CCT196969 MedChemExpress (MCE)

Product Name	CCT196969
Synonyms	CS-2447 CCT196969 CB93134226 CCT-196969 CCT 196969 1-(3-(tert-Butyl)-1-phenyl-1H-pyrazol-5-yl)-3-(2-fluoro-4-((3-oxo-3,4-dihydropyrido[2,3-b]pyra Urea, N-[4-[(3,4-dihydro-3-oxopyrido[2,3-b]pyrazin-8-yl)oxy]-2-fluorophenyl]-N'-[3-(1,1-dimethylethyl)-1-phenyl-1H-pyrazol-5-yl]-
CAS	1163719-56-9
EINECS
Chemical Formula	C27H24FN7O3
Molecular Weight	513.52
inchi
Package	10 mM * 1 mL;1 mg;5 mg;10 mg;25 mg;50 mg;100 mg
Price	Email to quote
Descriptions	CCT196969 CCT196969 MedChemExpress (MCE) HY-12846 1163719-56-9 99.36% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions CCT196969 CCT196969 MedChemExpress (MCE) HY-12846 1163719-56-9 99.36% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. CCT196969 is a pan-Raf inhibitor, which inhibits B-Raf, BRafV600E and CRAF with IC50s of 0.1, 0.04, and 0.01 μM, respectively. CCT196969 is a pan-Raf inhibitor with anti-SRC activity. CCT196969 is an orally available, well-tolerated B-Raf inhibitor that directly inhibits B-RafV600E in cells. CCT196969 inhibits B-Raf at 100 nM and B-RafV600E at 40 nM. It inhibits CRaf at 12 nM, SRC at 26 nM, and LCK at 14 nM. CCT196969 is active against melanoma and colorectal cancer cell lines that are mutant for B-Raf. CCT196969 induces caspase 3 and PARP cleavage, demonstrating that it induces apoptosis[1]. CCT196969 is extremely well tolerated and does not produce any significant adverse effects in vivo. It inhibits the growth of NRAS mutant DO4 tumor xenografts in nude mice. CCT196969 inhibits ERK and SRC and induce tumor regression in a PDX from the resistant tumor without causing body weight loss in the mice[1]. Mice: Tumors are established in female nude mice. Treatment is by oral gavage daily with vehicle (5% DMSO, 95% water), 90 mg/kg PLX4720, 20 mg/kg CCT196969, or 20 mg/kg CCT241161. All the inhibitors are administered 7 days/week, with no weekend break. Tumor size is determined by caliper measurements of tumor length, width, and depth volume is calculated as volume = 0.5236×length×width×depth (in millimeters)[1]. Cultured cells are seeded into 96-well plates (2,000 cells per well). At 24 hr later, serial dilutions of the B-Raf inhibitors PLX4720 and SB590885, the MEK inhibitor PD184352, or compounds CCT241161 and CCT196969 are added. Cells are incubated for a further 72 hr, and viability is measured by CellTiter-Glo assays. Relative survival in the presence of drugs is normalized to the untreated controls after background subtraction[1]. BRafV600E 0.04 μM (IC50) Braf 0.1 μM (IC50) CRAF 0.01 μM (IC50) LCK 0.02 μM (IC50) SRC 0.03 μM (IC50) \| \| \| \| \| \| \| \| \| \| [1]. Girotti MR, et al. Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma. Cancer Cell. 2015 Jan 12 27(1):85-96. [Content Brief]
Last Update	2025-04-01 14:45:47

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