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I-BET151 (GSK1210151A)

Selective BET inhibitor CAS# 1300031-49-5

I-BET151 (GSK1210151A)

Catalog No. BCC4476----Order now to get a substantial discount!

Product Name & Size Price Stock
I-BET151 (GSK1210151A):5mg $93.00 In stock
I-BET151 (GSK1210151A):10mg $158.00 In stock
I-BET151 (GSK1210151A):25mg $372.00 In stock
I-BET151 (GSK1210151A):50mg $651.00 In stock
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Chemical structure

I-BET151 (GSK1210151A)

3D structure

Chemical Properties of I-BET151 (GSK1210151A)

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.
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.
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.

Biological Activity of I-BET151 (GSK1210151A)

DescriptionI-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.
TargetsBRD2BRD3BRD4   
IC500.5 μM0.25 μM0.79 μM    

Protocol

Cell Assay [2]
For in vitro cell proliferation and apoptosis assays, myeloma cell lines are cultured by using RPMI 1640 medium supplemented with 10% fetal bovine serum, 2 mM L-glutamine, penicillin 500 IU/mL, and streptomycin 500 μg/mL. Cells are placed in 96-well U-bottom plates at final concentration of 0.2×106 cells per milliliter in a humidified incubator with 5% CO2 at 37°C. For stroma vs nonstroma experiments, myeloma cells are placed in flat-bottom 96-well plates with MS5 cells at >90% confluence or in wells without stroma. Compounds (ie, I-BET151, I-BET762, the inactive isomer I-BET768, and JQ1) are serially diluted into media and added to the cultures at the indicated concentrations, starting from a 10-mM DMSO stock solution. Primary myeloma cells are cultured in flat-bottom 96-well plates in the presence of MS5 stroma cells by using complete medium as above, supplemented with interleukin-6 (IL-6) at 5 ng/mL[2].

Animal Administration [2]
Mice[2] NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice are used. In total, 5×106 KMS11 myeloma cells are injected subcutaneously into 9- to 12-week-old NSG mice. When tumors are ≥5 mm in maximum diameter, mice are randomized to receive once daily intraperitoneal injection of either I-BET151 30 mg/kg in 0.9% NaCl plus Kleptose hydroxypropyl betadex 10% (w/v) and DMSO 5% (v/v) pH 5.0 or vehicle solution for a maximum of 21 days.

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.

I-BET151 (GSK1210151A) Dilution Calculator

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I-BET151 (GSK1210151A) Molarity Calculator

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Preparing Stock Solutions of I-BET151 (GSK1210151A)

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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Background on I-BET151 (GSK1210151A)

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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References on I-BET151 (GSK1210151A)

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.

Description

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

Keywords:

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