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Dubermatinib

Cat. No. M8915

All AbMole products are for research use only, cannot be used for human consumption.

Dubermatinib Structure
Synonym:

TP-0903

Size Price Availability Quantity
5mg USD 80  USD80 In stock
10mg USD 110  USD110 In stock
25mg USD 240  USD240 In stock
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Quality Control & Documentation
Biological Activity

Dubermatinib (TP-0903) is a potent and selective AXL inhibitor with an IC50 value of 27 nM. TP-0903 induces massive apoptosis in CLL B cells with LD50 values of nanomolar ranges.

In vitro: Dubermatinib (TP-0903) shows extremely potent activity in cell viability assays with an IC50 of 6 nM against the pancreatic cancer cell line PSN-1. TP-0903 is evaluated for its ability to block GAS6-mediated activation of AXL in pancreatic cancer cells. PSN-1 cells are serum-starved and then stimulated with GAS6 in the presence of various concentrations of TP-0903.

Product Citations
Customer Product Validations & Biological Datas
Source CNS Neurosci Ther (2020 Jul). Figure 5.TP-0903 (Abmole Bioscience, TX, USA)
Method In vitro cell viability assay
Cell Lines GBM cells
Concentrations different concentrations
Incubation Time 3 days
Results Moreover, an in vitro proliferation assay indicated that TP-0903 attenuated the growth of TMZ-resistant U87 cells, and more importantly, the gained TMZ resistance was significantly reversed by TP-0903.
Protocol (for reference only)
Cell Experiment
Cell lines PSN-1 cells
Preparation method For cell proliferation assays, 45 µL containing 1000 cells per well are seeded into solid white 384-well plates in appropriate cell growth media containing 10% FBS and incubated overnight at 37 °C and 5% CO2. The following day, test compounds are 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 EnVision microplate reader. Percent cell viability for test compounds is calculated by comparing treated wells to appropriate controls (e.g. vehicle treated) included on each plate.
Concentrations
Incubation time 96 hours
Animal Experiment
Animal models Female nude mice (6 weeks old) carrying GBM cells
Formulation -
Dosages 20 mg/kg/d
Administration tail vein injection
Chemical Information
Molecular Weight 516.06
Formula C24H30ClN7O2S
CAS Number 1341200-45-0
Solubility (25°C) DMSO 3 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Sinha S, et al. Clin Cancer Res. Targeted Axl Inhibition Primes Chronic Lymphocytic Leukemia B Cells to Apoptosis and Shows Synergistic/Additive Effects in Combination with BTK Inhibitors.

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Keywords: Dubermatinib, TP-0903 supplier, TAM Receptor, inhibitors, activators

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