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  3. I-BET151 dihydrochloride

I-BET151 dihydrochloride (Synonyms: GSK1210151A dihydrochloride)

Cat. No.: HY-110106
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I-BET151 dihydrochloride (GSK1210151A dihydrochloride) 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 dihydrochloride Chemical Structure

I-BET151 dihydrochloride Chemical Structure

CAS No. : 1883545-47-8

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Description

I-BET151 dihydrochloride (GSK1210151A dihydrochloride) 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 dihydrochloride (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 dihydrochloride (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 dihydrochloride 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 dihydrochloride 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 dihydrochloride (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

488.37

Formula

C₂₃H₂₃Cl₂N₅O₃

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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I-BET151 dihydrochloride
Cat. No.:
HY-110106
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