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Chemical Structure : MK-8353
CAS No.: 1184173-73-6
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 1 mg | $78 | In stock | |
| 5 mg | $188 | In stock | |
| 10 mg | $328 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 691.855 | |
| Formula | C37H41N9O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: 125 mg/mL (180 mM) |
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| 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 |
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1. Moschos SJ, et al. JCI Insight. 2018 Feb 22;3(4). pii: 92352.
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