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Chemical Structure : Avapritinib
CAS No.: 1703793-34-3
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $148 | In stock | |
| 10 mg | $198 | In stock | |
| 25 mg | $328 | In stock | |
| 50 mg | $528 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 498.57 | |
| Formula | C26H27FN10 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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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.
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