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XMD16-5

Catalog No. T3710   CAS 1345098-78-3

XMD16-5 is a TNK2 inhibitor. TNK2 genomic amplification has been associated with late-stage or metastatic lung and prostate Ys. Overexpression of TNK2 promoted metastasis in a mouse model of breast Y. TNK2 signaling is disrupted in breast, prostate and gastrointestinal tumors.

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XMD16-5 Chemical Structure
XMD16-5, CAS 1345098-78-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 37.00
2 mg In stock $ 51.00
5 mg In stock $ 92.00
10 mg In stock $ 147.00
25 mg In stock $ 237.00
50 mg In stock $ 437.00
100 mg In stock $ 648.00
500 mg In stock $ 1,380.00
1 mL * 10 mM (in DMSO) In stock $ 92.00
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Purity: 99.6%
Purity: 98.53%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description XMD16-5 is a TNK2 inhibitor. TNK2 genomic amplification has been associated with late-stage or metastatic lung and prostate Ys. Overexpression of TNK2 promoted metastasis in a mouse model of breast Y. TNK2 signaling is disrupted in breast, prostate and gastrointestinal tumors.
Targets&IC50 D163E:16nM, R806Q:77 nM
In vitro XMD16-5 is found to be potent in the inhibition of TNK2 phosphorylation. XMD8-87 and XMD16-5 potently inhibit phosphorylation of TNK2 truncation mutations found in solid tumor types.
Kinase Assay 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].
Cell Research 293T cells expressing TNK2 are plated in 6-well format at a density of 250,000 cells per well 48 hours prior to treatment. Cells are then treated with a 100 μL of XMD8-87 or XMD16-5 at 5 μmol/L and with 9 1:1 serial dilutions down to ≈10 nmol/L. Two additional samples are treated with DMSO only. Cells are then incubated for 6 hours at 37°C. Protein extraction is accomplished by adding 300 μL of lysis buffer to cells after removing media. Plates are gently shaken for 5 minutes at room temperature. Lysates are collected and cleared of incompletely solubilized material by spinning for 10 minutes at maximum speed in a microcentrifuge. Samples are prepared for SDS-PAGE using the EPage loading buffer.(Only for Reference)
Molecular Weight 416.48
Formula C23H24N6O2
CAS No. 1345098-78-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 77 mg/mL (185 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 5 mg/mL (12.01 mM)

TargetMolReferences and Literature

1. Maxson JE, et al. Cancer Res. 2016, 76(1):127-38.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Protease Inhibitor Library Kinase Inhibitor Library Bioactive Compound Library Lipid Metabolism Compound Library Inhibitor Library Metabolism Compound Library DNA Damage & Repair Compound Library Stem Cell Differentiation Compound Library Nuclear Receptor Compound Library

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Keywords

XMD16-5 1345098-78-3 DNA Damage/DNA Repair Metabolism Proteases/Proteasome PPAR Tyrosinase inhibit XMD-16-5 XMD16 5 Inhibitor XMD165 inhibitor

 

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