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KI0556CCT239065QuoteQuote

Chemical Characteristic

Product NameCCT239065
CAS No.1163719-51-4
Molecular Weight 555.7
FormulaC29H29N7O3S
SmilesN(C(=O)Nc1n(nc(c1)C(C)(C)C)c1ccc(cc1)C)c1c(cc(cc1)Oc1c2c([nH]c(=O)cn2)ncc1)SC
Chemical Structure

Biological activities

CCT239065 is a BRAFV600E inhibitor. The IC50 of CCT239065 is 13 nM against BRAFV600E. CCT239065 inhibits wild type BRAF with an IC50 of 81 nM. In contrast, CCT239065 prevents CRAF and LCK with IC50 of 12 and 6 nM, respectively. In addition, the IC50 of CCT239065 is 23 nM against SRC. CCT239065 inhibits signaling downstream of BRAFV600E in cancer cells, blocking DNA synthesis, and inhibiting proliferation. CCT239065 is more than 6 fold less active against wild type BRAF and more than 50 fold less active against VEGFR2/KDR than against BRAFV600E. CCT239065 inhibits the growth of cancer cell lines harboring V600D/EBRAF mutations, but is relatively ineffective in cell lines in which wild type BRAF. CCT239065 potently inhibits MEK and ERK phosphorylation in V600DBRAF WM266.4 cells. CCT239065 induces a profound increase in MEK and ERK phosphorylation and this is accompanied by increased cyclin D1 expression. The growth of established BRAFV600E A375M melanoma xenografts is reduced by p.o. administration of CCT239065 (20 mg/kg q.d.) for 24 days, with a significant growth inhibition of 50% on completion of the experiment.[1]

References

[1] Whittaker S, et al. A novel, selective, and efficacious nanomolar pyridopyrazinone inhibitor of V600EBRAF. Cancer Res. 2010, 70(20): 8036-8044.

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