Exarafenib | pan-RAF inhibitor | Probechem Biochemicals

Chemical Structure : Exarafenib

CAS No.: 2639957-39-2

Exarafenib (KIN-2787, KIN2787)

Catalog No.: PC-21219Not For Human Use, Lab Use Only.

Exarafenib (KIN-2787) is a highly potent and selective pan-RAF inhibitor with IC50 of 2.4/3.5/1.4 nM for ARAF/BRAF/CRAF, respectively.

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Biological Activity

Exarafenib (KIN-2787) is a highly potent and selective pan-RAF inhibitor with IC50 of 2.4/3.5/1.4 nM for ARAF/BRAF/CRAF, respectively.

Exarafenib (KIN-2787) intercepts the RAF protein in the dimer compatible αC-helix-IN conformation.

Exarafenib (KIN-2787) displays a class-leading selectivity profile in a full kinase panel of >600 kinases.

Exarafenib (KIN-2787) inhibits pERK signaling in monomeric class I altered cell lines (A375 EC50 = 62 nM and Colo800 EC50 = 103 nM), dimer-driven class II altered cell lines (NCI-H2405 EC50 = 10 nM, BxPC-3 EC50 = 51 nM, and OV-90 EC50 = 26 nM) and heterodimer class III altered cell lines (WM3629 EC50 = 9 nM, and CAL-12T EC50 = 18 nM).

Exarafenib (KIN-2787) inhibits both protomers of BRAFWT dimer signaling in a cellular context, a dose dependent inhibition of pERK (EC50 = 265 nM).

Exarafenib (KIN-2787) (1.5, 3, 5, and 10 mg/kg twice daily) exhibited dose-dependent tumor growth inhibition (TGI) of 68%, 79%, 88%, and 118% respectively in BxPC-3 xenograft tumors.

Physicochemical Properties

M.Wt	521.59
Formula	C26H34F3N5O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(3S)-N-[3-[2-[[(1R)-2-Hydroxy-1-methylethyl]amino]-6-(4-morpholinyl)-4-pyridinyl]-4-methylphenyl]-3-(2,2,2-trifluoroethyl)-1-pyrrolidinecarboxamide

References

1. Tim S. Wang, et al. Cancer Res (2023) 83 (7_Supplement): 4927.

2. Patent WO2022226261 A1

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Exarafenib (KIN-2787, KIN2787)

Biological Activity

Physicochemical Properties

References

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