MELK-8a (hydrochloride)
- Product Name
- MELK-8a (hydrochloride)
- CAS No.
- 2096992-20-8
- Chemical Name
- MELK-8a (hydrochloride)
- Synonyms
- MELK-8a (hydrochloride);NVP-MELK8a hydrochloride;1-Methyl-4-(4-(4-(3-(piperidin-4-ylmethoxy)pyridin-4-yl)-1H-pyrazol-1-yl)phenyl)piperazine hydrochloride;MELK-8a,inhibit,MELK,NVS-MELK8a,MELK8a hydrochloride,Maternal embryonic leucine zipper kinase,Inhibitor,MELK 8a hydrochloride
- CBNumber
- CB53167617
- Molecular Formula
- C25H33ClN6O
- Formula Weight
- 469.03
- MOL File
- 2096992-20-8.mol
MELK-8a (hydrochloride) Property
- 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
N-Bromosuccinimide Price
- Product number
- CS-6237
- Product name
- MELK-8ahydrochloride
- Purity
- 98.46%
- Packaging
- 5mg
- Price
- $420
- Updated
- 2021/12/16
- Product number
- orb611463
- Product name
- NVP-MELK8a hydrochloride
- Packaging
- 5mg
- Price
- $569.5
- Updated
- 2021/12/16
- Product number
- CS-6237
- Product name
- MELK-8ahydrochloride
- Purity
- 98.46%
- Packaging
- 10mg
- Price
- $600
- Updated
- 2021/12/16
- Product number
- orb611463
- Product name
- NVP-MELK8a hydrochloride
- Packaging
- 10mg
- Price
- $615.4
- Updated
- 2021/12/16
- Product number
- CS-6237
- Product name
- MELK-8ahydrochloride
- Purity
- 98.46%
- Packaging
- 1mg
- Price
- $180
- Updated
- 2021/12/16
MELK-8a (hydrochloride) Chemical Properties,Usage,Production
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
IC50: 2 nM (MELK)
MELK-8a (hydrochloride) Preparation Products And Raw materials
Raw materials
Preparation Products
MELK-8a (hydrochloride) Suppliers
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