2. MAPK/ERK Pathway
  3. Raf
  4. CCT196969

CCT196969 is a pan-Raf inhibitor, which inhibits B-Raf, BRafV600E and CRAF with IC50s of 0.1, 0.04, and 0.01 μM, respectively.

For research use only. We do not sell to patients.

CCT196969 Chemical Structure

CCT196969 Chemical Structure

CAS No. : 1163719-56-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 68 In-stock
Solution
10 mM * 1 mL in DMSO USD 68 In-stock
Solid
1 mg USD 30 In-stock
5 mg USD 60 In-stock
10 mg USD 95 In-stock
25 mg USD 200 In-stock
50 mg USD 320 In-stock
100 mg USD 520 In-stock
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

CCT196969 is a pan-Raf inhibitor, which inhibits B-Raf, BRafV600E and CRAF with IC50s of 0.1, 0.04, and 0.01 μM, respectively.

IC50 & Target[1]

BRafV600E

0.04 μM (IC50)

Braf

0.1 μM (IC50)

CRAF

0.01 μM (IC50)

LCK

0.02 μM (IC50)

SRC

0.03 μM (IC50)

In Vitro

CCT196969 is a pan-Raf inhibitor with anti-SRC activity. CCT196969 is an orally available, well-tolerated B-Raf inhibitor that directly inhibits B-RafV600E in cells. CCT196969 inhibits B-Raf at 100 nM and B-RafV600E at 40 nM. It inhibits CRaf at 12 nM, SRC at 26 nM, and LCK at 14 nM. CCT196969 is active against melanoma and colorectal cancer cell lines that are mutant for B-Raf. CCT196969 induces caspase 3 and PARP cleavage, demonstrating that it induces apoptosis[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CCT196969 Related Antibodies
In Vivo

CCT196969 is extremely well tolerated and does not produce any significant adverse effects in vivo. It inhibits the growth of NRAS mutant DO4 tumor xenografts in nude mice. CCT196969 inhibits ERK and SRC and induce tumor regression in a PDX from the resistant tumor without causing body weight loss in the mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

513.52

Formula

C27H24FN7O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC2=NC=CC(OC3=CC=C(NC(NC4=CC(C(C)(C)C)=NN4C5=CC=CC=C5)=O)C(F)=C3)=C2N=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 32 mg/mL (62.32 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9473 mL 9.7367 mL 19.4734 mL
5 mM 0.3895 mL 1.9473 mL 3.8947 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.63%

COA (259 KB) LCMS (270 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

Cultured cells are seeded into 96-well plates (2,000 cells per well). At 24 hr later, serial dilutions of the B-Raf inhibitors PLX4720 and SB590885, the MEK inhibitor PD184352, or compounds CCT241161 and CCT196969 are added. Cells are incubated for a further 72 hr, and viability is measured by CellTiter-Glo assays. Relative survival in the presence of drugs is normalized to the untreated controls after background subtraction[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice: Tumors are established in female nude mice. Treatment is by oral gavage daily with vehicle (5% DMSO, 95% water), 90 mg/kg PLX4720, 20 mg/kg CCT196969, or 20 mg/kg CCT241161. All the inhibitors are administered 7 days/week, with no weekend break. Tumor size is determined by caliper measurements of tumor length, width, and depth; volume is calculated as volume = 0.5236×length×width×depth (in millimeters)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9473 mL 9.7367 mL 19.4734 mL 48.6836 mL
5 mM 0.3895 mL 1.9473 mL 3.8947 mL 9.7367 mL
10 mM 0.1947 mL 0.9737 mL 1.9473 mL 4.8684 mL
15 mM 0.1298 mL 0.6491 mL 1.2982 mL 3.2456 mL
20 mM 0.0974 mL 0.4868 mL 0.9737 mL 2.4342 mL
25 mM 0.0779 mL 0.3895 mL 0.7789 mL 1.9473 mL
30 mM 0.0649 mL 0.3246 mL 0.6491 mL 1.6228 mL
40 mM 0.0487 mL 0.2434 mL 0.4868 mL 1.2171 mL
50 mM 0.0389 mL 0.1947 mL 0.3895 mL 0.9737 mL
60 mM 0.0325 mL 0.1623 mL 0.3246 mL 0.8114 mL
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CCT196969 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CCT1969691163719-56-9CCT 196969CCT-196969RafRaf kinasesInhibitorinhibitorinhibit

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