Dubermatinib

SKU: orb1306768

Description

Dubermatinib is a selective small molecule inhibitor targeting the Axl receptor tyrosine kinase. It is utilized in cancer research, particularly in studies of metastasis and drug resistance, and has demonstrated activity in both cellular assays and animal models.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1341200-45-0
• MW: 516.06
• Purity: 99.89% (May vary between batches)
• Formula: C₂₄H₃₀ClN₇O₂S
• SMILES: CN(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(CN3CCN(C)CC3)cc2)ncc1Cl
• Target: TAM Receptor,Apoptosis
• Solubility: DMSO:Slightly soluble

Bioactivity

• Target IC50:
  Axl:27 nM
• In Vivo:
  In the adult rat hippocampus, the intracerebroventricular administration of SAG (2.5 nM) significantly increases the number of newly generated cells and extends survival of hippocampal cells. In mice, SAG (20 μg/g, i.p.) effectively prevents GC-induced neonatal cerebellar developmental abnormalities.
• In Vitro:
  In pancreatic cancer cells (PSN-1), TP-0903 shows strong antiproliferative activity with IC50 of 6 M. TP-0903 also induces strong G2/M arrest by potently inhibiting Aurora A and B. In CLL B cells from all the patients with CLL, TP-0903 causes a dose-dependent induction of massive apoptosis by targeting phosphorylated Axl, and overcomes CLL BMSC-mediated protection of CLL B cells from apoptosis.
• Cell Research:
  For cell proliferation assays, 45 μL containing 1000 cells per well are seeded into solid white 384-well plates in appropriate media. The following day, TP-0903 is diluted in serum free growth media to 10x desired concentrations and 5 μL is added to each well. Combined compound and cells are incubated for 96 hours. Following incubation, 40 μL of ATP-Lite solution is added to each well, incubated for an additional 10 minutes at room temperature and luminescence is measured on an microplate reader.

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

Apoptosis, Axl, AXL, Dubermatinib, inhibit, Mer, Inhibitor, TP0903, TP-0903, TP 0903, TAM Receptor, TAMReceptor, Tyro3

Compound Identifiers

PubChem CID

56839178