Network Version
I-BET151 Data Sheet
| Product Name: | I-BET151 |
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|---|---|---|
| CAS No.: | 1300031-49-5 | |
| Cat. No.: | HY-13235 | |
| MWt: | 415.44 | |
| Formula: | C23H21N5O3 | |
| Purity : | >98% | |
| Solubility: | DMSO : ≥ 100 mg/mL (240.71 mM) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
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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]. 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]. |
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