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CC-90003

Chemical Structure : CC-90003

CAS No.: 1621999-82-3

CC-90003 (CC90003)

Catalog No.: PC-35813Not For Human Use, Lab Use Only.

CC-90003 (CC90003) is a potent and selective, covalent ERK1/2 inhibitor with IC50 of 10-20 nM, demonstrates excellent selectivity in a 258-kinase biochemical assay panel.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

CC-90003 (CC90003) is a potent and selective, covalent ERK1/2 inhibitor with IC50 of 10-20 nM, demonstrates excellent selectivity in a 258-kinase biochemical assay panel; potently inhibits 27 growth of KRAS mutant cell lines with GI50 of <1 uM, also is active against 28 of 37 (76%) KRAS-mutant cancer cell lines, shows cytotoxic effects in KRAS mutant PDAC, lung cancer and CRC cell lines, does not significantly inhibit proliferation of normal lung fibroblasts or bronchial epithelial cells; decreases colony formation ex-vivo and inhibits tumor growth in vivo of KRAS mutant PDX models, induces full regression and prevents regrowth of KRAS mutant Lung PDX model when combined with Docetaxel.

Physicochemical Properties

M.Wt 458.445
Formula C22H21F3N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(2-((2-((2-methoxy-5-methylpyridin-4-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)-5-methylphenyl)acrylamide

References

1. Aronchik I, et al. Mol Cancer Res. 2018 Oct 1. pii: molcanres.0554.2017. doi: 10.1158/1541-7786.MCR-17-0554.

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