CC-90003( CC90003 )

Catalog No. M12390 CAS No. 1621999-82-3

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Datasheet

HNMR

HPLC

MSDS

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Product Name

CC-90003
Note

Research use only, not for human use.
Brief Description

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

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.(In Vitro):CC-90003 is an irreversible and selective inhibitor of ERK 1/2 with antitumor activity.
In Vitro

CC-90003 is an irreversible and selective inhibitor of ERK 1/2 with antitumor activity.
In Vivo

——
Synonyms

CC90003
Pathway

MAPK/ERK Signaling
Target

ERK
Recptor

ERK
Research Area

Cancer
Indication

——

CAS Number

1621999-82-3
Formula Weight

458.445
Molecular Formula

C22H21F3N6O2
Purity

>98% (HPLC)
Solubility

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

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

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

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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