BLU-285

Inoa Kimia:

(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

Code 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

Ki InChi:

DWYRIWUZIJHQKQ-SANMLTNESA-N

Hua'ōlelo:

BLU-285, BLU 285, BLU285, Avapritinib

Hiki ke hoʻoheheʻe:Hiki ke hoʻoheheʻe ʻia ma DMSO

Waihona:0 - 4°C no ka wā pōkole (nā lā i nā pule), a i ʻole -20°C no ka wā lōʻihi (mau mahina).

wehewehe:

Ua hōʻike ʻo Avapritinib (BLU-285) i ka hana biochemical in vitro ma ka KIT exon 17 mutant enzyme, KIT D816V (IC50=0.27 nM). ʻO ka hana kelepona o Avapritinib ma KIT D816 mutants ua ana ʻia e ka autophosphorylation i ka mast cell leukemia cell line HMC1.2, a me ka P815 mouse mastocytoma cell line me IC50 = 4 a me 22 nM, kēlā me kēia. Ma nā pūnaewele Kasumi-1, ma (8;21) -positive AML cell line me ka KIT exon 17 N822K mutation, Avapritinib potently inhibits KIT N822K mutant autophosphorylation (IC50 = 40 nM), downstream signaling, a me ka cellular proliferation (IC50=). 75 nM)[1].

Pahuhopu: KIT