya KIT D816 bipimwa na autophosphorylation mumurongo wa selile ya mast selile yumuntu selile HMC1.2, hamwe nimbeba ya P815 mastocytoma selile hamwe na IC50 = 4 na 22 nM. Muri selile ya Kasumi-1, kuri (8; 21) -umurongo mwiza wa selile ya AML hamwe na KIT exon 17 N822K ihindagurika, Avapritinib irabuza cyane KIT N822K mutant autophosphorylation (IC50 = 40 nM), ibimenyetso byamanuka, hamwe no gukwirakwiza selile (IC50 = 75 nM) [1].

Intego: KIT