SCH900353 (MK-8353)

SCH900353 (MK-8353)

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Description

Background Information:

MK-8353 (SCH-900353) is an orally bioavailable potent inhibitor
targeting activated ERK1/2 with IC50 values of 23.0 and 8.8 nM,
respectively, and nonactivated ERK2 with IC50 of 0.5 nM, highly
selective over a panel of 227-human kinase; decreases levels of pERK1,
pERK2, and ribosomal S6 kinase (pRSK) protein formation, 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; displays in vivo antitumor efficacy
against BRAFV600 mutant Colo-205 colon cancer model and the BRAFV600
mutant SK-MEL-28 melanoma model.

Reference:

1. S. B. Boga, et al, MK-8353: Discovery of an Orally Bioavailable
Dual Mechanism ERK Inhibitor for Oncology, ACS Med. Chem. Lett.2018, 9
(7), 761-767, (June 14, 2018).

APIM050238: SCH900353 (MK-8353)

CAS No.: 1184173-73-6.
Molecular Formula: C37H41 N9O3S • H2O.
Molecular Weight: 709.9.
Purity: >99.5% Pure by Achiral and Chiral HPLCs.
QC: Achiral and Chiral HPLCs, MS, NMR, and Quantitative Elemental analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.

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