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  3. CPI-0610

CPI-0610 

Cat. No.: HY-12863 Purity: 99.95%
Handling Instructions

CPI-0610 is a potent, selective, and cell-active BET inhibitor. CPI-0610 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.

CPI-0610 Chemical Structure

CPI-0610 Chemical Structure

CAS No. : 1380087-89-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
50 mg USD 550 In-stock
Estimated Time of Arrival: December 31
100 mg USD 930 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

CPI-0610 is a potent, selective, and cell-active BET inhibitor. CPI-0610 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

CPI-0610 (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].
CPI-0610 (800 nM; 72 hours; INA6 and MM.1S cells) treatment leads to G1 cell cycle arrest[2].
CPI-0610 (800 nM; 72 hours; INA6 and MM.1S cells) treatment significantly increases apoptosis in MM cells after 72 hours[2].

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

CPI-0610 (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].

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.

1380087-89-7

SMILES

O=C(N)C[[email protected]@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)

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
10 mM 0.2734 mL 1.3668 mL 2.7337 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 (6.83 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (6.83 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.83 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.95%

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Keywords:

CPI-0610CPI0610CPI 0610Epigenetic Reader DomainInhibitorinhibitorinhibit

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CPI-0610
Cat. No.:
HY-12863
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