CC-90003

Research use only, not for human use.

CC-90003 (CC90003) is a potent and selective, covalent ERK1/2 inhibitor with IC50 of 10-20 nM.

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.

CC90003

MAPK/ERK Signaling

ERK

ERK

Cancer

——

1621999-82-3

458.45

C22H21F3N6O2

>98% (HPLC)

DMSO : ≥ 125 mg/mL 272.66 mM; H2O : < 0.1 mg/mL

C=CC(NC1=CC(C)=CC=C1NC2=NC(NC3=CC(OC)=NC=C3C)=NC=C2C(F)(F)F)=O

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

(-20℃)

With Ice Pack

≥ 2 years