Home MAPK Raf inhibitor CCT196969

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CCT196969 Raf inhibitor

Cat.No.S7743

CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
CCT196969 Raf inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 513.52

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Quality Control

Batch: S774301 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.89%
99.89

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (194.73 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 513.52 Formula

C27H24FN7O3

 Storage (From the date of receipt)
CAS No. 1163719-56-9 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC(C)(C)C1=NN(C(=C1)NC(=O)NC2=C(C=C(C=C2)OC3=C4C(=NC=C3)NC(=O)C=N4)F)C5=CC=CC=C5

Mechanism of Action

Targets/IC50/Ki
CRAF
(Cell-free assay)
0.01 μM
LCK
(Cell-free assay)
0.02 μM
Src
(Cell-free assay)
0.03 μM
V600E-BRAF
(Cell-free assay)
0.04 μM
BRAF
(Cell-free assay)
0.1 μM
In vitro

CCT196969 is active against melanoma and colorectal cancer cell lines that are mutant for BRAF, but not cancer cells that are wild-type for BRAF and NRAS. This compound induces caspase 3 and PARP cleavage, thus induces apoptosis. It does not drive paradoxical pathway activation and inhibit MEK/ERK in BRAF and NRAS mutant melanoma.
In vivo

CCT196969 is extremely well tolerated at the doses assessed and does not produce any significant adverse effects in vivo. Oral dosing at 10 mg/kg/day of this compound results in plasma concentrations ∼1 μM at 24 hr. It is orally bioavailable at ∼55%.
References

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