Product Name

CEP-32496

General description

CEP-32496 is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2, respectively insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2.

Synonym

Agerafenib

Purity

≥98.5%(HPLC)

CAS Number

1188910-76-0

Formula

C²⁴H²²F³N⁵O⁵

Molecular Weight

517.46

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

Solid

Solubility(25°C)

DMSO

~5mg/mL

Ethanol

Insoluble

Water

Very slightly soluble

l  Biological Information

Biochem/Physiol  Actions

Agerafenib is an orally available v-raf murine sarcoma viral oncogene homolog B1 (B-raf) serine/threonine protein kinase inhibitor with potential antineoplastic activity. Agerafenib specifically and selectively inhibits the activity of the mutated form (V600E) of B-raf kinase. This inhibits the activation of the RAF/mitogen-activated protein kinase kinase (MEK)/extracellular signal-related kinase (ERK) signaling pathway and may result in a decrease in the proliferation of tumor cells expressing the mutated B-raf gene. The Raf mutation BRAF V600E, in which valine is substituted for glutamic acid at residue 600, is frequently found in a variety of human tumors and results in the constitutive activation of the RAF/MEK/ERK signaling pathway that regulates cellular proliferation and survival.

l  Storage

Storage temp.

-20°C

l  Precautions and Disclaimer

This product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov