All AbMole products are for research use only, cannot be used for human consumption.
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.
CNS Neurosci Ther. 2020 Jul;26(7):777.
Retraction: Receptor tyrosine kinase AXL is correlated with poor prognosis and induces temozolomide resistance in glioblastoma
Dubermatinib purchased from AbMole
CNS Neurosci Ther. 2019 Oct 2.
Receptor tyrosine kinase AXL is correlated with poor prognosis and induces temozolomide resistance in glioblastoma.
Dubermatinib purchased from AbMole
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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. |
| 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 |
| 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 |
| Related TAM Receptor Products |
|---|
| Bemcentinib
Bemcentinib (R428) is a potent and selective small-molecule inhibitor of Axl kinase with IC50 of 14 nM. |
| SGI-7079
SGI-7079 is a novel Axl inhibitor. |
| UNC2250
UNC2250 is a potent and selective Mer inhibitor with IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3. |
| UNC2881
UNC2881 is a specific Mer tyrosine kinase inhibitor with IC50 of 4.3 nM, about 83- and 58-fold selectivity over Axl and Tyro3, respectively |
| RU-301
RU-301 is a pan-TAM receptor inhibitor that blocks Gas6-induced TAM activation and tumorigenicity, with Kd and IC50 values of 12 μM and 10 μM, respectively. |
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Products are for research use only. Not for human use. We do not sell to patients.
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