I-BLU-285
Imininingwane Yomkhiqizo
Omaka bomkhiqizo
| Usayizi Wephakethe | Ukutholakala | Intengo (USD) |
| 1g | Kukhona kusitoki | 900 |
| 5g | Kukhona kusitoki | 3600 |
| 10g | Kukhona kusitoki | 6200 |
| Osayizi abengeziwe | Thola Izingcaphuno | Thola Izingcaphuno |
Igama Lekhemikhali:
(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
Ikhodi ye-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
Ikhodi ye-InChi:
I-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
I-InChi Key:
DWYRIWUZIJHQKQ-SANMLTNESA-N
Igama elingukhiye:
BLU-285, BLU 285, BLU285, Avapritinib
Ukunyibilika:I-Soluble ku-DMSO
Isitoreji:0 - 4°C isikhathi esifushane (izinsuku ukuya emavikini), noma -20°C isikhathi eside (izinyanga).
Incazelo:
I-Avapritinib (BLU-285) ibonise umsebenzi we-biochemical in vitro ku-KIT exon 17 mutant enzyme, KIT D816V (IC50=0.27 nM). Umsebenzi weselula we-Avapritinib ku-KIT D816 eziguquguqukayo zikalwa nge-autophosphorylation kumugqa weseli we-mast cell leukemia HMC1.2, kanye nomugqa weseli we-P815 wegundane we-mastocytoma one-IC50=4 kanye no-22 nM, ngokulandelana. Kumaseli e-Kasumi-1, ku-(8;21) -positive AML cell line nokuguqulwa kwe-KIT exon 17 N822K, i-Avapritinib ivimbela ngamandla i-KIT N822K i-autophosphorylation eguquguqukayo (IC50=40 nM), ukusayinda phansi komfula, kanye nokwanda kwamaselula (IC50= 75 nM)[1].
Ithagethi: KIT
