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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.84%
- CAS 番号: 1341200-45-0
- 分子式: C24H30ClN7O2S
- 分子量:516.06
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Apoptosis Compound Library
HY-L003
-
Kinase Inhibitor Library
HY-L009
-
Protein Tyrosine Kinase Compound Library
HY-L016
-
Anti-Cancer Compound Library
HY-L025
-
Clinical Compound Library
HY-L026
-
Drug Repurposing Compound Library
HY-L035
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Highly Selective Inhibitors Library
HY-L158
-
Highly Selective Activators Library
HY-L159
-
Cell Death Library
HY-L162
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
Anti-Brain Cancer Compound Library
HY-L188
-
Protein Kinase Compound Library
HY-L196
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
MedChemExpress（MCE）の使用を引用している文献 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.
生物活性
|
Axl |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| PSN1 | EC50 |
222 nM
Compound: 13
|
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
|
[PMID: 22247788] |
| PSN1 | EC50 |
305 nM
Compound: 13
|
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
|
[PMID: 22247788] |
| PSN1 | IC50 |
0.06 μM
Compound: 13
|
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
|
[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
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 1341200-45-0
-
性状 Solid
-
分子量 516.06
-
分子式 C24H30ClN7O2S
-
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
-
別名
TP-0903
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (9)
-
Journal Impact Factor
-
Most Recent
-
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 -
-
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 -
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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
プロトコル
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.
純度とドキュメンテーション
-
データシート (272 KB)
-
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)
-
取扱説明書 (2659 KB)
参考文献
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9378 mL | 9.6888 mL | 19.3776 mL | 48.4440 mL |
Dubermatinib 関連分類
HY-12963 関連分類
Powered by Bioz