XMD16-5

SKU: orb1303863

Description

XMD16-5 is a potent and selective small molecule inhibitor of TNK2 (ACK1), a kinase implicated in promoting metastasis in cancers such as breast, prostate, and lung. This compound is a valuable research tool for investigating TNK2 signaling pathways in both in vitro cellular assays and in vivo preclinical models of cancer progression and metastasis.

Research Area

Metabolism Research, Molecular Biology, Protein Biochemistry

Key Properties

• CAS Number: 1345098-78-3
• MW: 416.48
• Purity: 99.98%
• Formula: C₂₃H₂₄N₆O₂
• SMILES: CN1c2ccccc2C(=O)Nc2cnc(Nc3ccc(cc3)N3CCC(O)CC3)nc12
• Target: Tyrosinase,PPAR
• Solubility: Ethanol:5 mg/mL (12.01 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.8 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:45 mg/mL (108.05 mM)

Bioactivity

• Target IC50:
  R806Q:77 nM|D163E:16nM
• 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.
• 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, TNK2, XMD16 5, XMD165, XMD-16-5, XMD16-5, Tyrosinase

Compound Identifiers

PubChem CID

57340666