ABBV-744 | BD2 Inhibitor | AmBeed-信号通路专用抑制剂

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	- +

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。

靶点	BET
描述	ABBV-744 is a selective BDII inhibitor with improved oral bioavailability. ABBV-744 exhibited antiproliferation to AML and androgen receptor (AR) positive prostate cancer cell line models, including models of Enzalutamide resistance. Consistent with this, ABBV-744 induced tumor growth inhibition in AML and prostate cancer xenograft models^[1]. Up to now, a phase1 study of ABBV-744 to acute myeloid leukaemia and prostate cancer is undergoing^[2].
作用机制	ABBV-744 preferentially binds to BD2 of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histones.^[3]

Cell Line Primary human bronchial epithelial cells Calu-3 cells OCI-AML2 HGC-27 cells AGS cells orbital fibroblasts (OFs)	Concentration	Treated Time	Description	References
Primary human bronchial epithelial cells	0.01–10 μM	72 h	Reduced ACE2 mRNA levels	Nat Cell Biol. 2022 Jan;24(1):24-34.
Calu-3 cells	10 μM	72 h	Reduced ACE2 mRNA levels	Nat Cell Biol. 2022 Jan;24(1):24-34.
OCI-AML2	100 nM	2 weeks	Identified SPOP as a key gene for BETi resistance	Proc Natl Acad Sci U S A. 2023 Apr 18;120(16):e2220134120.
HGC-27 cells	4.8 μM, 2.3 μM	48h, 72h	To evaluate the inhibitory effect of ABBV-744 on the proliferation of HGC-27 cells, the results showed that ABBV-744 significantly inhibited cell survival in a dose- and time-dependent manner.	Neoplasia. 2023 Nov;45:100936.
AGS cells	7.4 μM, 3.5 μM	48h, 72h	To evaluate the inhibitory effect of ABBV-744 on the proliferation of AGS cells, the results showed that ABBV-744 significantly inhibited cell survival in a dose- and time-dependent manner.	Neoplasia. 2023 Nov;45:100936.
orbital fibroblasts (OFs)	10, 100, 500 nM	24 h	To evaluate the effect of ABBV744 on TGF-β1-induced fibrosis marker expression, results showed ABBV744 significantly reduced mRNA and protein expression of α-SMA, COL1A1, and COL1A2	Invest Ophthalmol Vis Sci. 2023 Jun 1;64(7):9.

Species NSG mice Golden Syrian hamsters Nude mice Nude mice	Animal Model KMT2A-r leukemia xenograft model SARS-CoV-2 infection model BLCA subcutaneous transplantation model Subcutaneous tumor model	Administration	Dosage	Frequency	Description	References
NSG mice	KMT2A-r leukemia xenograft model	Oral administration	4.7 mg/kg	Daily administration for 3-4 weeks	Validated SPOP deficiency causes BETi resistance in vivo	Proc Natl Acad Sci U S A. 2023 Apr 18;120(16):e2220134120.
Golden Syrian hamsters	SARS-CoV-2 infection model	Oral gavage	20 mg/kg	Daily for 3 days	Reduced SARS-CoV-2 infection	Nat Cell Biol. 2022 Jan;24(1):24-34.
Nude mice	BLCA subcutaneous transplantation model	Intragastric administration	10 mg/kg	Daily for about 3 weeks	Combination of ABBV-744 with DDP significantly inhibited tumor growth and increased sensitivity to chemotherapy	J Exp Clin Cancer Res. 2024 Nov 18;43(1):303
Nude mice	Subcutaneous tumor model	Oral	14 mg/kg	21 days	To evaluate the inhibitory effect of ABBV-744 on gastric cancer cell growth in vivo, the results showed that ABBV-744 significantly suppressed tumor growth, and the effect was enhanced when combined with CQ.	Neoplasia. 2023 Nov;45:100936.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03360006	Prostate Cancer ... 展开 >> Acute Myeloid Leukemia (AML) 收起 <<	Phase 1	Recruiting	April 13, 2020	United States, California ... 展开 >> UC Irvine /ID# 160789 Recruiting Orange, California, United States, 92868 UC Davis Comp Cancer Ctr /ID# 202729 Recruiting Sacramento, California, United States, 95817 United States, Illinois Northwestern /ID# 171098 Recruiting Chicago, Illinois, United States, 60611 University of Chicago /ID# 160702 Recruiting Chicago, Illinois, United States, 60637-1443 United States, Ohio Cleveland Clinic Foundation /ID# 160756 Recruiting Cleveland, Ohio, United States, 44195 United States, Texas Univ TX, MD Anderson /ID# 160701 Recruiting Houston, Texas, United States, 77030 United States, Washington Swedish-Center for Blood Disor /ID# 166487 Recruiting Seattle, Washington, United States, 98104 收起 <<

CAS号	2138861-99-9
分子式	C₂₈H₃₀FN₃O₄
分子量	491.55
SMILES Code	O=C(C(N1)=CC(C(C2=CC(C(C)(O)C)=CC=C2OC3=C(C)C=C(F)C=C3C)=CN4C)=C1C4=O)NCC
MDL No.	MFCD31657409

ABBV-744 {[allProObj[0].p_purity_real_show]}

ABBV-744 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

ABBV-744 质控信息

ABBV-744 生物活性

ABBV-744 细胞实验

ABBV-744 动物实验

ABBV-744 临床研究

ABBV-744 参考文献

ABBV-744 实验方案

ABBV-744 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

别名
运输	蓝冰
InChI Key	OEDSFMUSNZDJFD-UHFFFAOYSA-N
Pubchem ID	132010322

ABBV-744 {[allProObj[0].p_purity_real_show]}

ABBV-744 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

ABBV-744 质控信息

ABBV-744 生物活性

ABBV-744 细胞实验

ABBV-744 动物实验

ABBV-744 临床研究

ABBV-744 参考文献

ABBV-744 实验方案

ABBV-744 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

ABBV-744 纯度/质量文件产品仅供科研