1. Epigenetics
    Apoptosis
  2. Epigenetic Reader Domain
    Apoptosis
  3. CPI-203

CPI-203 

Cat. No.: HY-15846 Purity: 99.40%
Handling Instructions

CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain, with an IC50 value of appr 37 nM (BRD4 α-screen assay).

For research use only. We do not sell to patients.

CPI-203 Chemical Structure

CPI-203 Chemical Structure

CAS No. : 1446144-04-2

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
2 mg USD 72 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
25 mg USD 480 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain, with an IC50 value of appr 37 nM (BRD4 α-screen assay).

IC50 & Target

IC50: 37 nM (BRD4)

In Vitro

CPI-203 inhibits BRD4 in vitro and in cells, but does not affect BRD4 kinase activity in vitro[1]. CPI-203 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, CPI-203 efficiently activates the cell death program in MCL cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

CPI-203 (2.5 mg/kg, i.p.) combined with lenalidomide, enhances the antitumoral properties of each single agent via the abrogation of MYC and IRF4 expression and the induction of apoptosis in n REC-1 tumor-bearing mice[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

399.90

Formula

C₁₉H₁₈ClN₅OS

CAS No.

1446144-04-2

SMILES

ClC1=CC=C(C(C2=C(N3C4=NN=C3C)SC(C)=C2C)=N[[email protected]]4CC(N)=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 47 mg/mL (117.53 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5006 mL 12.5031 mL 25.0063 mL
5 mM 0.5001 mL 2.5006 mL 5.0013 mL
10 mM 0.2501 mL 1.2503 mL 2.5006 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.25 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.25 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.25 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[2]

CB17-severe combined immunodeficiency (SCID) mice are inoculated subcutaneously with 107 cells of the indicated MCL cell line, and monitored for tumor growth and vital parameters as previously described. For lenalidomide and lenalidomide-bortezomib dosing, mice are randomly assigned into cohorts of 3-4 mice each and receive by intraperitoneal injection a twice weekly dose of bortezomib (0.15 mg/kg), a daily dose of lenalidomide (50 mg/kg), the combination of lenalidomide and bortezomib, or an equal volume of vehicle. In the lenalidomide-CPI-203 protocol, a total of 22 REC-1 tumor-bearing mice are randomly assigned to cohorts of 5-6 mice, receiving a twice daily intraperitoneal injection of 2.5 mg/kg CPI-203, a daily intraperitoneal injection of 50 mg/kg lenalidomide, both agents or an equal volume of vehicle. Between 26 and 29 days post-inoculation, animals are killed according to institutional guidelines and tumor samples are subjected to immunohistochemical staining using primary antibodies against phospho-histone H3, cleaved caspase-3 (5A1E) and MYC (D84C12), IRF4 (M-17) and platelet endothelial cell adhesion molecule-1 (PECAM-1) (M20), CD19 (LE-CD19), Blimp-1 (clone Ros195G/G5), PAX5 (clone 24), CCL3 and CD38, as previously described. Preparations are evaluated using an Olympus DP70 microscope and Cell B Basic Imaging Software.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

CPI-203CPI203CPI 203Epigenetic Reader DomainApoptosisInhibitorinhibitorinhibit

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CPI-203
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