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MK-8353

Chemical Structure : MK-8353

CAS No.: 1184173-73-6

MK-8353 (MK8353;SCH900353;SCH-900353)

Catalog No.: PC-62595Not For Human Use, Lab Use Only.

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

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

Biological Activity

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

Physicochemical Properties

M.Wt 691.855
Formula C37H41N9O3S
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

DMSO: 125 mg/mL (180 mM)

Chemical Name/SMILES

(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

References

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

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