Pelabresib | CPI-0610 | Epigenetic Reader Domain | AmBeed-信号通路专用抑制剂

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Pelabresib 98%

货号：A137689 同义名： CPI-0610

CPI-0610 is an inhibitor of BET bromodomains BRD2, BRD3, BRD4, and BRDT via binding to the acetylated lysine recognition motifs.

Pelabresib 化学结构
CAS号：1380087-89-7

Pelabresib 3D分子结构
CAS号：1380087-89-7

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Pelabresib 纯度/质量文件产品仅供科研

货号：A137689 标准纯度： 98% 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: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 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						99+%
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	+ BRD3, IC50: 0.25 μM BRD4, IC50: 0.5 μM						98%
Molibresib	+++ BET proteins, IC50: 35 nM						99%+
I-BRD9	+++ BRD9, pIC50: 7.3 BRD4, pIC50: 5.3						99%+
BI-7273	++++ BRD7, IC50: 117 nM BRD9, IC50: 19 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	++ 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	++++ 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	++++ 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	++++ BRD4-BD1, IC50: 119 nM BRD3-BD1, IC50: 9 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-BD1, IC50: 5 nM BRD4-BD2, IC50: 41 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			++ BRPF2, Kd: 500 nM BRPF1B, Kd: 100 nM				99%+
GSK-5959			++ BRPF3, pIC50: 7.1 BRPF2, pIC50: 5.2				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					++ 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					+ PCAF, IC50: 5 μM p300/CBP, IC50: 8.5 μM		99%+
SGC-CBP30					++++ EP300, IC50: 38 nM CREBBP, IC50: 21 nM		99%+
Nordihydroguaiaretic acid					✔	HER2,IGF-1R	99%+
Curcumin					+ p300, IC50: ~25 μM	Nrf2,Ferroptosis,NF-κB	98%
PF-CBP1 HCl					++ p300/CBP, IC50: 363nM CREBBP, IC50: 125nM		97%
CPI-637					+++ CBP, IC50: 0.03 μM EP300, IC50: 0.051 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。

Pelabresib 生物活性

靶点	BET BRD4-BD1, IC50:39 nM
描述	The Bromodomain and Extra-Terminal Domain (BET) family of proteins is characterized by the presence of two tandem bromodomains and an extra-terminal domain. It can play a crucial role in regulating gene transcription through epigenetic interactions between bromodomains and acetylated histones. CPI-0610 is a potent and selective benzoisoxazoloazepine BET bromodomain inhibitor with IC50 value of 39nM in a BRD4-BD1 TR-FRET assay. It effectively reduced the expression of downstream target MYC on RNA level in MV-4-11 cells with EC50 value of 180nM. Similarly, this downregulation of MYC could be also observed in vivo at dose of 15mg/kg, BID. Oral administration of CPI-0610 effectively inhibited MV-4-11 tumor growth in mouse xenograft at dose of 60mg/kg, QD or 30mg/kg, BID. Also, it synergized the tumor growth suppression of doxorubicin (2 mg/kg, IV, BIW) at dose of 10mg/kg, SC, BID. CPI-0610 treatment resulted in MM cytotoxicity at dose ranging in 200-1500nM post 72h in vitro by inducing G1 cell cycle arrest and caspase-dependent apoptosis. CPI-0610 significantly delayed tumor growth and increased the survival of MM-bearing SCID mice in a xenograft model at dose of 10mg/kg (dissolved in 0.5% (w/v) methylcellulose), SC, BID.
作用机制	CPI-0610 could bind in the acetyl-lysine recognition site and make direct hydrogen-bonding interactions with Asn140 of the target protein.^[1]

Pelabresib 动物研究

Dose

Mice^[1]: 30 mg/kg (p.o., s.c.); rat^[1]: 1 mg/kg (i.v.), 5 mg/kg (p.o.)

Administration

p.o., s.c., i.v.

Pharmacokinetics

Animal	Mice^[1]	Rats^[1]	Dogs^[1]
Dose	30 mg/kg	1 mg/kg (i.v.) 5 mg/kg (p.o.)	0.5 mg/kg (i.v.) 2.5 mg/kg (p.o.)
Administration	p.o. s.c.	i.v. p.o.	i.v. p.o.
AUC_0→inf	101 μM·h (p.o.) 49 μM·h (s.c.)		28 μM·h (p.o.)
F		76% (p.o.)	45% (p.o.)
T_1/2		0.93 h (i.v.)	9 h (i.v.)
T_max	0.42 h (p.o.) 1.3 h (s.c.)	1.2 h (p.o.)	1.3 h (p.o.)
AUC_0-inf		9.1 μM·h (p.o.)
CL		1.2 L/h/kg (i.v.)	0.11 L/h/kg (i.v.)
C_max	24 μM (p.o.) 8.4 μM (s.c.)	1.8 μM (p.o.)	2.9 μM (p.o.)
Vss		1.3 L/kg (i.v.)	1.2 L/kg (i.v.)

Pelabresib 参考文献

[1]Albrecht BK, Gehling VS, et al. Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials. J Med Chem. 2016 Feb 25;59(4):1330-9.

[2]Siu KT, Ramachandran J, et al. Preclinical activity of CPI-0610, a novel small-molecule bromodomain and extra-terminal protein inhibitor in the therapy of multiple myeloma. Leukemia. 2017 Aug;31(8):1760-1769.

Pelabresib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.73mL

0.55mL

0.27mL

13.67mL

2.73mL

1.37mL

27.34mL

5.47mL

2.73mL

Pelabresib 技术信息

CAS号	1380087-89-7
分子式	C₂₀H₁₆ClN₃O₂
分子量	365.813

别名	CPI-0610
运输	蓝冰

存储条件

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(287.03 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

动物实验配方

Pelabresib 98%

Pelabresib 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Pelabresib 质控信息

Pelabresib 生物活性

Pelabresib 动物研究

Pelabresib 参考文献

Pelabresib 实验方案

Pelabresib 技术信息

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Pelabresib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Pelabresib 质控信息

Pelabresib 生物活性

Pelabresib 动物研究

Pelabresib 参考文献

Pelabresib 实验方案

Pelabresib 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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