Home Tools

CCT196969

Catalog No. T4133 CAS 1163719-56-9

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

CCT196969, CAS 1163719-56-9

Pack Size	Availability	Price/USD
2 mg	In stock	$ 41.00
5 mg	In stock	$ 66.00
10 mg	In stock	$ 100.00
25 mg	In stock	$ 197.00
50 mg	In stock	$ 347.00
100 mg	In stock	$ 519.00
1 mL * 10 mM (in DMSO)	In stock	$ 70.00

Bulk Inquiry

Select Batch

Purity: 99.65%

Purity: 98.58%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
Targets&IC50	BRAF:0.1 μM, Raf:0.01 μM, Lck:0.02 μM, Src:0.03 μM, B-Raf (V600E):0.04 μM
In vitro	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. 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.
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%. CCT196969 is extremely well tolerated at the doses assessed and does not produce any significant adverse effects in vivo.
Cell Research	Cell lines: cell line derived from a vemurafenib-resistant melanoma. Method: The three cell lines derived from tumors displaying resistance to vemurafenib are incubated with DMSO (control),PLX4720,CCT196969,or CCT241161 (1 μM; 4 hr).Protein extracts are prepared in CLB1 lysis buffer,and samples are analyzed by Zeptosens RPPA(reverse phase protein arrays).
Animal Research	Animal Models: CD-1 mice. Formulation: 5% DMSO,95% water. Dosages: 20 mg/kg . Administration: oral gavage

Molecular Weight	513.52
Formula	C27H24FN7O3
CAS No.	1163719-56-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: Insoluble

DMSO: 100 mg/mL (194.73 mM)

H2O: Insoluble

References and Literature

1. Girotti MR,etal.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.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Inhibitor Library Target-Focused Phenotypic Screening Library Angiogenesis related Compound Library Anti-Ovarian Cancer Compound Library Anti-Liver Cancer Compound Library Fluorochemical Library NO PAINS Compound Library Anti-Cancer Compound Library

Related Products

Related compounds with same targets

B-Raf IN 15 Uplarafenib B-Raf IN 13 Sorafenib-d3 NVP-BHG712 Pelitinib LY2452473 GSK2008607

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

CCT196969 1163719-56-9 Angiogenesis MAPK Tyrosine Kinase/Adaptors Raf Src CCT 196969 Inhibitor inhibit CCT-196969 Raf kinases inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.