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Reactivos e instrumentos para inmunología, biología celular y biología molecular.

I-BET151 [1300031-49-5]

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Referencia HY-13235-5mg

embalaje : 5mg

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Teléfono : +1 850 650 7790

Marca : MedChemExpress

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Teléfono : +1 850 650 7790

Descripciòn

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]

Cellular Effect

Cell Line	Type	Value	Description	References
HEL	IC₅₀	1 μM Compound: I-BET151, GSK1210151A	Antiproliferative activity against human HEL cells harboring JAK2 V617F mutant assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay Antiproliferative activity against human HEL cells harboring JAK2 V617F mutant assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay	[PMID: 21964340]
HL-60	IC₅₀	195 nM Compound: I-BET151	Antiproliferative activity against human HL-60 cells after 72 hrs by cell titer glo assay Antiproliferative activity against human HL-60 cells after 72 hrs by cell titer glo assay	[PMID: 32691589]
HL-60	IC₅₀	890 nM Compound: I-BET151, GSK1210151A	Antiproliferative activity against human HL-60 cells harboring N-RAS assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay Antiproliferative activity against human HL-60 cells harboring N-RAS assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay	[PMID: 21964340]
HT-29	IC₅₀	0.945 μM Compound: 3, I-BET151	Growth inhibition of human HT-29 cells after 72 hrs by SRB assay Growth inhibition of human HT-29 cells after 72 hrs by SRB assay	[PMID: 25559428]
K562	IC₅₀	> 100 μM Compound: I-BET151, GSK1210151A	Antiproliferative activity against human K562 cells harboring BCR-ABL assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay Antiproliferative activity against human K562 cells harboring BCR-ABL assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay	[PMID: 21964340]
K562	IC₅₀	> 2000 nM Compound: 3, I-BET-151	Cytotoxicity against human K562 cells harboring BCR-ABL fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay Cytotoxicity against human K562 cells harboring BCR-ABL fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay	[PMID: 26080064]
MEG-01	IC₅₀	25 μM Compound: I-BET151, GSK1210151A	Antiproliferative activity against human MEG-01 cells harboring BCR-ABL assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay Antiproliferative activity against human MEG-01 cells harboring BCR-ABL assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay	[PMID: 21964340]
MM1.S	IC₅₀	0.299 μM Compound: 3, I-BET151	Growth inhibition of human MM1S cells after 72 hrs by SRB assay Growth inhibition of human MM1S cells after 72 hrs by SRB assay	[PMID: 25559428]
MOLM-13	IC₅₀	120 nM Compound: I-BET151, GSK1210151A	Antiproliferative activity against human MOLM-13 cells harboring MLL-AF9 assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay Antiproliferative activity against human MOLM-13 cells harboring MLL-AF9 assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay	[PMID: 21964340]
MOLM-13	IC₅₀	228 nM Compound: 3, I-BET-151	Cytotoxicity against human MOLM13 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay Cytotoxicity against human MOLM13 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay	[PMID: 26080064]
MOLM-13	IC₅₀	228 nM Compound: 5; I-BET151	Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay	[PMID: 28463487]
MV4-11	IC₅₀	0.119 μM Compound: 3, I-BET151	Growth inhibition of human MV4-11 cells after 72 hrs by SRB assay Growth inhibition of human MV4-11 cells after 72 hrs by SRB assay	[PMID: 25559428]
MV4-11	IC₅₀	126.9 nM Compound: I-BET151	Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer glo assay Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer glo assay	[PMID: 32691589]
MV4-11	IC₅₀	162 nM Compound: 3, I-BET-151	Cytotoxicity against human MV4-11 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay Cytotoxicity against human MV4-11 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay	[PMID: 26080064]
MV4-11	IC₅₀	162 nM Compound: 5; I-BET151	Growth inhibition of human MV4-11 cells after 4 days by WST-8 assay Growth inhibition of human MV4-11 cells after 4 days by WST-8 assay	[PMID: 28463487]
MV4-11	IC₅₀	167 nM Compound: I-BET151, GSK1210151A	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay	[PMID: 21964340]
MV4-11	IC₅₀	26 nM Compound: I-BET151, GSK1210151A	Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay	[PMID: 21964340]
NOMO-1	IC₅₀	15 nM Compound: I-BET151, GSK1210151A	Antiproliferative activity against human NOMO-1 cells harboring MLL-AF9 assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay Antiproliferative activity against human NOMO-1 cells harboring MLL-AF9 assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay	[PMID: 21964340]
PBMC	IC₅₀	0.16 μM Compound: I-BET151, GSK1210151A	Anti-inflammatory activity against LPS-stimulated human PBMC assessed as IL-6 production Anti-inflammatory activity against LPS-stimulated human PBMC assessed as IL-6 production	[PMID: 21964340]
RS4-11	IC₅₀	192 nM Compound: I-BET151, GSK1210151A	Antiproliferative activity against human RS4-11 cells harboring MLL-AF4 assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay Antiproliferative activity against human RS4-11 cells harboring MLL-AF4 assessed as inhibition of cell growth incubated for 4 hrs by CellTiter-Aqueous One assay	[PMID: 21964340]
Raji	IC₅₀	0.13 μM Compound: I-BET151, GSK1210151A	Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs	[PMID: 24900758]
THP-1	IC₅₀	134.2 nM Compound: I-BET151	Antiproliferative activity against human THP-1 cells after 72 hrs by cell titer glo assay Antiproliferative activity against human THP-1 cells after 72 hrs by cell titer glo assay	[PMID: 32691589]

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].

MedChemExpress (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 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].

MedChemExpress (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.

Peso molecular

415.44

Fòrmula

C₂₃H₂₁N₅O₃

No. CAS

1300031-49-5

Appearance

Solid

Color

White to khaki

SMILES

C[C@@H](N1C(C(C=C(OC)C(C2=C(C)ON=C2C)=C3)=C3N=C4)=C4NC1=O)C5=CC=CC=N5

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvente y solubilidad

In Vitro:

DMSO : ≥ 100 mg/mL (240.71 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution
Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution
Protocol 6

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: 0.5 mg/mL (1.20 mM); Suspended solution; Need ultrasonic

Pureza y Documentación

Purity: 99.47%

Ficha de datos (286 KB) SDS (479 KB)

COA (261 KB) LCMS (96 KB)

Instrucciones de manejo (2659 KB)

Referencias

[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. [Content Brief]

[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. [Content Brief]

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Referencia HY-13235-5mg

Contact local distributor :

Marca : MedChemExpress

Contact local distributor :

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