Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MELK-8a hydrochloride is a potent inhibitor of maternal embryonic leucine zipper kinase (MELK, IC50 = 2 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 147.00 | |
5 mg | In stock | $ 347.00 | |
10 mg | In stock | $ 497.00 | |
25 mg | In stock | $ 793.00 | |
50 mg | In stock | $ 1,130.00 | |
100 mg | In stock | $ 1,520.00 | |
500 mg | In stock | $ 2,970.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 358.00 |
Description | MELK-8a hydrochloride is a potent inhibitor of maternal embryonic leucine zipper kinase (MELK, IC50 = 2 nM). |
Targets&IC50 | MELK:2 nM |
In vitro | MELK-8a hydrochloride inhibits the growth of MDA-MB-468 cells and MCF-7 cells with an IC50 of approximately 0.06 and 1.2 μM, respectively. MELK-8a hydrochloride remains very potent with an IC50 of 140 nM when the ATP concentration in the biochemical assay is shifted from 20 μM to 2 mM. MELK-8a hydrochloride only inhibits seven off-target kinases in addition to MELK with >85% inhibition of binding at 1 μM demonstrating great selectivity. MELK-8a hydrochloride is at least 90-fold more selective in targeting MELK in all cases. MELK-8a hydrochloride is fairly soluble (0.22 g/L at pH 6.8) and shows a good permeability in the Caco-2 assay[1]. |
In vivo | In C57BL/6 mice, MELK-8a hydrochloride (30 mg/kg; s.c.) 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, MELK-8a hydrochloride (10 mg/kg; oral) shows very poor PK (3.6% oral bioavailability) consistent with very high in vivo clearance[1]. |
Molecular Weight | 469.02 |
Formula | C25H33ClN6O |
CAS No. | 2096992-20-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 100 mg/mL (213.21 mM)
DMSO: 8 mg/mL (17.06 mM), Sonification and heating are recommended.
You can also refer to dose conversion for different animals. More
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