INCB-057643 | Epigenetic Reader Domain Inhibitor | AmBeed-信号通路专用抑制剂

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INCB-057643 99%+

货号：A861913

INCB057643 is an inhibitor of BET and it can reduce homologous recombination efficiency and augment PARP inhibitor activity in ovarian cancer.

INCB-057643 化学结构
CAS号：1820889-23-3

INCB-057643 3D分子结构
CAS号：1820889-23-3

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INCB-057643 纯度/质量文件产品仅供科研

货号：A861913 标准纯度： 99%+ 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 (1), Ki: <0.085 μM BRD4 (2), Ki: 0.34 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 (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	++++ 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	++ 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	++++ 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 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	98%
ODM-207	✔						99%
GSK778	+++ BRD4-BD1, IC50: 143 nM BRD2-BD1, IC50: 75nM						97%
SRX3207	+ BRD42, IC50: 3070 nM BRD41, 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, 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			++++ 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					++++ CREBBP, IC50: 21 nM EP300, IC50: 38 nM		99%+
Nordihydroguaiaretic acid					✔	HER2,IGF-1R	99%+
Curcumin					+ p300, IC50: ~25 μM	NF-κB,Ferroptosis,Nrf2	98%
PF-CBP1 HCl					++ CREBBP, IC50: 125nM p300/CBP, IC50: 363nM		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。

INCB-057643 生物活性

靶点

描述

INCB-057643 is a BET inhibitor with oral bioavailability in preclinical models of hematologic malignancies. It inhibited the binding of BRD2/BRD3/BRD4 to an acetylated histone H4 peptide in the low nanomole range with selectivity against other bromodomain containing proteins^[1]. INCB057643 exhibited anti-proliferation against androgen-dependent prostate cancer VCaP and LNCaP cells with GI50 values ≤100 nM, as well as androgen-independent DU145 and PC3 with GI50 values ≥500 nM, respectively. Also it inhibited the proliferation of 22Rv1 cells expressing androgen-independent AR splice variants with GI50 value ranging in 150-250 nM. Oral administration of INCB057643 at dose of 3mg/kg resulted significant inhibition of tumor growth (T/C%: 42 and 45%, respectively) without weight loss caused by toxicity^[2]. The proliferation of human AML, DLBCL, and multiple myeloma cell lines inhibited by INCB-057643 could be observed with a corresponding decrease in MYC protein levels, G1 arrest and a concentration-dependently increased apoptosis. Also, treatment with INCB057643 led to repression of the LPS-stimulated production of cytokines IL-6, IL-10 and MIP-1α in human and mouse whole blood^[1].

INCB-057643 动物研究

Dose	Mice: 3 mg/kg^[3] (p.o., BID)
Administration	p.o.

INCB-057643 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02959437	Solid Tumors ... 展开 >>Advanced Malignancies Metastatic Cancer 收起 <<	Phase 1 Phase 2	Active, not recruiting	October 2021	United States, California ... 展开 >> City of Hope National Medical Center Duarte, California, United States, 91010 University of California San Diego La Jolla, California, United States, 92093 United States, Illinois The University of Chicago Chicago, Illinois, United States, 60637 United States, Pennsylvania University of Pennsylvania Health System Philadelphia, Pennsylvania, United States, 19014 United States, Tennessee Sarah Cannon Nashville, Tennessee, United States, 37203 Vanderbilt-Ingram Cancer Center Nashville, Tennessee, United States, 37232 United States, Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 United States, Washington University of Washington Seattle, Washington, United States, 98109 Spain Vall D Hebron Univ Barcelona, Spain, 08035 Univ De Navarra Pamplona, Spain, 31008 United Kingdom University College London Hospitals (Uclh) London, United Kingdom, W1t7ha Churchill Hospital Oxford, United Kingdom, Ox37le 收起 <<
NCT02711137	Solid Tumors	Phase 1 Phase 2	Active, not recruiting	December 2018	United States, Alabama ... 展开 >> University of Alabama Birmingham, Alabama, United States, 35294-3300 United States, California University of California La Jolla, California, United States, 92093 United States, Colorado Sarah Cannon Research Institute at Health One Denver, Colorado, United States, 80218 United States, Connecticut Yale University New Haven, Connecticut, United States, 06510 United States, Florida Sylvester Comprehensive Cancer Center Miami, Florida, United States, 33136 Hematology - Oncology Associates of Treasure Coast Port Saint Lucie, Florida, United States, 34952 United States, Michigan University of Michigan Ann Arbor, Michigan, United States, 48109 United States, Minnesota University of Minnesota Minneapolis, Minnesota, United States, 55455 United States, Missouri Washington University Saint Louis, Missouri, United States, 63110 United States, New York University of Rochester, Wilmot Cancer Center Rochester, New York, United States, 14642 United States, North Carolina University of North Carolina at Chapel Hill Chapel Hill, North Carolina, United States, 27599 Wake Forest Baptist Health Winston-Salem, North Carolina, United States, 27157 United States, Texas Oncology Consultants, P.A. Houston, Texas, United States, 77030 The Methodist Hospital Houston, Texas, United States, 77030 United States, Utah Huntsman Cancer Institute Salt Lake City, Utah, United States, 84112 United States, Washington MultiCare Institute for Research and Innovation Tacoma, Washington, United States, 98405 Belgium Institut Jules Bordet, Clinical Trial Conduct Unit Brussels, Belgium, B-1000 France HÔPITAL SAINT-LOUIS, Service Hématologie Adultes Paris, France, 75010 收起 <<

INCB-057643 参考文献

[1]Matthew C. S, Thomas M, et al. Preclinical characterization of the potent and selective BET inhibitor INCB057643 in models of hematologic malignancies. Cancer Research. Volume 77, Issue 13 Supplement, pp. 5071.

[2]Ramiro V, Gianluca C, et al. BET inhibitors INCB054329 and INCB057643 display significant activity in androgen-independent prostate cancer models. Volume 77, Issue 13 Supplement, pp. 5080.

INCB-057643 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.03mL

2.41mL

1.20mL

24.07mL

4.81mL

2.41mL

INCB-057643 技术信息

CAS号	1820889-23-3
分子式	C₂₀H₂₁N₃O₅S
分子量	415.463

别名
运输	蓝冰

存储条件

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 60 mg/mL(144.42 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

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT02959437	Solid Tumors ... 展开 >>Advanced Malignancies Metastatic Cancer 收起 <<	Phase 1 Phase 2	Active, not recruiting	October 2021	United States, California ... 展开 >> City of Hope National Medical Center Duarte, California, United States, 91010 University of California San Diego La Jolla, California, United States, 92093 United States, Illinois The University of Chicago Chicago, Illinois, United States, 60637 United States, Pennsylvania University of Pennsylvania Health System Philadelphia, Pennsylvania, United States, 19014 United States, Tennessee Sarah Cannon Nashville, Tennessee, United States, 37203 Vanderbilt-Ingram Cancer Center Nashville, Tennessee, United States, 37232 United States, Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 United States, Washington University of Washington Seattle, Washington, United States, 98109 Spain Vall D Hebron Univ Barcelona, Spain, 08035 Univ De Navarra Pamplona, Spain, 31008 United Kingdom University College London Hospitals (Uclh) London, United Kingdom, W1t7ha Churchill Hospital Oxford, United Kingdom, Ox37le 收起 <<
NCT02711137	Solid Tumors	Phase 1 Phase 2	Active, not recruiting	December 2018	United States, Alabama ... 展开 >> University of Alabama Birmingham, Alabama, United States, 35294-3300 United States, California University of California La Jolla, California, United States, 92093 United States, Colorado Sarah Cannon Research Institute at Health One Denver, Colorado, United States, 80218 United States, Connecticut Yale University New Haven, Connecticut, United States, 06510 United States, Florida Sylvester Comprehensive Cancer Center Miami, Florida, United States, 33136 Hematology - Oncology Associates of Treasure Coast Port Saint Lucie, Florida, United States, 34952 United States, Michigan University of Michigan Ann Arbor, Michigan, United States, 48109 United States, Minnesota University of Minnesota Minneapolis, Minnesota, United States, 55455 United States, Missouri Washington University Saint Louis, Missouri, United States, 63110 United States, New York University of Rochester, Wilmot Cancer Center Rochester, New York, United States, 14642 United States, North Carolina University of North Carolina at Chapel Hill Chapel Hill, North Carolina, United States, 27599 Wake Forest Baptist Health Winston-Salem, North Carolina, United States, 27157 United States, Texas Oncology Consultants, P.A. Houston, Texas, United States, 77030 The Methodist Hospital Houston, Texas, United States, 77030 United States, Utah Huntsman Cancer Institute Salt Lake City, Utah, United States, 84112 United States, Washington MultiCare Institute for Research and Innovation Tacoma, Washington, United States, 98405 Belgium Institut Jules Bordet, Clinical Trial Conduct Unit Brussels, Belgium, B-1000 France HÔPITAL SAINT-LOUIS, Service Hématologie Adultes Paris, France, 75010 收起 <<

INCB-057643 99%+

INCB-057643 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

INCB-057643 质控信息

INCB-057643 生物活性

INCB-057643 动物研究

INCB-057643 临床研究

INCB-057643 参考文献

INCB-057643 实验方案

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INCB-057643 生物活性

INCB-057643 动物研究

INCB-057643 临床研究

INCB-057643 参考文献

INCB-057643 实验方案

INCB-057643 技术信息

最近浏览的产品

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摩尔计算器

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总药量计算器

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