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Vepafestinib

CAT: 0804-HY-132846-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-132846-01Size:5 mg
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Description
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].
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.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2

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CatalogName
BA8998-5.1Vepafestinib

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