CPI 203

Product Description

CPI 203 is a 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. Also enhances fibroblast reprogramming to hiPSCs at low concentration. Orally bioavailable.

Solubility

Preparing Stock Solutions for CPI 203

The following data is based on the product molecular weight 399.90

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.50 mL	12.50 mL	25.01 mL
5 mM	0.50 mL	2.50 mL	5.00 mL
10 mM	0.25 mL	1.25 mL	2.50 mL
50 mM	0.05 mL	0.25 mL	0.50 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• King The ubiquitin ligase FBXW7 modulates leukemia-initiating cell activity by regulating MYC stability. Cell 2013 PMID: 23791182
• Shao Reprogramming by de-bookmarking the somatic transcriptional program through targeting of BET bromodomains. Cell Rep. 2016 PMID: 27653680
• Wong The bromodomain and extra-terminal inhibitor CPI203 enhances the antiproliferative effects of rapamycin on human neuroendocrine tumors. Cell Death Dis. 2014 PMID: 25299775