BET bromodomain inhibitor. Downregulates Myc expression, causes G1 cell cycle arrest and attenuates cell proliferation in human pancreatic neuroendocrine tumors. Arrests the growth of T cell acute lymphoblastic leukemia cells in vitro (EC50 = 91.2 nM). Also enhances the antitumor effect of rapamycin (Cat. No. 1292) in vitro and attenuates rapamycin induced Akt activation. Orally bioavailable.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 399.9. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.5 mL||12.5 mL||25.01 mL|
|5 mM||0.5 mL||2.5 mL||5 mL|
|10 mM||0.25 mL||1.25 mL||2.5 mL|
|50 mM||0.05 mL||0.25 mL||0.5 mL|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
Wong et al (2014) The bromodomain and extra-terminal inhibitor CPI203 enhances the antiproliferative effects of rapamycin on human neuroendocrine tumors. Cell Death Dis. 5 e1450 PMID: 25299775
King et al (2013) The ubiquitin ligase FBXW7 modulates leukemia-initiating cell activity by regulating MYC stability. Cell 153 1552 PMID: 23791182
If you know of a relevant reference for CPI 203, please let us know.
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Keywords: CPI 203, supplier, CPI203, BET, BRD4, domain, inhibitors, inhibits, (+)-JQ1, analogue, analog, 4499, Myc, G1, cell, cycle, arrest, antitumor, rapamycin, AKT, Bromodomains, Cell, Cycle, Inhibitors, Bromodomains, Tocris Bioscience
Citations for CPI 203
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