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Chemical Structure : BLU-667
CAS No.: 2097132-94-8
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $88 | In stock | |
| 10 mg | $128 | In stock | |
| 25 mg | $198 | In stock | |
| 50 mg | $328 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 533.612 | |
| Formula | C27H32FN9O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
100 mM in DMSO (53.3 mg/mL) |
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| 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 |
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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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