1. MAPK/ERK Pathway
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  3. CCT196969

CCT196969 

Cat. No.: HY-12846 Purity: 99.04%
Handling Instructions

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

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10 mM * 1 mL in DMSO USD 95 In-stock
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10 mg USD 132 In-stock
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100 mg USD 672 In-stock
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Based on 1 publication(s) in Google Scholar

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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].

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

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].

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

Molecular Weight

513.52

Formula

C₂₇H₂₄FN₇O₃

CAS No.

1163719-56-9

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 32 mg/mL (62.32 mM)

*"≥" 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
10 mM 0.1947 mL 0.9737 mL 1.9473 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
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
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Keywords:

CCT196969CCT 196969CCT-196969RafRaf kinasesInhibitorinhibitorinhibit

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CCT196969
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