Mivebresib (Synonyms: 米维布塞; ABBV-075)

目录号: HY-100015 纯度: 99.29%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Mivebresib (ABBV-075) 是一种有效的，口服活性的溴结构域和末端结构域 (BET) 抑制剂。Mivebresib 与 BRD4 结合的 K_i 为 1.5 nM。

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Mivebresib Chemical Structure

CAS No. : 1445993-26-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1045	In-stock
2 mg	￥580	In-stock
5 mg	￥950	In-stock
10 mg	￥1550	In-stock
25 mg	￥3200	In-stock
50 mg	￥4800	In-stock
100 mg	现货	询价
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

MCE 顾客使用本产品发表的 11 篇科研文献

: Mivebresib purchased from MCE. Usage Cited in: Cell Death Dis. 2019 Jul 19;10(8):557. [Abstract]; BET inhibitors reduce IDO1 transcription.The protein levels of IDO1 are determined by RT-qPCR and western blotting, respectively.

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生物活性
纯度 & 产品资料
参考文献

生物活性

Mivebresib (ABBV-075) is a potent and orally active bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a K_i of 1.5 nM^[1].

IC₅₀ & Target

IC50: 1.5 nM (BRD4)^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BXPC-3	IC₅₀	1.22 μM Compound: ABBV-075; 10	Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36202064]
CT26	IC₅₀	48.26 μM Compound: 6; ABBV-075	Antiproliferative activity against human CT26 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against human CT26 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 33862375]
GES1	IC₅₀	4.31 nM Compound: ABBV-075	Cytotoxicity against human GES1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human GES1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 36599264]
HCT-116	IC₅₀	0.55 μM Compound: 8; ABBV-075	Antiproliferation activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferation activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33214826]
HepG2	IC₅₀	4.29 nM Compound: ABBV-075	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 36599264]
HL-60	IC₅₀	0.09 μM Compound: ABBV-075	Antiproliferative activity against BRD4-sensitive human HL60 cells after 72 hrs by CCK8 assay Antiproliferative activity against BRD4-sensitive human HL60 cells after 72 hrs by CCK8 assay	[PMID: 28314513]
HL-60	IC₅₀	0.12 μM Compound: 7; Abbv-075	Antiproliferative activity against human HL60 cells assessed as reduction in cell viability by MTT assay Antiproliferative activity against human HL60 cells assessed as reduction in cell viability by MTT assay	[PMID: 31857846]
HT-29	IC₅₀	1.84 nM Compound: ABBV-075	Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 36599264]
K562	IC₅₀	> 10 μM Compound: ABBV-075	Antiproliferative activity against BRD4-independent human K562 cells after 72 hrs by CCK8 assay Antiproliferative activity against BRD4-independent human K562 cells after 72 hrs by CCK8 assay	[PMID: 28314513]
Kasumi 1	IC₅₀	6.3 nM Compound: 9; ABBV-075	Antiproliferative activity against human Kasumi-1 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay Antiproliferative activity against human Kasumi-1 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay	[PMID: 32208600]
MCF7	IC₅₀	12.27 nM Compound: ABBV-075	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 36599264]
MM1.S	IC₅₀	6.5 nM Compound: 9; ABBV-075	Antiproliferative activity against human MM1S cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay Antiproliferative activity against human MM1S cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay	[PMID: 32208600]
MV4-11	IC₅₀	0.07 μM Compound: ABBV-075	Antiproliferative activity against BRD4-sensitive human MV411 cells after 72 hrs by CCK8 assay Antiproliferative activity against BRD4-sensitive human MV411 cells after 72 hrs by CCK8 assay	[PMID: 28314513]
MV4-11	IC₅₀	1.9 nM Compound: 9; ABBV-075	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay	[PMID: 32208600]
MX1	EC₅₀	13 nM Compound: 63; ABBV-075	Antiproliferative activity against human MX1 cells after 72 hrs by Cell Titer Glo assay Antiproliferative activity against human MX1 cells after 72 hrs by Cell Titer Glo assay	[PMID: 28949521]
MX1	EC₅₀	13 nM Compound: 5	Antiproliferative activity against human MX1 cells incubated for 72 hrs by cell-titer Glo assay Antiproliferative activity against human MX1 cells incubated for 72 hrs by cell-titer Glo assay	[PMID: 29678460]
RS4-11	IC₅₀	6.4 nM Compound: 9; ABBV-075	Antiproliferative activity against human RS4:11 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay Antiproliferative activity against human RS4:11 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay	[PMID: 32208600]
U-266	IC₅₀	2.03 μM Compound: 6; ABBV-075	Antiproliferative activity against human U-266 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against human U-266 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 33862375]

体外研究
(In Vitro)

Mivebresib inhibit DHT-stimulated transcription of AR target genes without significant effect on AR protein expression. In addition to blocking the transcription activation downstream of AR, Mivebresib is also a potent inhibitor of MYC and the TMPRSS2-ETS fusion proteins^[1].

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

Clinical Trial

分子量

459.47

Formula

C₂₂H₁₉F₂N₃O₄S

CAS 号

1445993-26-9

性状

固体

颜色

White to off-white

中文名称

米维布塞

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	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (217.64 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)

H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1764 mL	10.8821 mL	21.7642 mL
5 mM	0.4353 mL	2.1764 mL	4.3528 mL
10 mM	0.2176 mL	1.0882 mL	2.1764 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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

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 (5.44 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： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.44 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

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: 99.29%

选择批次：

Data Sheet (639 KB) SDS (393 KB)

COA (198 KB) LCMS (96 KB)

产品使用指南 (1538 KB)

参考文献

[1]. EJ Faivre et al. Abstract 4694: ABBV-075, a novel BET family inhibitor, disrupts critical transcription programs that drive prostate cancer growth to induce potent anti-tumor activity in vitro and in vivo

Mivebresib 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

DMSO	1 mM	2.1764 mL	10.8821 mL	21.7642 mL	54.4105 mL
	5 mM	0.4353 mL	2.1764 mL	4.3528 mL	10.8821 mL
	10 mM	0.2176 mL	1.0882 mL	2.1764 mL	5.4411 mL
	15 mM	0.1451 mL	0.7255 mL	1.4509 mL	3.6274 mL
	20 mM	0.1088 mL	0.5441 mL	1.0882 mL	2.7205 mL
	25 mM	0.0871 mL	0.4353 mL	0.8706 mL	2.1764 mL
	30 mM	0.0725 mL	0.3627 mL	0.7255 mL	1.8137 mL
	40 mM	0.0544 mL	0.2721 mL	0.5441 mL	1.3603 mL
	50 mM	0.0435 mL	0.2176 mL	0.4353 mL	1.0882 mL
	60 mM	0.0363 mL	0.1814 mL	0.3627 mL	0.9068 mL
	80 mM	0.0272 mL	0.1360 mL	0.2721 mL	0.6801 mL
	100 mM	0.0218 mL	0.1088 mL	0.2176 mL	0.5441 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:

Mivebresib1445993-26-9ABBV-075米维布塞ABBV075ABBV 075Epigenetic Reader DomainApoptosisInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Mivebresib (Synonyms: 米维布塞; ABBV-075)

Customer Review

MCE 顾客使用本产品发表的 11 篇科研文献