| Field | Specification |
|---|---|
| Target | |
| Alternative names | TP-0903 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C24H30ClN7O2S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Dubermatinib, also known as TP-0903, is a potent and selective inhibitor of the Axl receptor tyrosine kinase, with an IC50 of 27 nM. It is supplied as an off-white to yellow solid (C24H30ClN7O2S, MW 516.06) at 99.47% purity.
Physical & Chemical Properties
| CAS Number | 1341200-45-0 |
|---|---|
| Molecular Formula | C24H30ClN7O2S |
| Molecular Weight | 516.06 g/mol |
| Purity | 99.47% |
| Appearance | Solid |
| Color | Off-white to yellow |
| SMILES | O=S(C1=CC=CC=C1NC2=NC(NC3=CC=C(CN4CCN(C)CC4)C=C3)=NC=C2Cl)(N(C)C)=O |
| Target | Axl |
| Signaling Pathway | Protein Tyrosine Kinase/RTK; Apoptosis |
| Solubility | In Vitro: DMSO: 2 mg/mL (3.88 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 1 year; -20°C, 6 months. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 2 mg/mL (3.88 mM) | requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 1 year) or -20°C (up to 6 months); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration. Percentages are volume ratios of the final working solution. Prepare the working solution fresh on the day of dosing; if precipitation or phase separation occurs, gentle warming or sonication can help.
Direct preparation of the working solution
These formulations are prepared directly, without a DMSO stock; use them promptly after preparation.
Protocol 1
| Composition | 0.5% CMC-Na/saline water |
|---|---|
| Result | 10 mg/mL (19.38 mM); suspension; requires sonication |
Data provided by the manufacturer.
In Vitro
Dubermatinib (TP-0903) is a potent inhibitor of AXL, with an IC50 of 0.027 μM. In cell viability assays against the pancreatic cancer cell line PSN-1, Dubermatinib (TP-0903) is extremely potent, with an IC50 of 6 nM. Its ability to block GAS6-mediated AXL activation in pancreatic cancer cells is evaluated by serum-starving PSN-1 cells and then stimulating them with GAS6 in the presence of various concentrations of TP-0903[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Cell Assay[1]
For cell proliferation assays, seed 45 μL containing 1000 cells per well into solid white 384-well plates in appropriate media. The next day, dilute Dubermatinib (TP-0903) in serum free growth media to 10x the desired concentrations and add 5 μL to each well. Incubate the combined compound and cells for 96 hours. After incubation, add 40 μL of ATP-Lite solution to each well, incubate for another 10 minutes at room temperature, and measure luminescence on a microplate reader[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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CDK4/6 inhibition overcomes venetoclax resistance mechanisms with enhanced combination activity in acute myeloid leukemia. Cell Rep Med 2025 Dec 29:102526. PMID: 41468895
AXL tyrosine kinase inhibitor TP-0903 induces ROS trigger neuroblastoma cell apoptosis via targeting the miR-335-3p/DKK1 expression. Cell Death Discov 2025 Aug 13;11(1):378. PMID: 40804038
Ozone alleviates MSU-induced acute gout pain via upregulating AMPK/GAS6/MerTK/SOCS3 signaling pathway. J Transl Med 2023 Dec 8;21(1):890. PMID: 38066599
Mesenchymal-epithelial transition and AXL inhibitor TP-0903 sensitise triple-negative breast cancer cells to the antimalarial compound, artesunate. Sci Rep 2024 Jan 3;14(1):425. PMID: 38172210
Electro-acupuncture Suppresses AXL Expression in Dorsal Root Ganglion Neurons and Enhances Analgesic Effect of AXL Inhibitor in Spinal Nerve Ligation Induced-Neuropathic Pain Rats. Neurochem Res 2021 Mar;46(3):504-512. PMID: 33387191
AXL signaling in primary sensory neurons contributes to chronic compression of dorsal root ganglion-induced neuropathic pain in rats. Mol Pain 2020 Jan-Dec:16:1744806919900814.
bioRxiv. 2024 Jul 25.
Single-cell RNA sequencing reveals microenvironment context-specific routes for epithelial-mesenchymal transition in pancreas cancer cells. bioRxiv 2023 May 31:2023.05.30.542969. PMID: 37398348
Preprints. 2023 May 15.
