2129515-96-2
Chemical Structure
Vepafestinib
Synonym(s): TAS0953/HM06
- CAS No.: 2129515-96-2
- Formula:C26H30N6O3
- Molecular Weight:474.55
IUPAC Name: 4-amino-N-(4-(methoxymethyl)phenyl)-7-(1-methylcyclopropyl)-6-(3-morpholinoprop-1-yn-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide
InChIKey: SFXVRNLGOSAWIV-UHFFFAOYSA-N
SMILES: O=C(C1=C(C#CCN2CCOCC2)N(C3(C)CC3)C4=NC=NC(N)=C41)NC5=CC=C(COC)C=C5
Biological Activity: Vepafestinib (TAS0953/HM06) is a next-generation brain-penetrant, selective and orally active RET inhibitor with an IC50 value of 0.33 nM. Vepafestinib inhibits the phosphorylation of RET and its downstream signaling pathways, thus blocking the growth and signal transduction of tumor cells and inducing cell cycle arrest and apoptosis. Vepafestinib can be used in the research of various RET-driven cancers, such as non-small cell lung cancer, thyroid cancer and other disease areas[1].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Vepafestinib | 98.61% | Vepafestinib (TAS0953/HM06) is a next-generation brain-penetrant, selective and orally active RET inhibitor with an IC50 value of 0.33 nM. Vepafestinib inhibits the phosphorylation of RET and its downstream signaling pathways, thus blocking the growth and signal transduction of tumor cells and inducing cell cycle arrest and apoptosis. Vepafestinib can be used in the research of various RET-driven cancers, such as non-small cell lung cancer, thyroid cancer and other disease areas. | ||||||||||||||||||||
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- [1]. Miyazaki I, et al. Vepafestinib is a pharmacologically advanced RET-selective inhibitor with high CNS penetration and inhibitory activity against RET solvent front mutations. Nat Cancer. 2023 Sep;4(9):1345-1361. doi: 10.1038/s43018-023-00630-y. Epub 2023 Sep 21. Erratum in: Nat Cancer. 2023 Oct;4(10):1526. [Content Brief]
Keywords
