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。

MK-8353 (SCH900353) is a potent, selective and orally available ERK1/2 inhibitor, with IC 50 s of 23.0 nM and 8.8 nM, respectively; MK-8353 has antitumor activity.

Solid

ERK2 8.8 nM (IC50) ERK1 23 nM (IC50

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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[1]. Moschos SJ, et al. Development of MK-8353, an orally administered ERK1/2 inhibitor, in patients with advanced solid tumors. JCI Insight. 2018 Feb 22;3(4). pii: 92352.

In Vitro: DMSO : 100 mg/mL (144.54 mM; Need ultrasonic)配制储备液