Mivebresib | ABBV-075 | BET Inhibitor | AmBeed-信号通路专用抑制剂

首页 / / / 表观遗传阅读框 / Mivebresib/米维布塞

Mivebresib/米维布塞 {[allProObj[0].p_purity_real_show]}

货号：A414117 同义名： ABBV-075

Mivebresib是一种bromodomain和extra terminal domain（BET）抑制剂。BRD2、BRD4、BRDT的Ki值在1 nM - 2.2 nM之间。

Mivebresib/米维布塞化学结构
CAS号：1445993-26-9

Mivebresib/米维布塞 3D分子结构
CAS号：1445993-26-9

规格	价格	会员价	库存	数量
{[ item.pr_size ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]}	现货	1周咨询	- +

购物车0 收藏询单

sales@ambeed.cn tech@ambeed.cn 400-920-2911 产品手册产品订购技术咨询
快速发货顺丰冷链运输，1-2 天到达

品质保证

技术支持

免费溶解

Mivebresib/米维布塞纯度/质量文件产品仅供科研

货号：A414117 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Cell, 2025. Ambeed. [ A122167 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]; • Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]; 更多 >

表观遗传阅读框亚型比较

产品名称	BET ↓ ↑	bromodomain ↓ ↑	BRPF ↓ ↑	CBP/beta-catenin ↓ ↑	p300/CBP ↓ ↑	其他靶点	纯度
MS436	++ BRD4 (1), Ki: <0.085 μM BRD4 (2), Ki: 0.34 μM						99%+
CPI-203	+++ BRD4, IC50: 37 nM						98+%
GSK1324726A	+++ BRD2, IC50: 31 nM BRD4, IC50: 22 nM						99%+
PFI-1	++ BRD2, IC50: 98 nM BRD4, IC50: 0.22 μM						98%
Apabetalone	+ BD2, IC50: 0.51 μM						99%
(+)-JQ1	+++ BRD4 (2), IC50: 33 nM BRD4 (1), IC50: 77 nM						98%
I-BET151	+ BRD3, IC50: 0.25 μM BRD4, IC50: 0.5 μM						98%
Molibresib	+++ BET proteins, IC50: 35 nM						99%+
I-BRD9	+++ BRD4, pIC50: 5.3 BRD9, pIC50: 7.3						99%+
BI-7273	++++ BRD7, IC50: 117 nM BRD9, IC50: 19 nM						97%
Pelabresib	+++ BRD4-BD1, IC50: 39 nM						98%
ARV-825	+++ BRD4 BD2, Kd: 28 nM BRD4 BD1, Kd: 90 nM						99%+
Birabresib							99%+
BI 2536	+++ BRD4, Kd: 37 nM					c-Myc	99%+
Bromosporine	++ BRD2, IC50: 0.29 μM BRD9, IC50: 0.122 μM	++++ CECR2, IC50: 17 nM					99%+
XMD8-92	++ BRD4 (1), Kd: 170 nM						99%+
Mivebresib	✔						99%+
BI-9564	++++ BRD9, Kd: 5.9 nM BRD7, Kd: 73 nM	++ CECR2, Kd: 77 nM					98%
AZD5153 6-Hydroxy-2-naphthoic acid	++++ FL-BRD4, IC50: 5 nM						99%+
PLX51107	++++ BRD4 BD2, Kd: 1.7 nM BRD3 BD1, Kd: 2.1 nM						99%+
FL-411	+ BRD4(1), IC50: 0.43 μM						99%+
ABBV-744	✔						99%+
dBET6	++++ BRD4, IC50: 14 nM						99%+
dBET1	++++ BRD4, IC50: 20 nM						99%+
MZ1	++++ Brd2(BD2), Kd: 62 nM Brd3(BD2), Kd: 13 nM						99%+
dBET57	+ BRD4_BD1, DC50: 500 nM						99%+
SF2523	+ BRD4, IC50: 241 nM					DNA-PK	99%+
INCB054329	++++ BRD3-BD1, IC50: 9 nM BRD4-BD1, IC50: 119 nM						99%
INCB-057643	✔						99%+
(E/Z)-ZL0420	+++ BRD4 BD2, IC50: 32 nM BRD4 BD1, IC50: 27 nM						99%+
BMS-986158	✔						99%
BRD4 Inhibitor-10	++++ BRD4-BD2, IC50: 41 nM BRD4-BD1, IC50: 5 nM						97%
A1874	✔						99%+
Y06036	++ BRD4 (1), Kd: 82 nM						99%+
Alobresib	✔					NF-κB	95%
ODM-207	✔						98%
GSK778	+++ BRD2-BD1, IC50: 75nM BRD4-BD1, IC50: 143 nM						97%
SRX3207	+ BRD42, IC50: 3070 nM BRD41, IC50: 3070 nM					Syk	98%
GSK046	+++ BRD3_BD2, IC50: 98 nM BRD4_BD2, IC50: 214 nM						98%
GSK620	✔						97%
Trotabresib	✔						99%
NHWD-870	✔						98%
CFT8634	++++ BRD9, DC50: 3 nM						98%
GSK2801		++ BAZ2A, Kd: 257 nM BAZ2B, Kd: 136 nM					99%+
KG-501		✔					99%+
UNC 669		+ L3MBTL3, IC50: 35 μM L3MBTL4, IC50: 6 μM					99%
PFI-3		+++ SMARCA2A, Kd: 72 nM SMARCA4, Kd: 55 nM					99%+
UNC1215		+++ L3MBTL3, IC50: 120 nM L3MBTL3- D274A, IC50: 3.5 μM					99%+
EED226		++ EED, Kd: 82 nM PRC2, Kd: 114 nM					99%+
BRD9539		✔					98%
UNC926		+ L3MBTL1, Kd: 3.9 μM					99%
666-15		++ CREB, IC50: 81 nM					99%+
UNC6852		+ EED, IC50: 247 nM					98%
BAZ1A-IN-1		+ BAZ1A, Kd: 0.52 μM					99%+
PFI-4			++ BRPF2, IC50: 7.9 μM BRPF1, IC50: 80 nM				99%+
OF-1			++ BRPF1B, Kd: 100 nM BRPF2, Kd: 500 nM				99%+
GSK-5959			++ BRPF3, pIC50: 7.1 BRPF2, pIC50: 5.2				99%
GSK6853			++++ BRPF1, pIC50: 8.1				99%+
NI-42			++++ BRPF3, IC50: 260 nM BRPF1, IC50: 48 nM				99%+
E-7386				+++ CBP/beta-catenin, IC50: 0.0484 μM			99%
I-CBP112					++ CBP, Kd: 151 nM p300, Kd: 167 nM		98+%
Histone Acetyltransferase Inhibitor II					+ p300, IC50: 5 μM		98%
C646					+ p300/CBP, Ki: 400 nM		99%+
Anacardic Acid					+ p300/CBP, IC50: 8.5 μM PCAF, IC50: 5 μM		99%+
SGC-CBP30					++++ EP300, IC50: 38 nM CREBBP, IC50: 21 nM		99%+
Nordihydroguaiaretic acid					✔	IGF-1R,HER2	99%+
Curcumin					+ p300, IC50: ~25 μM	Ferroptosis,NF-κB,Nrf2	98%
CPI-637					+++ EP300, IC50: 0.051 μM CBP, IC50: 0.03 μM		99%+
Foscenvivint					✔	β-catenin	99%+
A-485					++ p300 HAT, IC50: 0.06 μM		99%+
GNE-781	+ BRD4(1), IC50: 5100 nM				++++ CBP, IC50: 0.94 nM		99%
NEO2734	+++ BET, IC50: <30 nM				+++ p300/CBP, IC50: <30 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Mivebresib/米维布塞生物活性

靶点

描述

Mivebresib is a potent and selective inhibitor of the bromodomain and extra terminal domain family of proteins. It binds to the bromodomains of BRD2/4/T with K_i values of 1-2.2nM. It also exhibits 10-fold weaker potency for BRD3 with a K_i value of 12.2nM. Mivebresib is highly selective for 18 bromodomain proteins with K_d values >1μM ( >600-fold selectivity versus BRD4). It displayed moderate activity towards CREBBP with a K_d value of 87μM (54-fold selectivity versus BRD4). Mivebresib showed robust single agent activity in cancer cell lines derived from lymphomas, leukemia, and solid tumors. It disrupted cell cycle control of cancer cells, inhibiting apoptosis and oncogenesis^[3]. Mivebresib inhibited DHT-stimulated transcription of androgen receptor (AR) target genes without affecting the protein expression of AR. It disrupted DHT-stimulated recruitment of BRD4 to gene regulatory regions co-occupied by AR. Mivebresib also inhibited MYC and TMPRSS2-ETS fusion proteins with high potency^[4]. In flank xenograft mouse models, mivebresib exhibited potent anti-tumor activity comparable or superior to standard-of-care agents^[3].

Mivebresib/米维布塞细胞实验

Cell Line Ty-82 cells SKOV3 cells SCLC cell lines	Concentration	Treated Time	Description	References
Ty-82 cells	1 µM	12 or 24 hours	To investigate the effect of Mivebresib on IDO1 mRNA expression, results showed that Mivebresib significantly reduced IDO1 mRNA expression.	Cell Death Dis. 2019 Jul 19;10(8):557.
SKOV3 cells	1 µM	24 hours	To investigate the effect of Mivebresib on IDO1 protein expression, results showed that Mivebresib significantly reduced IDO1 protein expression.	Cell Death Dis. 2019 Jul 19;10(8):557.
SCLC cell lines	30 nM to >10 µM (IC50)	3 days	To evaluate the antiproliferative effects of Mivebresib on different SCLC cell lines, the results showed IC50 values ranging from 30 nmol/L to >10 µmol/L, indicating cell line-specific sensitivity to BET inhibition.	Mol Cancer Res. 2024 Aug 2;22(8):689-698.

Mivebresib/米维布塞动物实验

Species Balb/c Nude mice NSG mice Mice	Animal Model Human Ty-82 xenograft model MOLM13/GFP-Luc cell xenograft model Subcutaneous xenograft model	Administration	Dosage	Frequency	Description	References
Balb/c Nude mice	Human Ty-82 xenograft model	Oral	0.5 mg/kg	Once daily for 21 days	To investigate the effect of Mivebresib on tumor growth and IDO1 expression, results showed that Mivebresib significantly inhibited tumor growth and reduced IDO1 expression.	Cell Death Dis. 2019 Jul 19;10(8):557.
NSG mice	MOLM13/GFP-Luc cell xenograft model	Oral	1 mg/kg	Once daily for 2 weeks	To evaluate the anti-leukemia activity of ABBV-075 and/or ABT-199 against AML xenograft models, results showed that combination treatment significantly reduced AML xenograft growth and improved survival of mice.	Blood Cancer J. 2019 Jan 15;9(2):4.
Mice	Subcutaneous xenograft model	Intraperitoneal injection	100 mg/kg	Once daily for 5 days, followed by 2 days off, repeated	To evaluate the effect of Mivebresib on neuroblastoma xenograft models	Mol Cancer. 2023 May 29;22(1):88

Mivebresib/米维布塞参考文献

[1]Bui MH, Lin X, et al. Preclinical characterization of BET family bromodomain inhibitor ABBV-075 suggests combination therapeutic strategies. Cancer Res. 2017 Apr 17. pii: canres.1793.2016.

[2]Lin X, Huang X, et al. HEXIM1 as a Robust Pharmacodynamic Marker for Monitoring Target Engagement of BET Family Bromodomain Inhibitors in Tumors and Surrogate Tissues. Mol Cancer Ther. 2017 Feb;16(2):388-396.

[3]Abstract 4718: ABBV-075, a novel BET family bromodomain inhibitor, represents a promising therapeutic agent for a broad spectrum of cancer indications

[4]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/米维布塞实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.18mL

0.44mL

0.22mL

10.88mL

2.18mL

1.09mL

21.76mL

4.35mL

2.18mL

Mivebresib/米维布塞技术信息

CAS号	1445993-26-9
分子式	C₂₂H₁₉F₂N₃O₄S
分子量	459.47
SMILES Code	CCS(=O)(NC1=CC=C(OC2=CC=C(F)C=C2F)C(C3=CN(C)C(C4=C3C=CN4)=O)=C1)=O
MDL No.	MFCD30377200

别名	ABBV-075
运输	蓝冰
InChI Key	RDONXGFGWSSFMY-UHFFFAOYSA-N
Pubchem ID	71600087

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

细胞实验：

DMSO: 105 mg/mL(228.53 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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

方案二

Mivebresib/米维布塞 {[allProObj[0].p_purity_real_show]}

Mivebresib/米维布塞纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Mivebresib/米维布塞质控信息

Mivebresib/米维布塞生物活性

Mivebresib/米维布塞细胞实验

Mivebresib/米维布塞动物实验

Mivebresib/米维布塞参考文献

Mivebresib/米维布塞实验方案

Mivebresib/米维布塞技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

Mivebresib/米维布塞 {[allProObj[0].p_purity_real_show]}

Mivebresib/米维布塞 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Mivebresib/米维布塞 质控信息

Mivebresib/米维布塞 生物活性

Mivebresib/米维布塞 细胞实验

Mivebresib/米维布塞 动物实验

Mivebresib/米维布塞 参考文献

Mivebresib/米维布塞 实验方案

Mivebresib/米维布塞 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

请登录您的专属账户

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

Mivebresib/米维布塞纯度/质量文件产品仅供科研

Mivebresib/米维布塞质控信息

Mivebresib/米维布塞生物活性

Mivebresib/米维布塞细胞实验

Mivebresib/米维布塞动物实验

Mivebresib/米维布塞参考文献

Mivebresib/米维布塞实验方案

Mivebresib/米维布塞技术信息