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  3. I-BET151

I-BET151 (Synonyms: GSK1210151A)

Cat. No.: HY-13235 Purity: 99.81%
Handling Instructions

I-BET151 (GSK1210151A) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively.

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

I-BET151 Chemical Structure

I-BET151 Chemical Structure

CAS No. : 1300031-49-5

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Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 132 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 432 In-stock
Estimated Time of Arrival: December 31
100 mg USD 756 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 16 publication(s) in Google Scholar

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Description

I-BET151 (GSK1210151A) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively[1][2].

IC50 & Target

pIC50: 6.1 (BRD4), 6.3 (BRD2), 6.6 (BRD3)[1]

In Vitro

I-BET151 (1 μM; 72 hours) treatment displays the majority of live cells resided in the G0 phase and commensurate with a dose- and time-dependent decrease in cell proliferation and abrogation of bromodeoxyuridine incorporation[2].
I-BET151 (100 nM; 72 hours) causes a significant dose- and time-dependent decrease in the proportion of myeloma cells in S/G2 phase[2].

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

Cell Viability Assay[2]

Cell Line: H929 cells
Concentration: 1 μM
Incubation Time: 72 hours
Result: Displays the majority of live cells resided in the G0 phase and commensurate with a dose- and time-dependent decrease in cell proliferation and abrogation of bromodeoxyuridine incorporation.

Cell Proliferation Assay[2]

Cell Line: H929 cells
Concentration: 100 nM
Incubation Time: 72 hours
Result: Caused a significant dose- and time-dependent decrease in the proportion of myeloma cells in S/G2 phase.
In Vivo

I-BET151 demonstrates low blood clearance in the rat (~20% liver blood flow) and good oral systemic exposure which resulted in good oral bioavailability. High clearance is observed in the dog (~95% liver blood flow). The systemic exposure in the dog is low, resulting in a poor oral bioavailability of 16%. The high blood clearance in dog correlates well with the high intrinsic clearance observed in dog microsomes and hepatocytes, whereas the low intrinsic clearances seen in rat and mouse (mouse IVC 1.6 mL/min/g; CLb 8 mL/min/kg) correlate with lower in vivo blood clearances in these species. Due to the low systemic exposure observed in the dog, I-BET151 is investigated in the mini-pig as a potential second species for toxicological evaluation where it showed low clearance (~32% liver blood flow) and good bioavailability (65%)[1].
I-BET151 (30 mg/kg; i.p.; daily for 21 days)-treats mice has four- to five fold smaller myeloma tumors and a significantly reduces rate of tumor size doubling than vehicle-treated mice[2].

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

Animal Model: Mice (model of subcutaneous myeloma)[2]
Dosage: 50 mg/kg
Administration: I.p.; daily for 21 days
Result: Reduced rate of tumor size doubling than vehicle-treated mice.
Molecular Weight

415.44

Formula

C₂₃H₂₁N₅O₃

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 (240.71 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4071 mL 12.0354 mL 24.0709 mL
5 mM 0.4814 mL 2.4071 mL 4.8142 mL
10 mM 0.2407 mL 1.2035 mL 2.4071 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 (6.02 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

  • 4.

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

  • 5.

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

  • 6.

    Add each solvent one by one:  1% DMSO    99% saline

    Solubility: 0.5 mg/mL (1.20 mM); Suspended solution; Need ultrasonic

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

Purity: 99.81%

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Product Name:
I-BET151
Cat. No.:
HY-13235
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