货号:A129684
同义名:
AZD5153 HNT salt
AZD5153 is an inhibitor of BET/BRD4 bromodomain, the IC50 for BRD4 is 1.7 nM.
There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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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 |
+++
BRD4, IC50: 22 nM BRD2, IC50: 31 nM |
99%+ | |||||||||||||||||
PFI-1 |
++
BRD4, IC50: 0.22 μM BRD2, IC50: 98 nM |
98% | |||||||||||||||||
Apabetalone |
+
BD2, IC50: 0.51 μM |
99% | |||||||||||||||||
(+)-JQ1 |
+++
BRD4 (2), IC50: 33 nM BRD4 (1), IC50: 77 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 |
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 |
++
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 |
++++
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 |
+
BRD4BD1, 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 | 95% | ||||||||||||||||
ODM-207 | ✔ | 98% | |||||||||||||||||
GSK778 |
+++
BRD4-BD1, IC50: 143 nM BRD2-BD1, IC50: 75nM |
97% | |||||||||||||||||
SRX3207 |
+
BRD42, IC50: 3070 nM BRD41, IC50: 3070 nM |
Syk | 98% | ||||||||||||||||
GSK046 |
+++
BRD3BD2, IC50: 98 nM BRD4BD2, IC50: 214 nM |
98% | |||||||||||||||||
GSK620 | ✔ | 97% | |||||||||||||||||
Thalidomide-NH-C4-NH-Boc | ✔ | 98% | |||||||||||||||||
Trotabresib | ✔ | 99% | |||||||||||||||||
NHWD-870 | ✔ | 98% | |||||||||||||||||
CFT8634 |
++++
BRD9, DC50: 3 nM |
99% | |||||||||||||||||
GSK2801 |
++
BAZ2B, Kd: 136 nM BAZ2A, Kd: 257 nM |
99%+ | |||||||||||||||||
KG-501 | ✔ | 99%+ | |||||||||||||||||
UNC 669 |
+
L3MBTL3, IC50: 35 μM L3MBTL4, IC50: 6 μM |
99% | |||||||||||||||||
PFI-3 |
+++
SMARCA4, Kd: 55 nM SMARCA2A, Kd: 72 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 |
++
BRPF2, Kd: 500 nM BRPF1B, Kd: 100 nM |
99%+ | |||||||||||||||||
GSK-5959 |
++
BRPF2, pIC50: 5.2 BRPF3, pIC50: 7.1 |
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 |
++++
CREBBP, IC50: 21 nM EP300, IC50: 38 nM |
99%+ | |||||||||||||||||
Nordihydroguaiaretic acid | ✔ | IGF-1R,HER2 | 99%+ | ||||||||||||||||
Curcumin |
+
p300, IC50: ~25 μM |
Ferroptosis,NF-κB,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 |
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 |
|
描述 | AZD5153 shows a significant increase in efficacy for displacing the entire BRD4 compared to BD1, with IC50 values of 5.0 nM for full-length BRD4 and 1.6 μM for BD1. In U2OS cells, AZD5153 effectively disrupts BRD4 foci, reflected by an IC50 of 1.7 nM. Additionally, AZD5153 consistently lowers MYC protein expression in various cell lines, regardless of their response to AZD5153 treatment[1]. |
Animal study | The use of AZD5153 results in either the cessation or reduction of tumor growth in various xenograft models, including those for acute myeloid leukemia, multiple myeloma, and diffuse large B-cell lymphoma. The treatment with AZD5153 significantly alters the transcriptional activities related to MYC, E2F, and mTOR pathways[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.50mL 0.30mL 0.15mL |
7.49mL 1.50mL 0.75mL |
14.98mL 3.00mL 1.50mL |
CAS号 | 1869912-40-2 |
分子式 | C36H41N7O6 |
分子量 | 667.754 |
别名 | AZD5153 HNT salt |
运输 | 蓝冰 |
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 |
DMSO: 105 mg/mL(157.24 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 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
|
动物实验配方 |