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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;MELK-8a hydrochloride, 10 mM in DMSO;1-methyl-4-[4-[4-[3-(piperidin-4-ylmethoxy)pyridin-4-yl]pyrazol-1-yl]phenyl]piperazine;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
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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
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-6237
Product name
MELK-8ahydrochloride
Purity
98.46%
Packaging
5mg
Price
$420
Updated
2021/12/16
Biorbyt Ltd
Product number
orb611463
Product name
NVP-MELK8a hydrochloride
Packaging
5mg
Price
$569.5
Updated
2021/12/16
ChemScene
Product number
CS-6237
Product name
MELK-8ahydrochloride
Purity
98.46%
Packaging
10mg
Price
$600
Updated
2021/12/16
Biorbyt Ltd
Product number
orb611463
Product name
NVP-MELK8a hydrochloride
Packaging
10mg
Price
$615.4
Updated
2021/12/16
ChemScene
Product number
CS-6237
Product name
MELK-8ahydrochloride
Purity
98.46%
Packaging
1mg
Price
$180
Updated
2021/12/16
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MELK-8a (hydrochloride) Chemical Properties,Usage,Production

Uses

MELK-8a hydrochloride is a novel maternal embryonic leucine zipper kinase (MELK) inhibitor with an IC50 of 2 nM.

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.

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target

IC50: 2 nM (MELK)

References

[1] Touré BB, et al. Toward the Validation of Maternal Embryonic Leucine Zipper Kinase: Discovery, Optimization of Highly Potent and Selective Inhibitors, and Preliminary Biology Insight. J Med Chem. 2016 May 26;59(10):4711-23. DOI:10.1021/acs.jmedchem.6b00052

MELK-8a (hydrochloride) Preparation Products And Raw materials

Raw materials

Preparation Products

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MELK-8a (hydrochloride) Suppliers

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2096992-20-8, MELK-8a (hydrochloride)Related Search:


  • 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
  • 2096992-20-8