2-((5-chloro-2-((4-((4-methylpiperazin-1-yl)methyl)phenyl)amino)pyrimidin-4-yl)amino)-N,N-dimethylbenzenesulfonamide
TP-0903
CAS: 1341200-45-0
Molecular Formula: C24H30ClN7O2S
2-((5-chloro-2-((4-((4-methylpiperazin-1-yl)methyl)phenyl)amino)pyrimidin-4-yl)amino)-N,N-dimethylbenzenesulfonamide - Names and Identifiers
2-((5-chloro-2-((4-((4-methylpiperazin-1-yl)methyl)phenyl)amino)pyrimidin-4-yl)amino)-N,N-dimethylbenzenesulfonamide - Physico-chemical Properties
| Molecular Formula | C24H30ClN7O2S |
| Molar Mass | 516.06 |
| Density | 1.347±0.06 g/cm3(Predicted) |
| Melting Point | >198°C (dec.) |
| Boling Point | 664.7±65.0 °C(Predicted) |
| Solubility | DMSO: ≥ 30 mg/mL |
| Appearance | Solid |
| Color | Off-White to Light Yellow |
| pKa | 7.60±0.10(Predicted) |
| Storage Condition | Hygroscopic, -20°C Freezer, Under inert atmosphere |
| Use | Dubermatinib (TP-0903) is an efficient and selective Axl receptor tyrosine kinase inhibitor with an IC50 value of 27 nM. |
| Target | AXL |
| In vitro study | In pancreatic cancer cells (PSN-1), TP-0903 showed a strong antiproliferative activity with an IC50 of 6 M. TP-0903 induced A strong G2/M blockade by potent inhibition of Aurora A and B. In CLL B cells from CLL patients, TP-0903 induced massive apoptosis in a dose-dependent manner by targeting phosphorylated Axl and overcame the CLL BMSC-mediated protective effect on CLL B cell apoptosis. |
| In vivo study | In the adult rat hippocampus, intracerebroventricular administration of SAG (2.5 nM) significantly increased the number of new cells and prolonged the survival of hippocampal cells. In mice, SAG (20 μg/g, I. p.) effectively prevents GC-induced neonatal cerebellar dysplasia. |
2-((5-chloro-2-((4-((4-methylpiperazin-1-yl)methyl)phenyl)amino)pyrimidin-4-yl)amino)-N,N-dimethylbenzenesulfonamide - Reference
| Reference Show more | 1 Mollard A, Warner SL, Call LT, Wade ML, Bearss JJ, Verma A, Sharma S, Vankayalapati H, Bearss DJ. Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors. ACS Med Chem Lett. 2011 Dec 8;2(12):907-912.2 ToleroPharmaceuticals, Inc–TP-0903. http://www.toleropharmaceuticals.com/TP-0903.html. |
2-((5-chloro-2-((4-((4-methylpiperazin-1-yl)methyl)phenyl)amino)pyrimidin-4-yl)amino)-N,N-dimethylbenzenesulfonamide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.938 ml | 9.689 ml | 19.378 ml |
| 5 mM | 0.388 ml | 1.938 ml | 3.876 ml |
| 10 mM | 0.194 ml | 0.969 ml | 1.938 ml |
| 5 mM | 0.039 ml | 0.194 ml | 0.388 ml |
Last Update：2024-01-02 23:10:35
2-((5-chloro-2-((4-((4-methylpiperazin-1-yl)methyl)phenyl)amino)pyrimidin-4-yl)amino)-N,N-dimethylbenzenesulfonamide - Cell Experiment
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, 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
Last Update：2023-08-16 21:32:38
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Product Name: TP-0903 Visit Supplier Webpage Request for quotation
CAS: 1341200-45-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1341200-45-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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