CAS NO: | 2096992-20-8 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | MELK-8a hydrochloride is a novel maternal embryonic leucine zipper kinase (MELK) inhibitor with anIC50of 2 nM. | ||||||||||||||||
IC50& Target | IC50: 2 nM (MELK)[1] | ||||||||||||||||
体外研究 (In Vitro) | MELK-8a remains very potent (IC50=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 IC50of approximately 0.06 and 1.2 μM, respectively[1]. | ||||||||||||||||
体内研究 (In Vivo) | 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 (Tmax=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 highin vivoclearance[1]. | ||||||||||||||||
分子量 | 469.02 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C25H33ClN6O | ||||||||||||||||
CAS 号 | 2096992-20-8 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: H2O : ≥ 100 mg/mL(213.21 mM) DMSO : 8.6 mg/mL(18.34 mM;Need ultrasonic and warming) *"≥" means soluble, but saturation unknown. 配制储备液
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