CCT196969
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MedKoo CAT#: 406645

CAS#: 1163719-56-9

Description: CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. CCT196969 blocked growth of BRAF-mutant and NRAS-mutant melanoma cells, inhibiting MEK–ERK, in vitro and in vivo. CCT196969 also prevented growth of xenografts derived from patient tumours with acquired or intrinsic resistance to BRAF and MEK inhibitors. BRAF and MEK inhibitors are effective in BRAF mutant melanoma, but most patients eventually relapse with acquired resistance, and others present intrinsic resistance to these drugs.


Chemical Structure

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CCT196969
CAS# 1163719-56-9

Theoretical Analysis

MedKoo Cat#: 406645
Name: CCT196969
CAS#: 1163719-56-9
Chemical Formula: C27H24FN7O3
Exact Mass: 513.19247
Molecular Weight: 513.52
Elemental Analysis: C, 63.15; H, 4.71; F, 3.70; N, 19.09; O, 9.35

Price and Availability

Size Price Availability Quantity
5.0mg USD 255.0 2 Weeks
25.0mg USD 475.0 2 Weeks
100.0mg USD 935.0 2 Weeks
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Synonym: CCT196969; CCT-196969; CCT 196969.

IUPAC/Chemical Name: 1-(3-(tert-butyl)-1-phenyl-1H-pyrazol-5-yl)-3-(2-fluoro-4-((3-oxo-3,4-dihydropyrido[2,3-b]pyrazin-8-yl)oxy)phenyl)urea

InChi Key: KYYKGSDLXXKQCR-UHFFFAOYSA-N

InChi Code: InChI=1S/C27H24FN7O3/c1-27(2,3)21-14-22(35(34-21)16-7-5-4-6-8-16)32-26(37)31-19-10-9-17(13-18(19)28)38-20-11-12-29-25-24(20)30-15-23(36)33-25/h4-15H,1-3H3,(H,29,33,36)(H2,31,32,37)

SMILES Code: FC1=CC(OC2=C3C(NC(C=N3)=O)=NC=C2)=CC=C1NC(NC4=CC(C(C)(C)C)=NN4C5=CC=CC=C5)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 513.52 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Girotti MR, Lopes F, Preece N, Niculescu-Duvaz D, Zambon A, Davies L, Whittaker S, Saturno G, Viros A, Pedersen M, Suijkerbuijk BM, Menard D, McLeary R, Johnson L, Fish L, Ejiama S, Sanchez-Laorden B, Hohloch J, Carragher N, Macleod K, Ashton G, Marusiak AA, Fusi A, Brognard J, Frame M, Lorigan P, Marais R, Springer C. 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. doi: 10.1016/j.ccell.2014.11.006. Epub 2014 Dec 11. PubMed PMID: 25500121; PubMed Central PMCID: PMC4297292.



Additional Information