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

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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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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 USD 121 In-stock
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10 mM * 1 mL in DMSO USD 121 In-stock
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2 mg USD 60 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of CPI-203:

CPI-203 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

CPI-203 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

399.90

Formula

C19H18ClN5OS
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

ClC1=CC=C(C(C2=C(N3C4=NN=C3C)SC(C)=C2C)=N[C@H]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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 47 mg/mL (117.53 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5006 mL 12.5031 mL 25.0063 mL 62.5156 mL
5 mM 0.5001 mL 2.5006 mL 5.0013 mL 12.5031 mL
10 mM 0.2501 mL 1.2503 mL 2.5006 mL 6.2516 mL
15 mM 0.1667 mL 0.8335 mL 1.6671 mL 4.1677 mL
20 mM 0.1250 mL 0.6252 mL 1.2503 mL 3.1258 mL
25 mM 0.1000 mL 0.5001 mL 1.0003 mL 2.5006 mL
30 mM 0.0834 mL 0.4168 mL 0.8335 mL 2.0839 mL
40 mM 0.0625 mL 0.3126 mL 0.6252 mL 1.5629 mL
50 mM 0.0500 mL 0.2501 mL 0.5001 mL 1.2503 mL
60 mM 0.0417 mL 0.2084 mL 0.4168 mL 1.0419 mL
80 mM 0.0313 mL 0.1563 mL 0.3126 mL 0.7814 mL
100 mM 0.0250 mL 0.1250 mL 0.2501 mL 0.6252 mL
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CPI-203 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CPI-2031446144-04-2CPI203CPI 203Epigenetic Reader DomainApoptosisInhibitorinhibitorinhibit

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