| CAS NO: | 1184173-73-6 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 25mg | 电议 |
| Cas No. | 1184173-73-6 |
| 别名 | SCH900353 |
| Canonical SMILES | O=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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation 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. |
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