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首页-小分子抑制剂&激动剂-Tyrosine Kinase-RET Tyrosine Kinase (c-RET)-BLU-667
BLU-667

Chemical Structure : BLU-667

CAS No.: 2097132-94-8

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BLU-667 (Pralsetinib, BLU667)

货号: PC-63475Not For Human Use, Lab Use Only.

BLU-667 (Pralsetinib, BLU667) is a highly potent, selective, next generation RET inhibitor with IC50 of 0.3-0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion.

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10 mg ￥1280 In stock
25 mg ￥1980 In stock
50 mg ￥3280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: 98.57% (HPLC) Select Batch:

生物&药学活性

BLU-667 (Pralsetinib, BLU667) is a highly potent, selective, next generation RET inhibitor with IC50 of 0.3-0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion.
BLU-667 displays 8- to 28-fold more potent against WT RET than cabozantinib, vandetanib, and RXDX-105; shows 88-fold selectivity over VEGFR-2, >100-fold more selective for RET over 96% of kinases in a panel of 371 kinases.
BLU-667 inhibits RET autophosphorylation with cellular IC50 of 5 nM, at least 10 times more potently than cabozantinib, vandetanib, and RXDX-105.
BLU-667 inhibits phosphorylation of RET, SHC, and ERK1/2 in a panel of RET-driven cell lines at <10 nM, suppresses proliferation of KIF5B-RET Ba/F3 cells harboring V804L, V804M, or V804E variants as potently as WT RET.
BLU-667 demonstrates antitumor activity on diverse RET-driven in vivo models.

物理化学性质&存储条件

分子量 533.612
分子式 C27H32FN9O2
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

100 mM in DMSO (53.3 mg/mL)
Chemical Name/SMILES

(1s,4R)-N-((S)-1-(6-(4-fluoro-1H-pyrazol-1-yl)pyridin-3-yl)ethyl)-1-methoxy-4-(4-methyl-6-((5-methyl-1H-pyrazol-3-yl)amino)pyrimidin-2-yl)cyclohexane-1-carboxamide

参考文献

1. Subbiah V, et al. Cancer Discov. 2018 Apr 15. pii: CD-18-0338.

2. Piotrowska Z, et al. Cancer Discov. 2018 Dec;8(12):1529-1539.

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