1. Metabolic Enzyme/Protease
  2. Tyrosinase
  3. XMD16-5

XMD16-5 

Cat. No.: HY-101243 Purity: 98.73%
Handling Instructions

XMD16-5 is a potent TNK2 inhibitor with IC50 values of 16 and 77 nM for the D163E and R806Q mutations, respectively.

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

XMD16-5 Chemical Structure

XMD16-5 Chemical Structure

CAS No. : 1345098-78-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
25 mg USD 288 In-stock
Estimated Time of Arrival: December 31
50 mg USD 528 In-stock
Estimated Time of Arrival: December 31
100 mg USD 960 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

XMD16-5 is a potent TNK2 inhibitor with IC50 values of 16 and 77 nM for the D163E and R806Q mutations, respectively.

IC50 & Target

IC50: 16 nM (TNK2, D163E mutation), 77 nM (TNK2, R806Q mutation)[1]

In Vitro

XMD16-5 potently inhibits the growth of the TNK2 mutant expressing cell lines while having little or no effect on the control cells out to the highest tested concentrations (1,000 nM). XMD16-5 has IC50s of 16 nM and 77 nM for the D163E and R806Q mutations. The effects of XMD16-5 on TNK2 cell lines are largely due to on-target effects on TNK2. Auto-phosphorylation of overexpressed TNK2 mutants could be blocked with TNK2 inhibitor XMD16-5[1].

Molecular Weight

416.48

Formula

C₂₃H₂₄N₆O₂

CAS No.

1345098-78-3

SMILES

O=C1NC2=CN=C(NC3=CC=C(N4CCC(O)CC4)C=C3)N=C2N(C)C5=CC=CC=C15

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (240.11 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4011 mL 12.0054 mL 24.0108 mL
5 mM 0.4802 mL 2.4011 mL 4.8022 mL
10 mM 0.2401 mL 1.2005 mL 2.4011 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

Kinase targets are tested with biochemical enzymatic kinase assays using the SelectScreen Kinase Profiling Service to determine IC50 values. The compounds (XMD16-5) are assayed at 10 concentrations (3-fold serial dilutions starting from 1 μM) at an ATP concentration equal to the ATP Km[1].

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

Cell Assay
[1]

Cells are treated with the following inhibitors for 72 hours: dasatinib, AIM-100, XMD8-87 and XMD16-5. Cell viability is measured using a methanethiosulfonate (MTS)-based assay and absorbance (490 nm) is read at 1 and 3 hours after adding reagent[1].

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

References
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Keywords:

XMD16-5TyrosinaseInhibitorinhibitorinhibit

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Product Name:
XMD16-5
Cat. No.:
HY-101243
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