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份 库存999份
| 货号： | IMA1005-0005MG |
| 保存条件： | -20 |
| CAS号： | 391210-10-9 |
| 供应商： | 上海伟进生物科技有限公司 |
| 英文名： | PD0325901 (MEK1/2 inhibitor) |
| 规格： | 5mg/10mg/25mg |
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Biological Activity ........................................................................................................................................................................................................................................... PD0325901 is a selective, non ATP-competitive and highly potent inhibitor of mitogen-activated protein kinase kinase (MAPKK or MEK), with Ki value around 1 nM against activated MEK1 and MEK2.As an analog of CI-1040 (PD184352), PD0325901 is not only about 500-fold more potent than CI-1040 against the phosphorylation of ERK1 and ERK2 in vitro cell cultures, but shows higher potency of anticancer activity in vivo. PD0325901 is greatly improved in several beneficial pharmacological factors, including longer duration and greater potency of MEK inhibition, as well as greater solubility leading to improved bioavailability, and increased metabolic stability [1-2]. PD0325901 potently inhibits the proliferation of thyroid cancer cells (IC50 = 0.059-0.783 μM) and arrests cell cycle at the G0/G1 phase of cells harboring BRAF or RAS mutations but not cells harboring wild-type alleles or the RET/PTC1 rearrangement [3].PD0325901 exerts potent growth- inhibitory, proapoptotic, and antiangiogenic activity both in vitro and in vivo xenograft models of malignant melanoma, regardless of their BRAF mutation status [4]. PD0325901, when concurrent with GSK-3β inhibitor CHIR99021 prevent cell differentiation and sustain mESCs self-renewal [5]. In combination with ALK5 inhibitor SB431542, PD0325901 also improves the efficiency of the reprogramming process from human fibroblasts [6].
Chemical Properties .........................................................................................................................................................................................................................................
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