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| MELK-8a (hydrochloride) Basic information |
Product Name: | MELK-8a (hydrochloride) | Synonyms: | MELK-8a (hydrochloride);NVP-MELK8a hydrochloride;MELK-8a,inhibit,MELK,NVS-MELK8a,MELK8a hydrochloride,Maternal embryonic leucine zipper kinase,Inhibitor,MELK 8a hydrochloride | CAS: | 2096992-20-8 | MF: | C25H33ClN6O | MW: | 469.03 | EINECS: | | Product Categories: | | Mol File: | 2096992-20-8.mol | ![MELK-8a (hydrochloride) Structure](CAS/20211123/GIF/2096992-20-8.gif) |
| MELK-8a (hydrochloride) Chemical Properties |
storage temp. | Store at -20°C | solubility | DMF: insol; DMSO: insol; Ethanol: insol; PBS (pH 7.2): 1 mg/ml | form | A solid | color | Light yellow to yellow |
| MELK-8a (hydrochloride) Usage And Synthesis |
Biological Activity | MELK-8a hydrochloride is a novel inhibitor of maternal embryonic leucine zipper kinase (MELK) with IC50 of 2 nM. | in vivo | 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. | 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 (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. < /b> | target | |
| MELK-8a (hydrochloride) Preparation Products And Raw materials |
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