CC-90003

Catalog No.S8801

CC-90003 Chemical Structure

Molecular Weight(MW): 458.44

CC-90003 is an irreversible inhibitor of ERK1/2 with IC50s in the 10-20 nM range and shows good kinase selectivity in a 258-kinase biochemical assay.

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Biological Activity

Description CC-90003 is an irreversible inhibitor of ERK1/2 with IC50s in the 10-20 nM range and shows good kinase selectivity in a 258-kinase biochemical assay.
Targets
ERK1 [1]
()
ERK2 [1]
()
In vitro

In biochemical, cellular, and mass spectrometry assays of 347 kinases, CC-90003 was found to strongly inhibit kinase activities of ERK1 and ERK2 with IC50s in the 10 to 20 nmol/L range and had good kinase selectivity. In a 258-kinase biochemical assay panel, significant inhibition of 213 kinases (<50% inhibition), moderate inhibition of 28 kinases (50%–80% inhibition), and >80% inhibition of 17 kinases by CC-90003 were found. In an ActivX cellular kinase screening using A375 BRAF V600E-mutant melanoma cell line, only 5 of 194 kinases (ERK1, ERK2, MKK4, MKK6, and FAK) were inhibited by >80% at 1 mmol/L of CC-90003. At the same concentration, no significant inhibition (<14%) was found in a Cerep panel of 40 nonkinase enzymes and receptors. Through our iterative analyses, only 3 kinases, in addition to ERK1/2, were inhibited in cells at biologically relevant concentrations: KDR, FLT3, and PDGFRa. Tumors with BRAF mutations were particularly sensitive to CC-90003. In many, but not all cases, CC-90003 had cytotoxic effects in KRAS-mutant PDAC, lung cancer, and colorectal cancer cell lines. CC-90003 does not significantly inhibit proliferation of normal lung fibroblasts or bronchial epithelial cells[1].

In vivo

In in vivo studies of an HCT-116 xenograft model, CC-90003 was well tolerated at a range of doses (12.5 mg b.i.d.-100 mg qd), although doses of 50 mpk b.i.d. and 75 mpk b.i.d. group caused mortality by days 6 to 18 of study. Both dosing schedules (qd and b.i.d.) leads to tumor growth inhibition. CC-90003 inhibits tumor growth in vivo of three KRAS-mutant PDX models[1].

Protocol

Cell Research:

[1]

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  • Cell lines: KRAS-mutant cell lines
  • Concentrations: --
  • Incubation Time: 72 h
  • Method:

    The cells were plated at a density of 3,000 cells/well in 90 mL of growth media on 96-well clear bottom black-well plates and incubated with overnight under standard cell culture growth conditions at 37 C with 5% CO2. The followinging day, one plate for each cell line was used for "Day 0" cell growth control readout, whereas others were treated with 9-point3-fold dilutions of one compound or combination of compounds, and a DMSO control. Each concentration was tested in triplicate. Cell viability was measured 72 hours later.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Female athymic nude mice inoculated subcutaneously with 5×106 HCT-116 cancer cells
  • Formulation: 5% DMSO/15% Solutol/80% PBS
  • Dosages: 100 mg/kg qd and 50 mg/kg qd; 25 mg/kg b.i.d. and 12.5 mg/kg b.i.d.
  • Administration: orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 92 mg/mL (200.68 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 458.44
Formula

C22H21F3N6O2

CAS No. 1621999-82-3
Storage powder
in solvent
Synonyms N/A

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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.

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ERK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID