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CCT196969

Chemical Structure : CCT196969

CAS No.: 1163719-56-9

CCT196969 (CCT-196969;CCT 196969)

Catalog No.: PC-43255Not For Human Use, Lab Use Only.

CCT196969 is a potent, orally bioavailable pan-RAF inhibitor with IC50 of 100, 40 and 12 nM for B-Raf, B-Raf V600E and C-Raf, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

CCT196969 is a potent, orally bioavailable pan-RAF inhibitor with IC50 of 100, 40 and 12 nM for B-Raf, B-Raf V600E and C-Raf, respectively.
CCT196969 also potently inhibits SRC (IC50=26 nM) and LCK (IC50=14 nM), does not inhibit MEK1 or the MEK1 kinase COT.
CCT196969 inhibits cell proliferation of BRAF-selective-inhibitor-resistant cells with mean GI50 of 0.4 uM, NRAS mutant melanoma cells (GI50=0.6 uM); induces caspase 3 and PARP cleavage, induces apoptosis, inhibits the growth of PLX4720-resistant A375 xenografts (A375/R) in mice, without causing any body weight loss.

Physicochemical Properties

M.Wt 513.5229
Formula C27H24FN7O3
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

DMSO: ≥ 32 mg/mL

Chemical Name/SMILES

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]-

References

1. Girotti MR, et al. Cancer Cell. 2015 Jan 12;27(1):85-96.

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