TP-0903

Modify Date: 2024-01-06 21:48:41

TP-0903 Structure
TP-0903 structure
Common Name TP-0903
CAS Number 1341200-45-0 Molecular Weight 516.059
Density 1.3±0.1 g/cm3 Boiling Point 664.7±65.0 °C at 760 mmHg
Molecular Formula C24H30ClN7O2S Melting Point N/A
MSDS N/A Flash Point 355.8±34.3 °C

 Use of TP-0903


TP-0903 is a potent and selective Axl receptor tyrosine kinase inhibitor with an IC50 value of 27 nM.

 Names

Name 2-((5-chloro-2-((4-((4-methylpiperazin-1-yl)methyl)phenyl)amino)pyrimidin-4-yl)amino)-N,N-dimethylbenzenesulfonamide
Synonym More Synonyms

 TP-0903 Biological Activity

Description TP-0903 is a potent and selective Axl receptor tyrosine kinase inhibitor with an IC50 value of 27 nM.
Related Catalog
Target

IC50: 27nM (Axl)[1]

In Vitro TP-0903 displays a potent activity against AXL with an IC50 of 0.027 μM. 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[1].
Kinase Assay TP-0903 is diluted in kinase reaction buffer and are briefly incubated with Axl kinase. The reaction is initiated by the addition of ATP and fluorescein-labeled poly-GT substrate. Concentration of the various components in the assay (10 μL reaction volume) are: 1% DMSO, 93 ng/mL Axl kinase, 20 μL ATP, and 200 nM fluorescein poly-GT substrate. The incubation is for 60 min at room temperature, the enzyme reaction is stopped by addition of 10 μL terbium-labeled anti-phosphotyrosine PY20 antibody in EDTA-containing buffer. Final concentration of EDTA and antibody after addition to the reaction is 10 mM and 2 nM, respectively. After one hour incubation at room temperature, fluorescence is measured with excitation of 320 nm and dual emission of 495 and 520 nm on an microplate reader[1].
Cell Assay 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[1].
References

[1]. Mollard A, et al. Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors. ACS Med Chem Lett. 2011 Dec 8;2(12):907-912.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 664.7±65.0 °C at 760 mmHg
Molecular Formula C24H30ClN7O2S
Molecular Weight 516.059
Flash Point 355.8±34.3 °C
Exact Mass 515.187012
PSA 102.08000
LogP 2.30
Vapour Pressure 0.0±2.0 mmHg at 25°C
Index of Refraction 1.648
Storage condition -20℃

 Synonyms

Benzenesulfonamide, 2-[[5-chloro-2-[[4-[(4-methyl-1-piperazinyl)methyl]phenyl]amino]-4-pyrimidinyl]amino]-N,N-dimethyl-
2-{[5-Chloro-2-({4-[(4-methyl-1-piperazinyl)methyl]phenyl}amino)-4-pyrimidinyl]amino}-N,N-dimethylbenzenesulfonamide
tp0903
TP-0903
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Price: $136/10mM*1mLinDMSO

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