2. Epigenetics
  3. Epigenetic Reader Domain
  4. Pelabresib

Pelabresib  (Synonyms: CPI-0610)

Cat. No.: HY-12863 Purity: 99.95%
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Pelabresib (CPI-0610) is a potent, selective, orally active and cell-active BET inhibitor. Pelabresib inhibits BRD4-BD1 with an IC50 of 39 nM, and with an EC50 value of 0.18 μM for MYC.

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

Pelabresib Chemical Structure

Pelabresib Chemical Structure

CAS No. : 1380087-89-7

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10 mM * 1 mL in DMSO
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25 mg USD 660 In-stock
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Based on 1 publication(s) in Google Scholar

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Pelabresib Related Antibodies

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Description

Pelabresib (CPI-0610) is a potent, selective, orally active and cell-active BET inhibitor. Pelabresib inhibits BRD4-BD1 with an IC50 of 39 nM, and with an EC50 value of 0.18 μM for MYC[1].

IC50 & Target[1]

BRD4-BD1

39 nM (IC50)

In Vitro

Pelabresib (0-1500 nM; 72 hours; Multiple myeloma cell lines and primary MM cells) treatment reduces the viability of MM cells in a dose-dependent manner[2].
Pelabresib (800 nM; 72 hours; INA6 and MM.1S cells) treatment leads to G1 cell cycle arrest[2].
Pelabresib (800 nM; 72 hours; INA6 and MM.1S cells) treatment significantly increases apoptosis in MM cells after 72 hours[2].

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

Pelabresib Related Antibodies

Cell Viability Assay[2]

Cell Line: Multiple myeloma (MM) cell lines and primary MM cells
Concentration: 0 nM, 200 nM, 400 nM, 600 nM , 800 nM, 1000 nM, 1200 nM, or 1500 nM
Incubation Time: 72 huors
Result: Decreased viability of MM cells in a dose-dependent manner.

Cell Cycle Analysis[2]

Cell Line: INA6 and MM.1S cells
Concentration: 800 nM
Incubation Time: 72 hours
Result: Indeced G1 cell cycle arrest.

Apoptosis Analysis[2]

Cell Line: INA6 and MM.1S cells
Concentration: 800 nM
Incubation Time: 72 hours
Result: MM cells apoptosis was increased after 72 hours.
In Vivo

Pelabresib (30-60 mg/kg; oral administration; for 28 days; MV-4-11 mouse xenograft model) treatment results in substantial suppression of tumor growth over the time period examined (41%, 80%, and 74% tumor growth inhibition, respectively), without any significant body weight loss in the animals[1].

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

Animal Model: MV-4-11 mouse xenograft model[1]
Dosage: 30 mg/kg once daily, 30 mg/kg twice daily, or 60 mg/kg once daily
Administration: Oral administration; for 28 days
Result: Suppressed of tumor growth, without any significant body weight loss in the animals.
Molecular Weight

365.81

Formula

C20H16ClN3O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N)C[C@@H]1N=C(C2=CC=C(Cl)C=C2)C3=CC=CC=C3C4=C1ON=C4C
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 : 100 mg/mL (273.37 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 2.7337 mL 13.6683 mL 27.3366 mL
5 mM 0.5467 mL 2.7337 mL 5.4673 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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: ≥ 2.08 mg/mL (5.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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

Purity: 99.95%

SDS (251 KB)

COA (258 KB) LCMS (120 KB)

Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7337 mL 13.6683 mL 27.3366 mL 68.3415 mL
5 mM 0.5467 mL 2.7337 mL 5.4673 mL 13.6683 mL
10 mM 0.2734 mL 1.3668 mL 2.7337 mL 6.8341 mL
15 mM 0.1822 mL 0.9112 mL 1.8224 mL 4.5561 mL
20 mM 0.1367 mL 0.6834 mL 1.3668 mL 3.4171 mL
25 mM 0.1093 mL 0.5467 mL 1.0935 mL 2.7337 mL
30 mM 0.0911 mL 0.4556 mL 0.9112 mL 2.2780 mL
40 mM 0.0683 mL 0.3417 mL 0.6834 mL 1.7085 mL
50 mM 0.0547 mL 0.2734 mL 0.5467 mL 1.3668 mL
60 mM 0.0456 mL 0.2278 mL 0.4556 mL 1.1390 mL
80 mM 0.0342 mL 0.1709 mL 0.3417 mL 0.8543 mL
100 mM 0.0273 mL 0.1367 mL 0.2734 mL 0.6834 mL
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Pelabresib 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:

Pelabresib1380087-89-7CPI-0610CPI0610CPI 0610Epigenetic Reader DomainInhibitorinhibitorinhibit

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