Birabresib | MK-8628 | BRD2/3/4 Inhibitor | AmBeed-信号通路专用抑制剂

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Birabresib {[allProObj[0].p_purity_real_show]}

货号：A146187 同义名： MK-8628;OTX-015

Birabresib (OTX-015) 是一种强效的溴结构域 (BRD2/3/4) 抑制剂，IC50 值范围在 92 至 112 nM 之间。

Birabresib 化学结构
CAS号：202590-98-5

Birabresib 3D分子结构
CAS号：202590-98-5

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Birabresib 纯度/质量文件产品仅供科研

货号：A146187 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: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 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 (2), Ki: 0.34 μM BRD4 (1), Ki: <0.085 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 (1), IC50: 77 nM BRD4 (2), IC50: 33 nM						98%
I-BET151	+ BRD4, IC50: 0.5 μM BRD3, IC50: 0.25 μM						98%
Molibresib	+++ BET proteins, IC50: 35 nM						99%+
I-BRD9	+++ BRD4, pIC50: 5.3 BRD9, pIC50: 7.3						99%+
BI-7273	++++ BRD9, IC50: 19 nM BRD7, IC50: 117 nM						99+%
Pelabresib	+++ BRD4-BD1, IC50: 39 nM						98%
ARV-825	+++ BRD4 BD1, Kd: 90 nM BRD4 BD2, Kd: 28 nM						99%+
Birabresib							99%+
BI 2536	+++ BRD4, Kd: 37 nM					c-Myc	99%+
Bromosporine	++ BRD9, IC50: 0.122 μM BRD2, IC50: 0.29 μM	++++ CECR2, IC50: 17 nM					99%+
XMD8-92	++ BRD4 (1), Kd: 170 nM						99%+
Mivebresib	✔						99%+
BI-9564	++++ BRD7, Kd: 73 nM BRD9, Kd: 5.9 nM	++ CECR2, Kd: 77 nM					98%
AZD5153 6-Hydroxy-2-naphthoic acid	++++ FL-BRD4, IC50: 5 nM						99%+
PLX51107	++++ BRD3 BD1, Kd: 2.1 nM BRD4 BD2, Kd: 1.7 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	++++ Brd3(BD2), Kd: 13 nM Brd2(BD2), Kd: 62 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 BD1, IC50: 27 nM BRD4 BD2, IC50: 32 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	98%
ODM-207	✔						99%
GSK778	+++ BRD2-BD1, IC50: 75nM BRD4-BD1, IC50: 143 nM						97%
SRX3207	+ BRD41, IC50: 3070 nM BRD42, IC50: 3070 nM					Syk	98%
GSK046	+++ BRD4_BD2, IC50: 214 nM BRD3_BD2, IC50: 98 nM						98%
GSK620	✔						97%
Thalidomide-NH-C4-NH-Boc	✔						98%
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		+ L3MBTL4, IC50: 6 μM L3MBTL3, IC50: 35 μM					98%
PFI-3		+++ SMARCA2A, Kd: 72 nM SMARCA4, Kd: 55 nM					99%+
UNC1215		+++ L3MBTL3- D274A, IC50: 3.5 μM L3MBTL3, IC50: 120 nM					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			++ BRPF2, pIC50: 5.2 BRPF3, pIC50: 7.1				99%
GSK6853			++++ BRPF1, pIC50: 8.1				99%+
NI-42			++++ BRPF1, IC50: 48 nM BRPF3, IC50: 260 nM				99%+
E-7386				+++ CBP/beta-catenin, IC50: 0.0484 μM			97%
I-CBP112					++ p300, Kd: 167 nM CBP, Kd: 151 nM		98+%
Histone Acetyltransferase Inhibitor II					+ p300, IC50: 5 μM		98%
C646					+ p300/CBP, Ki: 400 nM		99%+
Anacardic Acid					+ PCAF, IC50: 5 μM p300/CBP, IC50: 8.5 μM		99%+
SGC-CBP30					++++ EP300, IC50: 38 nM CREBBP, IC50: 21 nM		99%+
Nordihydroguaiaretic acid					✔	IGF-1R,HER2	99%+
Curcumin					+ p300, IC50: ~25 μM	Nrf2,NF-κB,Ferroptosis	98%
PF-CBP1 HCl					++ CREBBP, IC50: 125nM p300/CBP, IC50: 363nM		97%
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		98%
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。

Birabresib 生物活性

靶点	BET BRDs, EC50:10-19 nM
描述	The Bromodomain and extra-terminal domain BET (bromodomain and extra-terminal domain) family is characterized by the presence of two tandem bromodomains and an extra-terminal domain. BET proteins can govern the assembly of histone acetylation-dependent chromatin complexes, thus regulating gene expression. OTX015 (MK-8628) was the first in class inhibitor to enter clinical trials in hematologic diseases with IC50 value from 92 to 112nM for BRD2, BRD3, and BRD4, respectivelyDevelopment of the BET bromodomain inhibitor OTX015 http://mct.aacrjournals.org/content/12/11_Supplement/C244.short. After treatment with OTX015, a series of gene reported to be frequently affected by BET inhibition has been quantified in U87MG cells. Transient increases can be seen after 4h exposure to 500nM OTX015 for both C-MYC and CDKN1A but returned to basal levels after 24h. SESN3, HEXIM-1, HIST2H2BE, and HIST1H2BK gene all increased significantly after 4 and 24h exposure to OTX015, while MTHFD1L levels were significantly decreased after 24h exposure. A distinct pattern was seen for HIST2H4A and HIST1H2BJ with the significant increase was seen after 4h reversed to a significant decrease after 24h^[1]. OTX015 can inhibit the growth of a variety of human cancer cell lines and had GI50 values ranged from 60 to 200nM for most hematologic malignancies tested. Oral administration of OTX015 showed 79% TGI at 100mg/kg, qd, and 61% TGI at 10mg/kg, bid, in Ty82 BRD-NUT midline carcinoma tumor miceDevelopment of the BET bromodomain inhibitor OTX015 http://mct.aacrjournals.org/content/12/11_Supplement/C244.short. OTX015 also showed anti-proliferative activity in a large panel of cell lines derived from mature B-cell lymphoid tumors with median IC50 of 240nM, without significant differences among the different histotypes. OTX015 presented in-vitro synergism with several anti-cancer agents, especially with mTOR and BTK inhibitors^[2].
作用机制	OTX015 may have competitive inhibition on BRD2, BRD3, and BRD4Development of the BET bromodomain inhibitor OTX015 http://mct.aacrjournals.org/content/12/11_Supplement/C244.short.

Birabresib 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
Rosetta2 DE3 cells		Function assay	30 mins	Displacement of FAM-labeled ZBA248 from BRD3 BD2 (306 to 417 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki=4 nM	26080064

Birabresib 动物研究

Dose

Mice^[1]: 20 mg/kg - 25 mg/kg (i.p.), 100 mg/kg (p.o.)

Administration

i.p., p.o.

Pharmacokinetics

Animal	Mice^[3]
Dose	50 mg/kg
Administration	i.h.
C_max	~ 750 ng/ml (4 h)

Birabresib 参考文献

[1]Berenguer-Daizé C, Astorgues-Xerri L, et al. OTX015 (MK-8628), a novel BET inhibitor, displays in vitro and in vivo antitumor effects alone and in combination with conventional therapies in glioblastoma models. Int J Cancer. 2016 Nov 1;139(9):2047-55.

[2]Boi M, Gaudio E, et al. The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs. Clin Cancer Res. 2015 Apr 1;21(7):1628-38.

[3]Gaudio E, Tarantelli C, et al. Bromodomain inhibitor OTX015 (MK-8628) combined with targeted agents shows strong in vivo antitumor activity in lymphoma. Oncotarget. 2016 Sep 6;7(36):58142-58147.

Birabresib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.16mL

2.03mL

1.02mL

20.33mL

4.07mL

2.03mL

Birabresib 技术信息

CAS号	202590-98-5
分子式	C₂₅H₂₂ClN₅O₂S
分子量	491.993

别名	MK-8628;OTX-015;(−)-OTX015;HY-15743
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 50 mg/mL(101.63 mM)，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

动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 8 mg/mL clear

PO 0.5% CMC-Na 40 mg/mL suspension

Birabresib {[allProObj[0].p_purity_real_show]}

Birabresib 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Birabresib 质控信息

Birabresib 生物活性

Birabresib 细胞研究

Birabresib 动物研究

Birabresib 参考文献

Birabresib 实验方案

Birabresib 技术信息

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Birabresib {[allProObj[0].p_purity_real_show]}

Birabresib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Birabresib 质控信息

Birabresib 生物活性

Birabresib 细胞研究

Birabresib 动物研究

Birabresib 参考文献

Birabresib 实验方案

Birabresib 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

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Birabresib 纯度/质量文件产品仅供科研