Dubermatinib
Based on 9 publication(s) in Google Scholar
Dubermatinib (TP-0903) is a potent and selective Axl receptor tyrosine kinase inhibitor with an IC50 value of 27 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.84%
- No. CAS: 1341200-45-0
- Fòrmula: C24H30ClN7O2S
- Peso molecular:516.06
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Dubermatinib
More- Cell Rep Med. 2025 Dec 29:102526. [Abstract]
- Cell Death Discov. 2025 Aug 13;11(1):378. [Abstract]
- J Transl Med. 2023 Dec 8;21(1):890. [Abstract]
- Sci Rep. 2024 Jan 3;14(1):425. [Abstract]
- Neurochem Res. 2021 Mar;46(3):504-512. [Abstract]
- Mol Pain. 2020 Jan-Dec:16:1744806919900814. [Abstract]
- bioRxiv. 2024 Jul 25.
- bioRxiv. 2023 May 31:2023.05.30.542969. [Abstract]
- Preprints. 2023 May 15.
Actividad biológica
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Axl |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PSN1 | EC50 |
222 nM
Compound: 13
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Inhibition of AXL in human PSN1 cells assessed as decrease in GAS6-induced phospho-AXL level after 2 hrs by EILSA
Inhibition of AXL in human PSN1 cells assessed as decrease in GAS6-induced phospho-AXL level after 2 hrs by EILSA
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[PMID: 22247788] |
| PSN1 | EC50 |
305 nM
Compound: 13
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Inhibition of AXL-mediated AKT Ser473 phosphorylation in human PSN1 cells assessed as decrease in GAS6-induced phospho-AKT level after 2 hrs by ELISA
Inhibition of AXL-mediated AKT Ser473 phosphorylation in human PSN1 cells assessed as decrease in GAS6-induced phospho-AKT level after 2 hrs by ELISA
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[PMID: 22247788] |
| PSN1 | IC50 |
0.06 μM
Compound: 13
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Cytotoxicity against human PSN1 cells after 96 hrs by ATP-lite luminescence assay
Cytotoxicity against human PSN1 cells after 96 hrs by ATP-lite luminescence assay
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[PMID: 22247788] |
Dubermatinib (TP-0903) displays a potent activity against AXL with an IC50 of 0.027 μM. 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. Dubermatinib (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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1341200-45-0
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Appearance Solid
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Peso molecular 516.06
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Fòrmula C24H30ClN7O2S
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Color Off-white to yellow
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SMILES
O=S(C1=CC=CC=C1NC2=NC(NC3=CC=C(CN4CCN(C)CC4)C=C3)=NC=C2Cl)(N(C)C)=O
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Synonyms
TP-0903
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (9)
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Journal Impact Factor
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Most Recent
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Cell Rep Med
CDK4/6 inhibition overcomes venetoclax resistance mechanisms with enhanced combination activity in acute myeloid leukemia. [Abstract]2025 Dec 29:102526. PMID: 41468895 -
Cell Death Discov
AXL tyrosine kinase inhibitor TP-0903 induces ROS trigger neuroblastoma cell apoptosis via targeting the miR-335-3p/DKK1 expression. [Abstract]2025 Aug 13;11(1):378. PMID: 40804038 -
J Transl Med
Ozone alleviates MSU-induced acute gout pain via upregulating AMPK/GAS6/MerTK/SOCS3 signaling pathway. [Abstract]2023 Dec 8;21(1):890. PMID: 38066599 -
Sci Rep
Mesenchymal-epithelial transition and AXL inhibitor TP-0903 sensitise triple-negative breast cancer cells to the antimalarial compound, artesunate. [Abstract]2024 Jan 3;14(1):425. PMID: 38172210 -
Neurochem Res
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. [Abstract]2021 Mar;46(3):504-512. PMID: 33387191 -
Mol Pain
AXL signaling in primary sensory neurons contributes to chronic compression of dorsal root ganglion-induced neuropathic pain in rats. [Abstract]2020 Jan-Dec:16:1744806919900814. PMID: 31884887 -
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bioRxiv
Single-cell RNA sequencing reveals microenvironment context-specific routes for epithelial-mesenchymal transition in pancreas cancer cells. [Abstract]2023 May 31:2023.05.30.542969. PMID: 37398348 -
Solvente y solubilidad
DMSO : 2 mg/mL (3.88 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 10 mg/mL (19.38 mM); Suspended solution; Need ultrasonic
Protocolo
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, Dubermatinib (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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.9378 mL | 9.6888 mL | 19.3776 mL | 48.4440 mL |
Dubermatinib Related Classifications
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