I-BET151 (GSK1210151A)Selective BET inhibitor CAS# 1300031-49-5 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 1300031-49-5 | SDF | Download SDF |
| PubChem ID | 52912189 | Appearance | Powder |
| Formula | C23H21N5O3 | M.Wt | 415.44 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | GSK1210151A | ||
| Solubility | DMSO : ≥ 100 mg/mL (240.71 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 7-(3,5-dimethyl-1,2-oxazol-4-yl)-8-methoxy-1-[(1R)-1-pyridin-2-ylethyl]-3H-imidazo[4,5-c]quinolin-2-one | ||
| SMILES | CC1=C(C(=NO1)C)C2=C(C=C3C(=C2)N=CC4=C3N(C(=O)N4)C(C)C5=CC=CC=N5)OC | ||
| Standard InChIKey | VUVUVNZRUGEAHB-CYBMUJFWSA-N | ||
| Standard InChI | InChI=1S/C23H21N5O3/c1-12-21(14(3)31-27-12)16-9-18-15(10-20(16)30-4)22-19(11-25-18)26-23(29)28(22)13(2)17-7-5-6-8-24-17/h5-11,13H,1-4H3,(H,26,29)/t13-/m1/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | I-BET151 is a selective inhibitor of BET with IC50 value of 0.5 μM, 0.25 μM and 0.79 μM for BRD2, BRD3 and BRD4, respectively. | |||||
| Targets | BRD2 | BRD3 | BRD4 | |||
| IC50 | 0.5 μM | 0.25 μM | 0.79 μM | |||
I-BET151 (GSK1210151A) Dilution Calculator
I-BET151 (GSK1210151A) Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.4071 mL | 12.0354 mL | 24.0709 mL | 48.1417 mL | 60.1772 mL |
| 5 mM | 0.4814 mL | 2.4071 mL | 4.8142 mL | 9.6283 mL | 12.0354 mL |
| 10 mM | 0.2407 mL | 1.2035 mL | 2.4071 mL | 4.8142 mL | 6.0177 mL |
| 50 mM | 0.0481 mL | 0.2407 mL | 0.4814 mL | 0.9628 mL | 1.2035 mL |
| 100 mM | 0.0241 mL | 0.1204 mL | 0.2407 mL | 0.4814 mL | 0.6018 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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I-BET151 (GSK1210151A) is a selective inhibitor of BET with pIC50 value of 6.1 [1].
BET (bromo and extraterminal) is a member of bromodomain family and has been shown to be associated with a variety of diseases (human squamous cell carcinoma and other cancers). BET inhibitor has been implicated as a promising therapy for human cancer treatment [2].
I-BET151 is a selective BET inhibitor and 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 [2]. In globlastoma cell line U87MG, administration of I-BET151 arrested cells in the G1 phase and reduced cell proliferation ability [3].
When treated with myeloma implanted mouse model with I-BET151, it reduced tumor volume in a four- or five- fold compared with control group [2]. In immunocompromised mouse model with U87MG cells xenograft, administration of I-BET151 in a concentration of 10 mg/kg i.p. daily significantly reduced tumor volume compared with saline treated group [3].
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. 22(8): p. 2968-72.
[2]. Chaidos, A., et al., Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood, 2014. 123(5): p. 697-705.
[3]. Chan, C.H., et al., BET bromodomain inhibition suppresses transcriptional responses to cytokine-Jak-STAT signaling in a gene-specific manner in human monocytes. Eur J Immunol, 2015. 45(1): p. 287-97.
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Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).[Pubmed:22437115]
Bioorg Med Chem Lett. 2012 Apr 15;22(8):2968-72.
A novel series of quinoline isoxazole BET family bromodomain inhibitors are discussed. Crystallography is used to illustrate binding modes and rationalize their SAR. One member, I-BET151 (GSK1210151A), shows good oral bioavailability in both the rat and minipig as well as demonstrating efficient suppression of bacterial induced inflammation and sepsis in a murine in vivo endotoxaemia model.
