CPI-637

Name: CPI-637
Brand: MedChemExpress
SKU: HY-100482
Rating: 5.0 (11 reviews)

Cat. No.: HY-100482 Purity: 99.91%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

CPI-637 is a selective and potent CBP/EP300 bromodomain inhibitor with IC₅₀ values of 0.03 μM, 0.051 μM and 11.0 μM for CBP, EP300 and BRD4 BD-1, respectively, and an EC₅₀ of 0.3 μM for CBP.

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

CPI-637 Chemical Structure

CAS No. : 1884712-47-3

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 106	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 106	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 96	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 144	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 720	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 11 publication(s) in Google Scholar

11 Publications Citing Use of MCE CPI-637

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

BRD4 BD1

11 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	IC₅₀	3.13 μM Compound: 2; CPI-637	Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition by Celltiter-Glo assay Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition by Celltiter-Glo assay	[PMID: 34962793]
HEK293	EC₅₀	0.3 μM Compound: 28; CPI-637	Inhibition of Halo-tagged histone H3.3 binding to CBP (unknown origin) expressed in HEK293 cells after overnight incubation by luciferase reporter gene based BRET assay Inhibition of Halo-tagged histone H3.3 binding to CBP (unknown origin) expressed in HEK293 cells after overnight incubation by luciferase reporter gene based BRET assay	[PMID: 27190605]
LNCaP	IC₅₀	0.65 μM Compound: 2; CPI-637	Antiproliferative activity against human LNCaP cells assessed as cell growth inhibition by Celltiter-Glo assay Antiproliferative activity against human LNCaP cells assessed as cell growth inhibition by Celltiter-Glo assay	[PMID: 34962793]
LNCaP C4-2B	IC₅₀	3.35 μM Compound: 2; CPI-637	Antiproliferative activity against human LNCaP C4-2B cells assessed as inhibition of cell growth by Celltiter-Glo assay Antiproliferative activity against human LNCaP C4-2B cells assessed as inhibition of cell growth by Celltiter-Glo assay	[PMID: 34962793]

In Vitro

CPI-637 (Compound 28) inhibits MYC expression in AMO-1 cells (EC₅₀ value of 0.60 μM) ^[1].

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

Molecular Weight

386.45

Formula

C₂₂H₂₂N₆O

CAS No.

1884712-47-3

Appearance

Solid

Color

White to off-white

SMILES

O=C1NC2=CC=CC(C3=CC4=C(N(C)N=C4C5=CN(C)N=C5)C=C3)=C2N[C@H](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 : 9.62 mg/mL (24.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5877 mL	12.9383 mL	25.8766 mL
5 mM	0.5175 mL	2.5877 mL	5.1753 mL
10 mM	0.2588 mL	1.2938 mL	2.5877 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 0.96 mg/mL (2.48 mM); Clear solution

This protocol yields a clear solution of ≥ 0.96 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (9.6 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: 0.96 mg/mL (2.48 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 0.96 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (9.6 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.96 mg/mL (2.48 mM); Clear solution

This protocol yields a clear solution of ≥ 0.96 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (9.6 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Purity: 99.94%

Select Batch:

Data Sheet (278 KB) SDS (251 KB)

COA (256 KB) HNMR (183 KB) LCMS (325 KB)

Handling Instructions (2659 KB)

References

[1]. Taylor AM, et al. Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637). ACS Med Chem Lett. 2016 Mar 15;7(5):531-6. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5877 mL	12.9383 mL	25.8766 mL	64.6914 mL
	5 mM	0.5175 mL	2.5877 mL	5.1753 mL	12.9383 mL
	10 mM	0.2588 mL	1.2938 mL	2.5877 mL	6.4691 mL
	15 mM	0.1725 mL	0.8626 mL	1.7251 mL	4.3128 mL
	20 mM	0.1294 mL	0.6469 mL	1.2938 mL	3.2346 mL

CPI-637 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-6371884712-47-3CPI637CPI 637Epigenetic Reader DomainHistone AcetyltransferaseHATsHATInhibitorinhibitorinhibit

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CPI-637

Customer Review

CPI-637 Related Antibodies

11 Publications Citing Use of MCE CPI-637

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Acetyltransferase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

CPI-637 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

CPI-637 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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SAFETY DATA SHEET (SDS)

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