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Selpercatinib
- LOXO-292
Axon 3195
CAS:
2152628-33-4
Purity:
99%
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C29H31N7O3
- MW: 525.6
Description
Selpercatinib is a potent, highly selective, ATP-competitive RET inhibitor with an IC50 value of 4 nM (KIF5B-RET). Selpercatinib demonstrated potent and selective anti-RET activity preclinically against human cancer cell lines harboring endogenous RET gene alterations.
More Information
| Parent CAS No. | 2152628-33-4 |
|---|---|
| Chemical Name | 6-(2-Hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile |
| SMILES | C1(OC)N=CC(CN2C3CC2CN(C2N=CC(C4C5=C(C#N)C=NN5C=C(OCC(O)(C)C)C=4)=CC=2)C3)=CC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C29H31N7O3/c1-29(2,37)18-39-24-9-25(28-21(10-30)13-33-36(28)17-24)20-5-6-26(31-12-20)34-15-22-8-23(16-34)35(22)14-19-4-7-27(38-3)32-11-19/h4-7,9,11-13,17,22-23,37H,8,14-16,18H2,1-3H3 |
| InChiKey | XIIOFHFUYBLOLW-UHFFFAOYSA-N |
| CID | 134436906 |
| Short Description | RET inhibitor |
References
- V Subbiah et al. Selective RET kinase inhibition for patients with RET-altered cancers. Ann Oncol. 2018 Aug; 29(8): 1869–1876.
- BH Durham et al. Activating mutations in CSF1R and additional receptor tyrosine kinases in histiocytic neoplasms. Nat Med. 2019;25(12):1839-1842.
- R Newton et al. Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RET V804M Kinase. ACS Med Chem Lett. 2020 Feb 28;11(4):497-505.
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