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MK8353
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MK8353图片
CAS NO:1184173-73-6
包装与价格:
包装价格(元)
5mg电议
25mg电议

产品介绍
MK8353 (SCH900353) 是一种有效的、选择性的、可口服的 ERK1/2 抑制剂,IC50 分别为 23.0 nM 和 8.8 nM; MK8353 具有抗肿瘤活性。
Cas No.1184173-73-6
别名SCH900353
Canonical SMILESO=C([C@@]1(SC)CN(CC(N2CC=C(C3=CC=C(C4=NN(C)C=N4)C=C3)CC2)=O)CC1)NC5=CC6=C(NN=C6C7=CC=C(OC(C)C)N=C7)C=C5
分子式C37H41N9O3S
分子量691.84
溶解度Soluble in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

MK-8353 is a potent, selective and orally available ERK1/2 inhibitor. It is a clinical candidate suitable for twice daily oral dosing as a potential new cancer therapeutic.

MK-8353 demonstrates kinase selectivity over a 227-human kinase panel; no additional kinase in the panel was inhibited by more than 35% at the 0.1 μM concentration, and only 3 kinases (CLK2, FLT4, and Aurora B) were inhibited >50% at the 1.0 μM concentration. MK-8353 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.

MK-8353 administered by oral gavage at 60 mg/kg twice daily results in at least 50% tumor growth inhibition or regression in 83% of the animal models (including LOX, Colo-205, MIA PaCa-2, and Calu-6 cells).

References

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.