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ARV-825 {[allProObj[0].p_purity_real_show]}

货号:A370626

ARV-825是一种PROTAC,连接Cereblon和BRD4的配体,结合BRD4的BD1和BD2,Kd值分别为90 nM和28 nM。

ARV-825 化学结构 CAS号:1818885-28-7
ARV-825 化学结构
CAS号:1818885-28-7
ARV-825 3D分子结构
CAS号:1818885-28-7
ARV-825 化学结构 CAS号:1818885-28-7
ARV-825 3D分子结构 CAS号:1818885-28-7
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ARV-825 纯度/质量文件 产品仅供科研

货号:A370626 标准纯度: {[allProObj[0].p_purity_real_show]}
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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 +++

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 (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 +++

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 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 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 +++

BRD4BD2, IC50: 214 nM

BRD3BD2, IC50: 98 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 ++

PRC2, Kd: 114 nM

EED, Kd: 82 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 ++

BRPF1, IC50: 80 nM

BRPF2, IC50: 7.9 μM

99%+
OF-1 ++

BRPF1B, Kd: 100 nM

BRPF2, Kd: 500 nM

99%+
GSK-5959 ++

BRPF2, pIC50: 5.2

BRPF3, pIC50: 7.1

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

99%
I-CBP112 ++

p300, Kd: 167 nM

CBP, Kd: 151 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 HER2,IGF-1R 99%+
Curcumin +

p300, IC50: ~25 μM

Ferroptosis,Nrf2,NF-κB 98%
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。

ARV-825 生物活性

靶点
  • BET

    BRD4 BD1, Kd:90 nM

    BRD4 BD2, Kd:28 nM

描述 ARV-825 is a PROTAC targeting on BRD4, consisting of a BRD4-ligand JQ-1 linked to a cereblon E3 ligase ligand Pomalidomide, with Kds values of 90nM and 28nM for affinity to BD1 and BD2. ARV-825 led to a fast and efficient degradation of BRD4 at concentration ranging in 1-300nM in Namalwa and CA-46 cells and a dose-dependent degradation of BRD4 post 1-24h in Namalwa and Ramos cells exposure to 100nM ARV-825. Also, it led to a more significant c-MYC suppression than JQ1 or OTX015 by depletion of BRD4 by ARV-825 at different concentration (0.1, 0.3 and 1μM) or time point (2-24h), as well as a longer lasting effect after washout (6, 24h). Consistent with this downregulation of c-MYC, ARV-825 achieved a superior effect on suppression of BL cell proliferation and apoptosis induction compared with JQ1 or OTX015, including Namalwa, CA-46, Ramos and DAUDI cell lines[1].

ARV-825 细胞实验

Cell Line
Concentration Treated Time Description References
MDA-MB-231 0.4 µM 12, 24, or 48 hours ARV-825 significantly reduced the expression levels of BET proteins BRD4 and BRD2, although the reduction of BRD4 was milder in the resistant cells. J Exp Clin Cancer Res. 2019 Aug 30;38(1):383.
MDA-MB-231R 0.4 µM 12, 24, or 48 hours ARV-825 significantly reduced the expression levels of BET proteins BRD4 and BRD2, although the reduction of BRD4 was milder in the resistant cells. J Exp Clin Cancer Res. 2019 Aug 30;38(1):383.
MDA-MB-231 0.5 µM 24 hours ARV-825 inhibits mammosphere formation in MDA-MB-231 cells and reduces CD44+/CD24- and ALDH expressing subpopulations. Cell Commun Signal. 2023 Nov 3;21(1):315.
HCC1937 0.1 µM 24 hours ARV-825 inhibits mammosphere formation in HCC1937 cells and reduces ALDH expressing subpopulations. Cell Commun Signal. 2023 Nov 3;21(1):315.
SKO-007(J3) 0.2 µM 24 hours ARV-825 significantly downregulated IRF4 and cMYC expression and upregulated MICA expression. J Hematol Oncol. 2016 Dec 1;9(1):134.
LPS141 200 nM 24 hours To evaluate the anti-proliferative effect of ARV-825 on LPS141 cells, results showed that ARV-825 significantly inhibited cell proliferation. Nat Commun. 2019 Mar 22;10(1):1353.
MLS402 200 nM 24 hours To evaluate the anti-proliferative effect of ARV-825 on MLS402 cells, results showed that ARV-825 significantly inhibited cell proliferation. Nat Commun. 2019 Mar 22;10(1):1353.
SUP-T1 cells 20 nM 24 hours ARV-825 treatment resulted in downregulation of MYC and CD44 expression, along with decreased protein levels of NOTCH1, MYC, and CD44. Leukemia. 2022 May;36(5):1261-1273.
KOPT-K1 cells 50 nM 24 hours ARV-825 treatment led to significant downregulation of CD44 and CD44v8-10 mRNA and increased intracellular ROS levels. Leukemia. 2022 May;36(5):1261-1273.
SET2 cells 1.0 µM 24 hours To compare the effects of ARV-825 and OTX015 on the levels of BRD4 and BRD2 in sAML SET2 cells, the results showed that ARV-825 significantly reduced the levels of BRD4 and BRD2. Leukemia. 2017 Sep;31(9):1951-1961.
GL261 cells 0.0625 μg/ml 24 hours To evaluate the cytotoxicity of cRGD-P/ARV-DOX on GL261 cells, the results showed that cRGD-P/ARV-DOX had greater cytotoxicity to GL261 cells at 24 h and 48 h. Mater Today Bio. 2022 Sep 12;16:100423.
B16 cells 200 ng/mL 24 hours ARV-825 significantly reduced the viability of B16 cells, and MNC@Ca/MnCO3/ARV nanoparticles showed stronger cytotoxicity, significantly inducing ferroptosis in B16 cells. Mater Today Bio. 2025 Jan 24;31:101523.
DC2.4 cells 200 ng/mL 24 hours ARV-825 showed no significant toxicity to DC2.4 cells, indicating its safety for normal immune cells. Mater Today Bio. 2025 Jan 24;31:101523.
SKO-007(J3) 0.2 µM 48 hours ARV-825 significantly inhibited IRF4 and cMYC mRNA expression and upregulated MICA mRNA expression. J Hematol Oncol. 2016 Dec 1;9(1):134.
GL261 cells 100 ng/mL 48 hours To evaluate the effects of ARV-825 on cell proliferation, cell cycle, and apoptosis, results showed that ARV-825 significantly inhibited cell proliferation, induced apoptosis, and blocked the cell cycle. Adv Sci (Weinh). 2024 Dec;11(48):e2409753.
LN229 cells 100 ng/mL 48 hours To evaluate the effects of ARV-825 on cell proliferation, cell cycle, and apoptosis, results showed that ARV-825 significantly inhibited cell proliferation, induced apoptosis, and blocked the cell cycle. Adv Sci (Weinh). 2024 Dec;11(48):e2409753.
U251 cells 100 ng/mL 48 hours To evaluate the effects of ARV-825 on cell proliferation, cell cycle, and apoptosis, results showed that ARV-825 significantly inhibited cell proliferation, induced apoptosis, and blocked the cell cycle. Adv Sci (Weinh). 2024 Dec;11(48):e2409753.
U87 cells 100 ng/mL 48 hours To evaluate the effects of ARV-825 on cell proliferation, cell cycle, and apoptosis, results showed that ARV-825 significantly inhibited cell proliferation, induced apoptosis, and blocked the cell cycle. Adv Sci (Weinh). 2024 Dec;11(48):e2409753.
UKE1 cells 256 ± 12.45 nM 48 hours To compare the effects of ARV-825 and OTX015 on apoptosis in UKE1 cells, the results showed that ARV-825 induced significant apoptosis at a concentration of 256 ± 12.45 nM. Leukemia. 2017 Sep;31(9):1951-1961.
U251 cells 0.125 μg/ml 48 hours To evaluate the cytotoxicity of cRGD-P/ARV-DOX on U251 cells, the results showed that cRGD-P/ARV-DOX had better synergetic anti-cancer effects at 48 h. Mater Today Bio. 2022 Sep 12;16:100423.
BT549 0.2, 0.4, and 1 µM 48 or 96 hours ARV-825 exhibited significant antiproliferative activity in BT549 cells. J Exp Clin Cancer Res. 2019 Aug 30;38(1):383.
SKOV3 0.2, 0.4, and 1 µM 48 or 96 hours ARV-825 exhibited significant antiproliferative activity in SKOV3 cells. J Exp Clin Cancer Res. 2019 Aug 30;38(1):383.
OVCAR3 0.2, 0.4, and 1 µM 48 or 96 hours ARV-825 exhibited significant antiproliferative activity in OVCAR3 cells. J Exp Clin Cancer Res. 2019 Aug 30;38(1):383.
Jurkat 1 µM 7 days ARV-825 significantly inhibited the proliferation of Jurkat cells and suppressed cell growth by inducing cell cycle arrest and apoptosis. Cancer Cell Int. 2021 Apr 22;21(1):230.
CCRF-CEM 1 µM 7 days ARV-825 significantly inhibited the proliferation of CCRF-CEM cells and suppressed cell growth by inducing cell cycle arrest and apoptosis. Cancer Cell Int. 2021 Apr 22;21(1):230.
Molt4 1 µM 7 days ARV-825 significantly inhibited the proliferation of Molt4 cells and suppressed cell growth by inducing cell cycle arrest and apoptosis. Cancer Cell Int. 2021 Apr 22;21(1):230.
6 T-CEM 1 µM 7 days ARV-825 significantly inhibited the proliferation of 6 T-CEM cells and suppressed cell growth by inducing cell cycle arrest and apoptosis. Cancer Cell Int. 2021 Apr 22;21(1):230.

ARV-825 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice GL261 subcutaneous tumor model Intravenously injected 10 mg/kg Every two days for a total of four times To evaluate the antitumor efficacy of ARV-825 in vivo, results showed that ARV-825 significantly inhibited tumor growth and prolonged the survival of mice. Adv Sci (Weinh). 2024 Dec;11(48):e2409753.
Nude mice T-ALL xenograft model Intraperitoneal injection 10 mg/kg Once daily for 14 days ARV-825 significantly inhibited tumor growth in the T-ALL xenograft model and suppressed tumor proliferation by downregulating BRD4 and c-Myc protein expression. Cancer Cell Int. 2021 Apr 22;21(1):230.
C57BL/6 mice Melanoma model IntratumOral injection 100 μL Injected on days 7, 11, and 15, continued until day 22 MNC@Ca/MnCO3/ARV/anti-PD1 nanoparticles significantly inhibited melanoma growth and enhanced anti-tumor immune responses, successfully constructing an in situ tumor vaccine. Mater Today Bio. 2025 Jan 24;31:101523.
C57BL/6 mice Subcutaneous glioma model Intravenous injection 2.5 mg/kg Every three days for three consecutive times To evaluate the anti-tumor efficacy of cRGD-P/ARV-DOX in the subcutaneous glioma model, the results showed that cRGD-P/ARV-DOX significantly inhibited tumor growth. Mater Today Bio. 2022 Sep 12;16:100423.
Balb/c Nude mice TNBC tumor model Intravenous injection 3.5 mg/kg Every other day for a total of 5 times To evaluate the antitumor effect of ARV-MBs combined with ultrasound in the TNBC tumor model, the results showed that ARV-MBs combined with ultrasound significantly inhibited tumor growth, with a tumor inhibition rate of 81.4%. Biomater Res. 2024 Aug 13;28:0064
NSG mice LPS141 xenograft model Intraperitoneal injection 5 mg/kg Once daily, 5 days per week, continuous treatment To evaluate the anti-tumor effect of ARV-825 on the LPS141 xenograft model, results showed that ARV-825 significantly delayed tumor growth and prolonged mouse survival. Nat Commun. 2019 Mar 22;10(1):1353.
Mice T-ALL PDX model Intraperitoneal injection 5 mg/kg or 10 mg/kg Three times a week for several weeks ARV-825 treatment significantly reduced leukemia burden and prolonged the survival of mice. Leukemia. 2022 May;36(5):1261-1273.

ARV-825 动物研究

Dose Mice: 5 mg/kg[2] (i.p.), 10 mg/kg[3] (i.p.), 50 mg/kg[4] (i.p.)
Administration i.p.

ARV-825 参考文献

[1]Lu J, Qian Y, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63.

ARV-825 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.08mL

0.22mL

0.11mL

5.41mL

1.08mL

0.54mL

10.83mL

2.17mL

1.08mL

ARV-825 技术信息

CAS号1818885-28-7
分子式C46H47ClN8O9S
分子量 923.43
SMILES Code CC1=NN=C2N1C(SC(C)=C3C)=C3C(C4=CC=C(Cl)C=C4)=N[C@H]2CC(NC5=CC=C(OCCOCCOCCOCCNC6=C(C(N(C7CCC(NC7=O)=O)C8=O)=O)C8=CC=C6)C=C5)=O
MDL No. MFCD29472237
别名
运输蓝冰
InChI Key RWLOGRLTDKDANT-TYIYNAFKSA-N
Pubchem ID 92044400
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, 2-8°C

溶解方案

DMSO: 50 mg/mL(54.15 mM),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

请根据您的动物给药指南选择适当的溶解方案。
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
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