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  3. I-BET282

I-BET282 

Cat. No.: HY-19760 Purity: 99.11%
Handling Instructions

I-BET282 is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282 shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD).

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

I-BET282 Chemical Structure

I-BET282 Chemical Structure

CAS No. : 1422554-34-4

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 99 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 750 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

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Description

I-BET282 is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282 shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD)[1].

In Vitro

I-BET282 has a weak inhibition of the hERG potassium ion channel (pIC50 4.4-5.1 in a variety of assay formats). I-BET282 shows a low potential to inhibit CYP proteins in vitro, with no evidence of time-dependent inhibition of 2D6 or 3A4[1].

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

In Vivo

I-BET282 (Male CD1 Mice; 3 mg/kg-p.o.; 1 mg/kg-i.v.) treatment shows the Clb, LBF, Vss, t1/2 (i.v.), and F values of 23 mL/min/kg, 19%, 1.9 L/kg, and 51%, respectively. I-BET282 (Male Wistar Han Rats; 1 mg/kg; p.o.) treatment shows the AUC0-t, Cmax and Tmax values of 467 ng h/mL, 125 ng/mL, and 1 hour, respectively[1].

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

Molecular Weight

450.53

Formula

C₂₅H₃₀N₄O₄

CAS No.
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 (221.96 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2196 mL 11.0980 mL 22.1961 mL
5 mM 0.4439 mL 2.2196 mL 4.4392 mL
10 mM 0.2220 mL 1.1098 mL 2.2196 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 (5.55 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
I-BET282
Cat. No.:
HY-19760
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