Home MAPK Raf inhibitor - Src 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

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

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

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

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Mechanism of Action

Targets/IC50/Ki
CRAF [1]
(Cell-free assay)
0.01 μM
LCK [1]
(Cell-free assay)
0.02 μM
Src [1]
(Cell-free assay)
0.03 μM
V600E-BRAF [1]
(Cell-free assay)
0.04 μM
BRAF [1]
(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[1].
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%[1].
References

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