BLU-285

Ingoa matū:

(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)pirimidin-5-yl)ethana-1-amine

Waehere 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

Waehere 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)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

Kī InChi:

DWYRIWUZIJHQKQ-SANMLTNESA-N

Kupumatua:

BLU-285, BLU 285, BLU285, Avapritinib

Wairewa:Wairewa i roto i te DMSO

Rokiroki:0 - 4°C mo te wa poto (ra ki nga wiki), -20°C ranei mo te wa roa (marama).

Whakaahuatanga:

Kua whakaatu a Avapritinib (BLU-285) i te mahi koiora in vitro i runga i te KIT exon 17 mutant enzyme, KIT D816V (IC50=0.27 nM). Ko te mahi pūtau o Avapritinib i runga i te KIT D816 mutants ka inehia e te autophosphorylation i roto i te mast cell leukemia cell line HMC1.2, me te P815 kiore mastocytoma cell line ki te IC50=4 me te 22 nM, ia. I roto i nga pūtau Kasumi-1, i te (8; 21) -pai te raina pūtau AML me te KIT exon 17 N822K te whakarereketanga, ka kaha te whakakore a Avapritinib i te KIT N822K autophosphorylation mutant (IC50 = 40 nM), te tohu o raro, me te tipu o te pūtau (IC50=). 75 nM)[1].

Whāinga: KIT