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Purity: ≥98%
I-BET151 (also known as GSK-1210151A) is a novel, potent and selective BET (Bromodomain and extra terminal domain) inhibitor with anticancer activity. It inhibits BRD2, BRD3 and BRD4 with IC50s of 0.5 μM, 0.25 μM, and 0.79 μM in cell-free assays, respectively. I-BET151 has the similar inhibition function as TMZ. When tested with 6 myeloma cell lines, I-BET151 treatment decreased cells percent in S/G2 phase and increased cell apoptosis in a time- and dose- dependent manner. In globlastoma cell line U87MG, administration of I-BET151 arrested cells in the G1 phase and reduced cell proliferation ability.
| ln Vitro |
I-BET151 (1 μM; 72 hours) treatment demonstrated that the majority of viable cells were in G0 phase, congruent with dose- and time-dependent decreases in cell proliferation and elimination of bromodeoxyuridine accumulation [2]. I-BET151 (100 nM; 72 hours) causes a dose- and time-dependent decrease in the fraction of S/G2 phase myeloma cells [2].
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| ln Vivo |
I-BET151 shows good oral systemic exposure and low blood clearance (roughly 20% hepatic blood flow) in rats, which translates into good oral bioavailability. Dogs exhibited high clearance, or about 95% of hepatic blood flow. In dogs, oral bioavailability can be as low as 16% due to low systemic exposure. While the low intrinsic clearance seen in rats and mice (mouse IVC 1.6 mL/min/g; CLb 8 mL/min/kg) is associated with lower in vivo blood clearance in these species, the high blood clearance in dogs is well correlated with the high intrinsic clearance observed in dog microsomes and hepatocytes. Owing to the low systemic exposure seen in dogs, minipigs were investigated as a possible second species for toxicological assessment. In these animals, I-BET151 demonstrated good bioavailability (65%) and low clearance (~32% hepatic blood flow)[1][2].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: H929 cells Tested Concentrations: 1 μM Incubation Duration: 72 hrs (hours) Experimental Results: 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 Types: H929 cells Tested Concentrations: 100 nM Incubation Duration: 72 hrs (hours) Experimental Results: Caused a significant dose- and time-dependent decrease in the proportion of myeloma cells in S/G2 phase. |
| Animal Protocol |
Animal/Disease Models: Mice (model of subcutaneous (sc) myeloma)[2]
Doses: 50 mg/kg Route of Administration: Ip; daily for 21 days Experimental Results: decreased rate of tumor size doubling than vehicle-treated mice. |
| References |
[1]. Seal J, et al. Identification of a novel series of BET family bromodomain inhibitors: Binding mode and profile of I-BET151 (GSK1210151A). Bioorg Med Chem Lett. 2012 Apr 15;22(8):2968-72.
[2]. Chaidos A, et al. Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood. 2014 Jan 30;123(5):697-705. |
| Molecular Formula |
C23H21N5O3
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| Molecular Weight |
415.44
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| CAS # |
1300031-49-5
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| Related CAS # |
I-BET151 dihydrochloride;1883545-47-8
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| SMILES |
O=C(N1[C@@H](C2=NC=CC=C2)C)NC3=C1C4=CC(OC)=C(C5=C(C)ON=C5C)C=C4N=C3
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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