Molibresib (Synonyms: I-BET762; GSK525762; GSK525762A)

目录号: HY-13032 纯度: 99.94%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Molibresib (I-BET762; GSK525762) 是 BET 溴结构域 抑制剂，IC₅₀ 为32.5-42.5 nM。

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Molibresib Chemical Structure

CAS No. : 1260907-17-2

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1026	In-stock
2 mg	￥750	In-stock
5 mg	￥1100	In-stock
10 mg	￥1960	In-stock
50 mg	现货	询价
100 mg		询价
200 mg		询价

or 大包装询价

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Customer Review

Other Forms of Molibresib:

MCE 顾客使用本产品发表的 20 篇科研文献

: Molibresib purchased from MCE. Usage Cited in: Nat Med. 2017 Sep;23(9):1055-1062. [Abstract]; Western blot of WCL of C4-2 cells treated with vehicle (DMSO) or different doses of JQ1 or i-BET for 24 h. Actin is used as a loading control.

: Molibresib purchased from MCE. Usage Cited in: Oncotarget. 2016 Jun 21;7(25):38319-38332. [Abstract]; iBET762 partially disrupts the interaction between full-length ERG and BRD4 (A), and between T1-E4 ERG and BRD4 (B).

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Molibresib (I-BET762; GSK525762) is a BET bromodomain inhibitor with IC₅₀ of 32.5-42.5 nM.

IC₅₀ & Target

IC50: 32.5-42.5 nM (BET)^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
697	EC₅₀	1.17 μM Compound: 2; GSK525762A	Cytotoxicity against human 697 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay Cytotoxicity against human 697 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	[PMID: 29170024]
HepG2	EC₅₀	700 nM Compound: 3, I-BET762, GSK525762A	Induction of human ApoA1 gene expression in stably transfected human HepG2 cells coexpressing luciferase reporter gene after 18 hrs by luminescence assay Induction of human ApoA1 gene expression in stably transfected human HepG2 cells coexpressing luciferase reporter gene after 18 hrs by luminescence assay	[PMID: 22924434]
HepG2	EC₅₀	700 nM Compound: 2, GSK525762A	Induction of human ApoA1 gene expression in stably transfected human HepG2 cells coexpressing luciferase reporter gene after 18 hrs by luminescence assay Induction of human ApoA1 gene expression in stably transfected human HepG2 cells coexpressing luciferase reporter gene after 18 hrs by luminescence assay	[PMID: 21568322]
HL-60	IC₅₀	0.12 μM Compound: I-BET762	Cytotoxicity against human HL60 cells by MTS assay Cytotoxicity against human HL60 cells by MTS assay	[PMID: 29657099]
K562	IC₅₀	> 2000 nM Compound: 2, I-BET-762	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]
Kasumi 1	IC₅₀	0.21 μM Compound: 1; IBET762	Antiproliferative activity against human Kasumi-1 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human Kasumi-1 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30905542]
LOUCY	EC₅₀	> 5 μM Compound: 2; GSK525762A	Cytotoxicity against human Loucy cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay Cytotoxicity against human Loucy cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	[PMID: 29170024]
MM1.S	IC₅₀	0.23 μM Compound: 2; I-BET762	Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay	[PMID: 28586718]
MM1.S	IC₅₀	141 nM Compound: 1; I-BET762	Antiproliferative activity against human MM1S cells assessed as cell growth inhibition after 4 days by CCK8 assay Antiproliferative activity against human MM1S cells assessed as cell growth inhibition after 4 days by CCK8 assay	[PMID: 31461688]
MM1.S	IC₅₀	349.2 nM Compound: 2; I-BET762	Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay	[PMID: 29525435]
MOLM-13	IC₅₀	241 nM Compound: 2, I-BET-762	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	241 nM Compound: 4; I-BET762	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	0.8 μM Compound: 1; I-BET762	Cytotoxicity against human MV411 cells after 72 hrs by CellTiter-Glo assay Cytotoxicity against human MV411 cells after 72 hrs by CellTiter-Glo assay	[PMID: 30268702]
MV4-11	IC₅₀	1.23 μM Compound: I-BET-762	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 32631570]
MV4-11	IC₅₀	112 nM Compound: 1; I-BET762	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition after 4 days by CCK8 assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition after 4 days by CCK8 assay	[PMID: 31461688]
MV4-11	IC₅₀	93 nM Compound: 2, I-BET-762	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	93 nM Compound: 4; I-BET762	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]
NALM-6	EC₅₀	0.39 μM Compound: 2; GSK525762A	Cytotoxicity against human NALM6 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay Cytotoxicity against human NALM6 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	[PMID: 29170024]
Raji	IC₅₀	0.19 μM Compound: I-BET762	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]

体外研究
(In Vitro)

Molibresib (I-BET 762) shows the highest affinity interaction with BET. Molibresib binds to the tandem bromodomains of BET with high affinity (dissociation constant K_d of 50.5-61.3 nM). Molibresib displaces, with high efficacy (half-maximum inhibitory concentration IC₅₀ of 32.5-42.5 nM), a tetra-acetylated H4 peptide that had been pre-bound to tandem bromodomains of BET^[1]. Molibresib has high affinity for BD1/BD2 domain of BRD2/3/4 proteins. Molibresib treatment leads to a reduction in the recruitment of all three proteins to chromatin^[2]. Molibresib inhibits OPM-2 cell proliferation with IC₅₀ of 60.15 nM^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

The antimyeloma activity of Molibresib (I-BET 762) is tested dosed orally in an in vivo systemic xenograft model generated by injecting OPM-2 cells into NOD-SCID mice. Daily oral doses of Molibresib up to 10 mg/kg and 30 mg/kg given every other day are well tolerated with no clear impact on body weight compared with vehicle control. The plasma hLC concentration is significantly reduced in mice treated with Molibresib^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

423.90

Formula

C₂₂H₂₂ClN₅O₂

CAS 号

1260907-17-2

性状

固体

颜色

Off-white to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

细胞实验：

DMSO 中的溶解度 : 200 mg/mL (471.81 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

1M HCl 中的溶解度 : 100 mg/mL (235.90 mM; 超声助溶; 酸性条件溶解 (HCL 调节，pH≈1))

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3590 mL	11.7952 mL	23.5905 mL
5 mM	0.4718 mL	2.3590 mL	4.7181 mL
10 mM	0.2359 mL	1.1795 mL	2.3590 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.90 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (5.90 mM); 澄清溶液
方案三

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.90 mM); 澄清溶液
方案四

请依序添加每种溶剂： 1% DMSO 99% Saline
Solubility: ≥ 0.5 mg/mL (1.18 mM); 澄清溶液

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.94%

选择批次：

Data Sheet (630 KB) SDS (393 KB)

COA (291 KB) LCMS (95 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Nicodeme E, et al. Suppression of inflammation by a synthetic histone mimic. Nature. 2010 Dec 23;468(7327):1119-23. [Content Brief]

[2]. Asangani IA, et al. Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer. Nature. 2014 Jun 12;510(7504):278-82. [Content Brief]

[3]. 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]

Cell Assay ^[2]	VCaP, LNCaP, 22RV1, DU145 and PC3 prostate cancer cell lines are seeded in 96-well plates at 2000-10,000 cells/well (optimum density for growth) in a total volume of 100μL media containing 10% FBS. Serially diluted compounds in 100μL media are added to the cells 12hr later. Following 96 hr. incubation, cell viability is assessed by Cell-Titer GLO. The values are normalized and IC₅₀ is calculated using GraphPad Prism software. For long-term colony formation assay, 10,000-50,000 cells/well are seeded in six-well plates and treated with either 100 nM or 500 nM of JQ1 or DMSO. After 12 days cells are fixed with methanol, stained with crystal violet and photographed. For colorimetric assays, the stained wells are treated with 500μL 10% acetic acid and the absorbance is measured at 560nm using a spectrophotometer^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Mice^[3] The antimyeloma efficacy of orally administered Molibresib is tested in a systemic xenograft myeloma model. For this purpose, sublethally irradiated (200 cGy) NOD/SCID mice age 9 to 11 weeks are given 10⁷ OPM-2 myeloma cells via tail vein injection. On day 15 following inoculation, animals are started on oral treatment with Molibresib at escalating doses or vehicle (1% methylcellulose and 0.2% sodium lauryl sulfate), which is continued up to day 83. Specifically, 1 group of mice are treated with vehicle and 4 groups with different dosing schedules of Molibresib: 3 mg/kg per day; 10 mg/kg per day; 30 mg/kg on alternate days; and 30 to 20 mg/kg per day (ie, 30 mg/kg per day for 14 days, followed by 2 weeks [days 15 to 31] off treatment [drug is withheld due to a decline in body weight until animals has regained weight], follow by 20 mg/kg per day until termination of the experiment [days 43 to 82]). Blood samples (~70 μL) are removed at 0.5 hours after oral administration of Molibresib on day 15 (treatment initiation); days 27, 45, and 82 (3, 10, and 20 to 30 mg/kg once per day groups only); and day 83 (30 mg/kg once every other day group only). The blood is centrifuged to obtain 20 μL plasma and stored at -20°C prior to analysis for Molibresib by using a specific liquid chromatography/mass spectrometry/mass spectrometry assay. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Nicodeme E, et al. Suppression of inflammation by a synthetic histone mimic. Nature. 2010 Dec 23;468(7327):1119-23. [Content Brief] [2]. Asangani IA, et al. Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer. Nature. 2014 Jun 12;510(7504):278-82. [Content Brief] [3]. 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]

Molibresib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

1M HCl / DMSO	1 mM	2.3590 mL	11.7952 mL	23.5905 mL	58.9762 mL
	5 mM	0.4718 mL	2.3590 mL	4.7181 mL	11.7952 mL
	10 mM	0.2359 mL	1.1795 mL	2.3590 mL	5.8976 mL
	15 mM	0.1573 mL	0.7863 mL	1.5727 mL	3.9317 mL
	20 mM	0.1180 mL	0.5898 mL	1.1795 mL	2.9488 mL
	25 mM	0.0944 mL	0.4718 mL	0.9436 mL	2.3590 mL
	30 mM	0.0786 mL	0.3932 mL	0.7863 mL	1.9659 mL
	40 mM	0.0590 mL	0.2949 mL	0.5898 mL	1.4744 mL
	50 mM	0.0472 mL	0.2359 mL	0.4718 mL	1.1795 mL
	60 mM	0.0393 mL	0.1966 mL	0.3932 mL	0.9829 mL
	80 mM	0.0295 mL	0.1474 mL	0.2949 mL	0.7372 mL
	100 mM	0.0236 mL	0.1180 mL	0.2359 mL	0.5898 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Molibresib1260907-17-2I-BET762 GSK525762 GSK525762AGSK525762GSK 525762GSK-525762Epigenetic Reader DomainInhibitorinhibitorinhibit

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Molibresib (Synonyms: I-BET762; GSK525762; GSK525762A)

Customer Review

Other Forms of Molibresib:

MCE 顾客使用本产品发表的 20 篇科研文献

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参考文献

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完整储备液配制表

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Molibresib (Synonyms: I-BET762; GSK525762; GSK525762A)

Customer Review

Other Forms of Molibresib:

Molibresib 相关抗体

MCE 顾客使用本产品发表的 20 篇科研文献

Molibresib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

Molibresib 相关抗体:

摩尔计算器

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Molibresib 相关分类

完整储备液配制表

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