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CPI-203 Epigenetic Reader Domain inhibitor

Name: CPI-203
Brand: Selleck Chemicals
SKU: S7304
Availability: InStock
Rating: 5 (15 reviews)

Cat.No.S7304

CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.

Chemical Structure

Molecular Weight: 399.90

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.69%

99.69

Related Targets	HDAC JAK Histone Methyltransferase AMPK PKC PARP HIF Histone Acetyltransferase Aurora Kinase Sirtuin PRMT Histone Demethylase EZH1/2 DNA Methyltransferase Pim LSD1 MLL JMJD G9a/GLP NSD FTO MicroRNA PAD SETD SMYD DOT1 COMT WDR5 HNMT SAM MTase
Related Products	Birabresib (OTX015) I-BET151 (GSK1210151A) Molibresib (I-BET-762) SGC-CBP30 EED226 Apabetalone (RVX-208) KG-501 compound 3i (666-15) PFI-3 AZD5153 6-hydroxy-2-naphthoic acid PFI-1 (PF-6405761) Mivebresib (ABBV-075) ABBV-744 UNC1215 I-BRD9 Bromosporine PLX51107 GSK1324726A (I-BET726) Pelabresib (CPI-0610) PF-CBP1 HCl INCB054329 MS436 GSK2801 UNC669 MZ-1 NEO2734 (EP31670) OF-1 CPI-637 GSK6853 I-CBP112

Chemical Information, Storage & Stability

Molecular Weight	399.90	Formula	C₁₉H₁₈ClN₅OS	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1446144-04-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)N)C4=CC=C(C=C4)Cl)C

Solubility

In vitro
Batch:

DMSO : 79 mg/mL (197.54 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 46 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.950mg/ml (9.88mM)	Taking the 1 mL working solution as an example, add 50 μL of 79 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.658mg/ml (1.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 13.16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	IL-6 ^[1] (Cell-based assay) 30 nM BRD4 ^[1] (Cell-free assay) 37 nM MYC ^[1] (Cell-based assay) 99 nM
In vitro	CPI203 inhibits BRD4 in vitro and in cells, while does not affect BRD4 kinase activity in vitro. ^[1] CPI203 exerts a cytostatic effect in all the 9 MCL cell lines analyzed with GI50 ranging from 0.06 to 0.71 μM, with low cytotoxicity in normal PBMCs from healthy donors. Furthermore, CPI203, by targeting IRF4 and MYC, efficiently activates the cell death program in MCL cells. ^[2]
Kinase Assay	BRD4 α-screen assay
Kinase Assay	The BRD4 α-screen assay is a proximity-based assay using a tetraacteylated H4 peptide and the isolated bromodomain 1 of human BRD4. IC50 values are calculated using a 10-point serial dilution of BET inhibitor.
In vivo	BRD4 mediates CTD Ser2 phosphorylation in vivo. ^[1] In REC-1 tumor-bearing mice, the combination of CPI203 (2.5 mg/kg i.p.) synergistically augments the antitumoral properties of each single agent via the abrogation of MYC and IRF4 expression and the induction of apoptosis. ^[2]
References	[1] https://pubmed.ncbi.nlm.nih.gov/22509028/ [2] https://pubmed.ncbi.nlm.nih.gov/24721791/

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