Home MAPK Raf inhibitor - Src inhibitor CCT196969 For research use only.

CCT196969

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

CCT196969 Chemical Structure

CCT196969 Chemical Structure

CAS No. 1163719-56-9

Purity & Quality Control

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

CCT196969 Related Products

Signaling Pathway

Raf Signaling Pathways

Raf Signaling Pathway

Biological Activity

Description CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
Targets
CRAF [1]
(Cell-free assay)		 LCK [1]
(Cell-free assay)		 Src [1]
(Cell-free assay)		 V600E-BRAF [1]
(Cell-free assay)		 BRAF [1]
(Cell-free assay)
0.01 μM 0.02 μM 0.03 μM 0.04 μM 0.1 μM
In vitro
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. CCT196969 induces caspase 3 and PARP cleavage, thus induces apoptosis. CCT196969 does not drive paradoxical pathway activation and inhibit MEK/ERK in BRAF and NRAS mutant melanoma[1].
In Vivo
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 CCT196969 results in plasma concentrations ∼1 μM at 24 hr. It is orally bioavailable at ∼55%[1].
Animal Research Animal Models CD-1 mice
Dosages 20 mg/kg 
Administration oral gavage

Chemical Information & Solubility

Molecular Weight 513.52 Formula

C27H24FN7O3
CAS No. 1163719-56-9 SDF Download CCT196969 SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (194.73 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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