CPI 203

Name: CPI 203
Brand: Tocris Bioscience
SKU: 5331
Rating: 5 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 5331

(1)

Citations (2)

COA / SDS

BET bromodomain inhibitor; arrests cell cycle at G1 phase

Key Product Details

Description:	BET bromodomain inhibitor; arrests cell cycle at G₁ phase
Alternative Names:	TEN 010
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)
Molecular Weight:	399.9

View Full Technical Details for CPI 203

Technical Data
Citations / Reviews (1)

Biological Activity for CPI 203

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.

Compound Libraries for CPI 203

CPI 203 is also offered as part of the Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.

Technical Data for CPI 203

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for CPI 203

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

Preparing Stock Solutions for CPI 203

The following data is based on the product molecular weight 399.9.

Batch specific molecular weights may vary from batch to batch due to the degree 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	2.50 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

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References for CPI 203

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