CPI 203

Cat. No. 5331

CPI 203 C19H18ClN5OS [1446144-04-2]

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Chemical Name: (6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide

Biological Activity

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.

Technical Data

M.Wt:
399.9
Formula:
C19H18ClN5OS
Solubility:
Soluble to 100 mM in DMSO and to 10 mM in ethanol
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
1446144-04-2

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

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.

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Citations are publications that use Tocris products.

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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, Tocris Bioscience, Bromodomain Inhibitor products

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