Avapritinib (BLU-285) | mutant KIT/PDGFRα inhibitor | Probechem Biochemicals

Chemical Structure : Avapritinib

CAS No.: 1703793-34-3

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Avapritinib (BLU-285, BLU285)

货号: PC-62100Not For Human Use, Lab Use Only.

Avapritinib (BLU-285) is a potent and highly selective inhibitor of mutant KIT and PDGFRα with IC50 of 0.6, 0.27 and 0.24 nM for KIT del557-558, KIT D816V and PDGFRA D842V, respectively.

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5 mg	￥1280	In stock
10 mg	￥1980	In stock
25 mg	￥3480	In stock
50 mg	￥5280	In stock
100 mg		Get quote

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生物&药学活性

Avapritinib (BLU-285) is a potent and highly selective inhibitor of mutant KIT and PDGFRα with IC50 of 0.6, 0.27 and 0.24 nM for KIT del557-558, KIT D816V and PDGFRA D842V, respectively.
Avapritinib (BLU-285) displays weak inhibition against WT KIT with IC50 of 73 nM, >150-fold more potent on KIT D816V than several important kinase antitargets such as VEGFR2, SRC and FLT3.
Avapritinib (BLU-285) inhibits other well-characterized disease-driving KIT mutants both in vitro and in vivo in preclinical models.
Avapritinib (BLU-285) demonstrates marked activity in patients with diseases associated with KIT and PDGFRA (GIST) activation loop mutations.

物理化学性质&存储条件

分子量	498.57
分子式	C26H27FN10
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(1S)-1-(4-fluorophenyl)-1-[2-[4-[6-(1-methylpyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]piperazin-1-yl]pyrimidin-5-yl]ethanamine

参考文献

1. Cancer Discov. 2017 Dec 12. doi: 10.1158/2159-8290.

2. Evans EK, et al. Sci Transl Med. 2017 Nov 1;9(414). pii: eaao1690.

3. Cancer Discov. 2018 Jan;8(1):OF20. doi: 10.1158/2159-8290.

Avapritinib (BLU-285, BLU285)

生物&药学活性

物理化学性质&存储条件

参考文献

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Avapritinib (BLU-285, BLU285)

生物&药学活性

物理化学性质&存储条件

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