Vepafestinib

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].

Product Specifications

CAS Number

[2129515-96-2]

Product Name Alternative

TAS0953/HM06

UNSPSC

12352005

Target

Apoptosis; RET

Type

Reference compound

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/vepafestinib.html

Purity

98.61

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(C1=C(C#CCN2CCOCC2)N(C3(C)CC3)C4=NC=NC(N)=C41)NC5=CC=C(COC)C=C5

Molecular Formula

C26H30N6O3

Molecular Weight

474.55

References & Citations

[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. |[2]Vepafestinib: a RET-selective inhibitor with enhanced CNS penetrance targets therapy-resistant mutants. Nat Cancer. 2023 Sep;4 (9) :1220-1221.