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MK-8353

CAS No. : 1184173-73-6

MCE 国际站：MK-8353

产品活性：MK-8353 (SCH900353) 是一种有效的，选择性的，可口服的 ERK1/2 抑制剂，IC₅₀ 值分别为 23.0 nM 和 8.8 nM；MK-8353 具有抗肿瘤活性。

研究领域：MAPK/ERK Pathway  |  Stem Cell/Wnt

作用靶点：ERK

In Vitro: MK-8353 is a potent, selective and orally available ERK1/2 inhibitor, with IC₅₀s of 23.0 nM and 8.8 nM, respectively; MK-8353 has antitumor activity. MK-8353 only at 1 μM shows >50% inhibition on 3 kinases (CLK2, FLT4, and Aurora B), and no other kinases tested are inhibited by >35% at 0.1 μM. MK-8353 also shows potent antitumor activity against various cancer cell lines, such Malme-3M cells (Melanoma), Colo-205 cells (Colon), NCI-H292 cells (Lung), A-549 cells (NSCLC), 8505C cells (Thyroid), SW-626 cells (Ovarian), with EC₅₀s of 21 nM, 19 nM, 130 nM, 230 nM, 210 nM, 108 nM.

In Vivo: MK-8353 (60 mg/kg, p.o., bid (twice daily)) causes at least 50% tumor growth inhibition or regression in 83% of the animal models bearing different tumor cells, including LOX, Colo-205, MIA PaCa-2, and Calu-6 cells.

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