ChemicalBook > CAS DataBase List > MELK-8a (hydrochloride)

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
More
Less

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
More
Less

Hazard and Precautionary Statements (GHS)

More
Less

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
More
Less

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

More
Less

MELK-8a (hydrochloride) Suppliers

Tel
+1-781-999-5354 +1-00000000000
Email
marketing@targetmol.com
Country
United States
ProdList
32161
Advantage
58
Tel
+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
Country
United States
ProdList
6391
Advantage
58
Tel
Email
support@targetmol.com
Country
United States
ProdList
38631
Advantage
58
Tel
+1-+1(833)-552-7181
Email
sales@aladdinsci.com
Country
United States
ProdList
57505
Advantage
58
Tel
--
Fax
--
Email
cayman@caymanchem.com
Country
United States
ProdList
6213
Advantage
81
Tel
--
Fax
--
Email
sales@medchemexpress.com
Country
United States
ProdList
6398
Advantage
58

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
  • 2096992-20-8