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  2. MELK

MELK-8a hydrochloride 

Cat. No.: HY-100368A Purity: 99.23%
Handling Instructions

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

For research use only. We do not sell to patients.

MELK-8a hydrochloride Chemical Structure

MELK-8a hydrochloride Chemical Structure

CAS No. : 2096992-20-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 433 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Top Publications Citing Use of Products

    MELK-8a hydrochloride purchased from MCE. Usage Cited in: Cell Rep. 2017 Dec 5;21(10):2829-2841.

    A375 cells are treated with MELK-8a for 48 h and analyzed for indicated proteins by immunoblot analysis. ACTINB is used for as a loading control.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    IC50 & Target

    IC50: 2 nM (MELK)[1]

    In Vitro

    MELK-8a remains very potent (IC50=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 IC50 of approximately 0.06 and 1.2 μM, respectively[1].

    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 (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, 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[1].

    Solvent & Solubility
    In Vitro: 

    DMSO : 8.6 mg/mL (18.34 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1321 mL 10.6605 mL 21.3211 mL
    5 mM 0.4264 mL 2.1321 mL 4.2642 mL
    10 mM 0.2132 mL 1.0661 mL 2.1321 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Cell Assay
    [1]

    MDA-MB-468 and MCF7 cells are seeded in growth medium into 96-well plates at 1000 and 4000 cells/well, respectively. Sixteen hours after plating, MELK-8a are added and incubated for 7 days. For each well, ATPLite reagent is added and incubated. Luminescence is measured on an multilabel plate reader[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Mice: For pharmacokinetic studies, the intravenous and oral dose is prepared in a solution containing 5% ethanol, 100% PG, 5% CremophorEL, and 80% PBS. The subcutaneous dose is formulated in 10% PG and 25% (20%, v/v) Solutol. Plasma samples are collected at specified time points and stored frozen (−20 °C) until MELK-8a analysis. An LC−MS/MS method is used to quantitate MELK-8a drug levels in plasma[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    469.02

    Formula

    C₂₅H₃₃ClN₆O

    CAS No.

    2096992-20-8

    SMILES

    CN(CC1)CCN1C2=CC=C(N3C=C(C4=CC=NC=C4OCC5CCNCC5)C=N3)C=C2.Cl

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
    MELK-8a hydrochloride
    Cat. No.:
    HY-100368A
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    MELK-8a hydrochloride

    Cat. No.: HY-100368A