CPI 203

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Cat.No. 5331 - CPI 203 | C19H18ClN5OS | CAS No. 1446144-04-2
Description: BET bromodomain inhibitor; arrests cell cycle at G1 phase
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
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

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.

Compound Libraries

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Technical Data

M. Wt 399.9
Formula C19H18ClN5OS
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1446144-04-2
PubChem ID 71291068
InChI Key QECMENZMDBOLDR-AWEZNQCLSA-N
Smiles NC(C[C@@H]1N=C(C4=CC=C(Cl)C=C4)C3=C(SC(C)=C3C)N2C1=NN=C2C)=O

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 4 10
DMSO 39.99 100

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

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References

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

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 for CPI 203

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Literature in this Area

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Cancer

Cancer Research Product Guide

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Epigenetics

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics

Epigenetics Research Bulletin

Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

  • Bromodomains
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Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.