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A1874 99%+

货号:A1147982 Ambeed 开学季,买赠积分,赢豪礼

A1874 is a nutlin-based PROTAC targeting on BRD4, consist of a BRD4-ligand JQ1 linked to a MDM2 E3 ligase ligand RG7388.

A1874 化学结构 CAS号:2064292-12-0
A1874 化学结构
CAS号:2064292-12-0
A1874 3D分子结构
CAS号:2064292-12-0
A1874 化学结构 CAS号:2064292-12-0
A1874 3D分子结构 CAS号:2064292-12-0
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A1874 纯度/质量文件 产品仅供科研

货号:A1147982 标准纯度: 99%+
批次查询: 批次纯度:

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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

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 +

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 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 +++

BRD4BD2, IC50: 214 nM

BRD3BD2, 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。

A1874 生物活性

靶点
  • BET

描述 A1874 is a nutlin-based PROTAC targeting on BRD4, consist of a BRD4-ligand JQ1 linked to a MDM2 E3 ligase ligand RG7388. A1874 possesses dual function as it dose-dependently degraded its target BRD4, accompanied with the downregulation of c-MYC, as well as stabilization of P53 and upregulated P21 due to the efficient engagement of MDM2 by RG7388 in HCT116 cells exposure to A1874 at concentration ranging in 100nM-10μM post 24h. A1874 at concentration of 100nM achieved a near-maximum degradation of BRD4 by 98%. Incubation with A1874 ultimately resulted in a 97% loss in HCT116 cell viability, much more potent than JQ1 or RG7388 alone, for a synergistic antiproliferative effect by the combination of the E3 ligase ligand and targeting warhead. It seems that the potency to cell viability of A1874 may corelate to the status of P53 as A1874 was less potent against the cell line with mutant P53 or P53 depletion. A1875 is the inactive version of A1874[1].

A1874 参考文献

[1]Hines J, Lartigue S, et al. MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53. Cancer Res. 2019 Jan 1;79(1):251-262.

A1874 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

0.85mL

0.17mL

0.09mL

4.26mL

0.85mL

0.43mL

8.52mL

1.70mL

0.85mL

A1874 技术信息

CAS号2064292-12-0
分子式C58H62Cl3F2N9O7S
分子量 1173.59
别名
运输蓝冰
存储条件

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 145 mg/mL(123.55 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
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