MELK8A HYDROCHLORIDE
中文名称 | MELK8A HYDROCHLORIDE |
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中文同义词 | 母体胚胎亮氨酸拉链激酶(MELK)抑制剂(MELK-8A HYDROCHLORIDE);化合物 T11996;化合物MELK-8A HYDROCHLORIDE;盐酸MELK-8A;1-甲基-4-(4-(4-(3-(哌啶-4-基甲氧基)吡啶-4-基)-1H-吡唑-1-基)苯基)哌嗪盐酸盐;化合物MELK-8A HYDROCHLORIDE,10 MM DMSO 溶液;1-甲基-4-(4-(4-(4-(3-(哌啶-4-甲基))吡啶-4-基)-1H-吡唑-1-基)苯基苯基)盐酸哌嗪 |
英文名称 | MELK-8a (hydrochloride) |
英文同义词 | MELK-8a (hydrochloride);NVP-MELK8a hydrochloride;MELK-8a,inhibit,MELK,NVS-MELK8a,MELK8a hydrochloride,Maternal embryonic leucine zipper kinase,Inhibitor,MELK 8a hydrochloride;1-Methyl-4-(4-(4-(3-(piperidin-4-ylmethoxy)pyridin-4-yl)-1H-pyrazol-1-yl)phenyl)piperazine hydrochloride;MELK-8a hydrochloride, 10 mM in DMSO;1-methyl-4-[4-[4-[3-(piperidin-4-ylmethoxy)pyridin-4-yl]pyrazol-1-yl]phenyl]piperazine |
CAS号 | 2096992-20-8 |
分子式 | C25H33ClN6O |
分子量 | 469.03 |
EINECS号 | |
相关类别 | 细胞生物学试剂 |
Mol文件 | 2096992-20-8.mol |
结构式 | ![]() |
MELK8A HYDROCHLORIDE 性质
储存条件 | Store at -20°C |
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溶解度 | DMF: 不溶; DMSO: 不溶;乙醇:insol; PBS(pH 7.2):1 mg/mL |
形态 | 固体 |
颜色 | 浅黄至黄色 |
IC50: 2 nM (MELK)
MELK-8a remains very potent (IC 50 =140 nM) when the ATP concentration in the biochemical assay is shifted from 20 μM to 2 mM. Its potency is well tracked between full-length MELK versus catalytic domain construct (5 nM versus 2 nM). It only inhibits seven off-target kinases in addition to MELK with >85% inhibition of binding at 1 μM demonstrating great selectivity. The compound is at least 90-fold more selective in targeting MELK in all cases. MELK-8a is fairly soluble (0.22 g/L at pH 6.8) and shows a good permeability in the Caco-2 assay. MELK-8a inhibits the growth of MDA-MB-468 cells and MCF-7 cells with an IC 50 of approximately 0.06 and 1.2 μM, respectively.
Subcutaneous administration of MELK-8a at 30 mg/kg in C57BL/6 mice results in good plasma exposure. The compound adsorption into the systemic circulation is rapid (T max =0.4 h) and peak plasma concentration reaches 6.6 μM. An ascending dose PK study in female athymic nude mice shows that the rate of compound release is maximal at 120 mg/kg and all clearance mechanisms can be saturated at 240 mg/kg. However, when administered orally at 10 mg/kg in C57BL/6 male mice, it shows very poor PK (3.6% oral bioavailability) consistent with very high in vivo clearance.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2025/02/08 | HY-100368A | MELK8A HYDROCHLORIDE MELK-8a hydrochloride | 2096992-20-8 | 5mg | 2800元 |
2025/02/08 | HY-100368A | MELK8A HYDROCHLORIDE MELK-8a hydrochloride | 2096992-20-8 | 10mg | 4100元 |