MK-8353 hydrochloride ( MK8353 )

Catalog No. M13053 CAS No. 1951448-73-9

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Datasheet

HNMR

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Product Name

MK-8353 hydrochloride
Note

Research use only, not for human use.
Brief Description

MK-8353 hydrochloride (SCH-900353) is a highly potent, orally bioavailable, dual-specificity ERK1/2 inhibitor with IC50 of 23.0/8.8 nM, respectively.
Description

MK-8353 hydrochloride (SCH-900353) is a highly potent, orally bioavailable, dual-specificity ERK1/2 inhibitor with IC50 of 23.0/8.8 nM, respectively; inhibits nonactivated ERK2 with IC50 of 0.5 nM, demonstrates excellent kinase selectivity over a 227-human kinase panel; decreases pERK1, pERK2, and ribosomal S6 kinase (pRSK) proteins, with complete suppression of pERK1 and pERK2 observed at 30 nM in A2058 cells, inhibits the in vitro proliferation of a panel of BRAFV600-mutant and RAS-mutant cancer cell lines; exhibits in vivo antitumor activity against BRAFV600 mutant Colo-205 colon cancer model and the BRAFV600 mutant SK-MEL-28 melanoma model.Colon Cancer Phase 1 Clinical
Synonyms

MK8353
Pathway

MAPK/ERK Signaling
Target

ERK
Recptor

ERK
Research Area

Cancer
Indication

Colon Cancer

CAS Number

1951448-73-9
Formula Weight

728.31
Molecular Formula

C37H42ClN9O3S
Purity

>98% (HPLC)
Solubility

——
SMILES

——
Chemical Name

(S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide hydrochloride

1. Moschos SJ, et al. JCI Insight. 2018 Feb 22;3(4). pii: 92352.

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