ARV-771 | PROTAC BET Degrader | AmBeed-信号通路专用抑制剂

ARV-771 {[allProObj[0].p_purity_real_show]}

货号：A365449

ARV-771是一种高效、选择性、口服生物利用度良好的雄激素受体（AR）降解PROTAC。它通过与雄激素受体结合，促进其降解，抑制与AR相关的肿瘤生长。ARV-771在治疗包括转移性去势抵抗前列腺癌在内的多种前列腺癌中展示了显著的研究潜力。

ARV-771 化学结构
CAS号：1949837-12-0

ARV-771 3D分子结构
CAS号：1949837-12-0

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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						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	+++ BRD9, pIC50: 7.3 BRD4, pIC50: 5.3						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	++ 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	++++ BRD7, Kd: 73 nM BRD9, Kd: 5.9 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	+ BRD4_BD1, 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	+ BRD41, IC50: 3070 nM BRD42, 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		++ 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		+++ 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			++ BRPF1, IC50: 80 nM BRPF2, IC50: 7.9 μM				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					✔	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-771 生物活性

描述

ARV-771 is a PROTAC targeting on pan-BET, containing a BRD4-binding moiety (JQ-1) and a VHL-binding moiety. Treatment with ARV-771 led to an efficient degradation of BRD2, 3 and 4 in CRPC cell lines (22Rv1, VCaP, and LnCaP95 cell lines) at concentration of 4, 11 and 34nM post 16h, and achieved a superior suppression of c-MYC on mRNA level at concentration of 10nM post 16h compared with BET small molecular inhibitor JQ-1 and OTX-015. Consistent with this effect on c-MYC by ARV-771, ARV-771 caused higher levels of CRPC cell growth inhibition and cell apoptosis compared with the treatment with JQ-1, OTX-015 and enzalutamide. Unlike BET inhibitors, the attenuation of AR signaling and AR levels could also be observed after ARV-771 treatment. Administration of ARV-771, s.c., once daily demonstrated efficiency in multiple tumor xenograft models of CRPC at various doses ranging in 3-30mg/kg. ARV-766 works as a negative control of ARV-771^[1].

ARV-771 细胞实验

Cell Line A549 cells RH41 cells LnCaP95 cells VCaP cells 22Rv1 cells B16F10 cells HeLa cells HCCLM3 Hep3B HepG2 BH1406 cells MDA-MB-436 MDA-MB-231 RH4 cells H460 A549	Concentration	Treated Time	Description	References
A549 cells	50 and 100 nM	16 hours	Induced degradation of BRD4 protein	J Med Chem. 2024 May 9;67(9):7301-7311.
RH41 cells	297.7 nM (IC50)	120 hours	Assessed cell proliferation inhibition, ARV-771 had an IC50 of 297.7 nM, showing higher potency than JQ1	Pharmaceuticals (Basel). 2023 Jan 29;16(2):199.
LnCaP95 cells	<5 nM	16 hours	ARV-771 effectively degrades BRD2/3/4 proteins in LnCaP95 cells with a DC50 value <5 nM	Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9.
VCaP cells	<5 nM	16 hours	ARV-771 effectively degrades BRD2/3/4 proteins in VCaP cells with a DC50 value <5 nM	Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9.
22Rv1 cells	<5 nM	16 hours	ARV-771 effectively degrades BRD2/3/4 proteins in 22Rv1 cells with a DC50 value <5 nM	Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9.
B16F10 cells	10, 20, 50, 100, 200 nM	24 hours	Evaluate the effect of ARV@PDSA on BRD4 protein degradation, showing that ARV@PDSA degrades BRD4 more effectively than free ARV-771 at low concentrations.	Adv Sci (Weinh). 2023 Jun;10(16):e2207439.
HeLa cells	10, 20, 50, 100, 200 nM	24 hours	Evaluate the effect of ARV@PDSA on BRD4 protein degradation, showing that ARV@PDSA degrades BRD4 more effectively than free ARV-771 at low concentrations.	Adv Sci (Weinh). 2023 Jun;10(16):e2207439.
HCCLM3	0.5 µM	24 hours	To evaluate the effect of ARV-771 on HCC cell viability, results showed that ARV-771 dose-dependently inhibited HCC cell viability.	Front Pharmacol. 2022 May 4;13:858901.
Hep3B	0.25 µM	24 hours	To evaluate the effect of ARV-771 on HCC cell viability, results showed that ARV-771 dose-dependently inhibited HCC cell viability.	Front Pharmacol. 2022 May 4;13:858901.
HepG2	0.5 µM	24 hours	To evaluate the effect of ARV-771 on HCC cell viability, results showed that ARV-771 dose-dependently inhibited HCC cell viability.	Front Pharmacol. 2022 May 4;13:858901.
BH1406 cells	10 µM	4 days	Evaluate the growth inhibitory effect of ARV-771 on BH1406 cells, showing that ARV-771 significantly inhibited the growth of BH1406 cells and had synergistic effects with BAY-293.	Transl Lung Cancer Res. 2024 Nov 30;13(11):2987-2997.
MDA-MB-436	0.45 µM	4 days	Inhibited cell growth and migration, mainly affected cytokines and their receptors	Breast Cancer Res Treat. 2024 Nov;208(1):89-101.
MDA-MB-231	0.12 µM	4 days	Inhibited cell growth and migration, significantly reduced expression of ERBB family receptors	Breast Cancer Res Treat. 2024 Nov;208(1):89-101.
RH4 cells	100 nM	6 hours	Assessed BRD4 degradation efficacy, immunofluorescence showed near-complete removal of BRD4 from the cell nucleus	Pharmaceuticals (Basel). 2023 Jan 29;16(2):199.
H460	5 µM		Inhibited radiation-induced and cisplatin-induced tumour cell surface PD-L1 expression	Clin Transl Med. 2022 Jan;12(1):e718.
A549	5 µM		Inhibited radiation-induced and cisplatin-induced tumour cell surface PD-L1 expression	Clin Transl Med. 2022 Jan;12(1):e718.

Cell Line

Concentration

Treated Time

Description

References

A549 cells

50 and 100 nM

16 hours

Induced degradation of BRD4 protein

J Med Chem. 2024 May 9;67(9):7301-7311.

RH41 cells

297.7 nM (IC50)

120 hours

Assessed cell proliferation inhibition, ARV-771 had an IC50 of 297.7 nM, showing higher potency than JQ1

Pharmaceuticals (Basel). 2023 Jan 29;16(2):199.

LnCaP95 cells

<5 nM

16 hours

ARV-771 effectively degrades BRD2/3/4 proteins in LnCaP95 cells with a DC50 value <5 nM

Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9.

VCaP cells

<5 nM

16 hours

ARV-771 effectively degrades BRD2/3/4 proteins in VCaP cells with a DC50 value <5 nM

Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9.

22Rv1 cells

<5 nM

16 hours

ARV-771 effectively degrades BRD2/3/4 proteins in 22Rv1 cells with a DC50 value <5 nM

Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9.

B16F10 cells

10, 20, 50, 100, 200 nM

24 hours

Evaluate the effect of ARV@PDSA on BRD4 protein degradation, showing that ARV@PDSA degrades BRD4 more effectively than free ARV-771 at low concentrations.

Adv Sci (Weinh). 2023 Jun;10(16):e2207439.

HeLa cells

10, 20, 50, 100, 200 nM

24 hours

Evaluate the effect of ARV@PDSA on BRD4 protein degradation, showing that ARV@PDSA degrades BRD4 more effectively than free ARV-771 at low concentrations.

Adv Sci (Weinh). 2023 Jun;10(16):e2207439.

HCCLM3

0.5 µM

24 hours

To evaluate the effect of ARV-771 on HCC cell viability, results showed that ARV-771 dose-dependently inhibited HCC cell viability.

Front Pharmacol. 2022 May 4;13:858901.

Hep3B

0.25 µM

24 hours

To evaluate the effect of ARV-771 on HCC cell viability, results showed that ARV-771 dose-dependently inhibited HCC cell viability.

Front Pharmacol. 2022 May 4;13:858901.

HepG2

0.5 µM

24 hours

To evaluate the effect of ARV-771 on HCC cell viability, results showed that ARV-771 dose-dependently inhibited HCC cell viability.

Front Pharmacol. 2022 May 4;13:858901.

BH1406 cells

10 µM

4 days

Evaluate the growth inhibitory effect of ARV-771 on BH1406 cells, showing that ARV-771 significantly inhibited the growth of BH1406 cells and had synergistic effects with BAY-293.

Transl Lung Cancer Res. 2024 Nov 30;13(11):2987-2997.

MDA-MB-436

0.45 µM

4 days

Inhibited cell growth and migration, mainly affected cytokines and their receptors

Breast Cancer Res Treat. 2024 Nov;208(1):89-101.

MDA-MB-231

0.12 µM

4 days

Inhibited cell growth and migration, significantly reduced expression of ERBB family receptors

Breast Cancer Res Treat. 2024 Nov;208(1):89-101.

RH4 cells

100 nM

6 hours

Assessed BRD4 degradation efficacy, immunofluorescence showed near-complete removal of BRD4 from the cell nucleus

Pharmaceuticals (Basel). 2023 Jan 29;16(2):199.

H460

5 µM

Inhibited radiation-induced and cisplatin-induced tumour cell surface PD-L1 expression

Clin Transl Med. 2022 Jan;12(1):e718.

A549

5 µM

Inhibited radiation-induced and cisplatin-induced tumour cell surface PD-L1 expression

Clin Transl Med. 2022 Jan;12(1):e718.

ARV-771 动物实验

Species Nu/Nu mice SCID mice Nude mice Nude mice	Animal Model 22Rv1 tumor xenograft model A549 xenograft model HepG2 xenograft model HeLa tumor model	Administration	Dosage	Frequency	Description	References
Nu/Nu mice	22Rv1 tumor xenograft model	Subcutaneous injection	10 mg/kg	Once daily for 3 days	ARV-771 significantly reduces BRD4 and c-MYC levels and induces tumor regression in the 22Rv1 tumor xenograft model	Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9.
SCID mice	A549 xenograft model	Intraperitoneal injection	20 mg/kg	5 days ON/2 days OFF for 19 days	Significantly inhibited tumor growth without observable toxicity	J Med Chem. 2024 May 9;67(9):7301-7311.
Nude mice	HepG2 xenograft model	Intraperitoneal injection	20 mg/kg	Every other day for 25 days	To evaluate the inhibitory effect of ARV-771 on HCC progression in vivo, results showed that ARV-771 significantly inhibited tumor growth.	Front Pharmacol. 2022 May 4;13:858901.
Nude mice	HeLa tumor model	Intravenous injection	3 mg/kg and 10 mg/kg	Every other day for 12 days	Evaluate the anti-tumor efficacy of ARV@PDSA in vivo, showing significant tumor growth inhibition, BRD4 degradation, and c-Myc downregulation.	Adv Sci (Weinh). 2023 Jun;10(16):e2207439.

Species

Nu/Nu mice SCID mice Nude mice Nude mice

Animal Model

22Rv1 tumor xenograft model A549 xenograft model HepG2 xenograft model HeLa tumor model

Administration

Dosage

Frequency

Description

References

Nu/Nu mice

22Rv1 tumor xenograft model

Subcutaneous injection

10 mg/kg

Once daily for 3 days

ARV-771 significantly reduces BRD4 and c-MYC levels and induces tumor regression in the 22Rv1 tumor xenograft model

Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9.

SCID mice

A549 xenograft model

Intraperitoneal injection

20 mg/kg

5 days ON/2 days OFF for 19 days

Significantly inhibited tumor growth without observable toxicity

J Med Chem. 2024 May 9;67(9):7301-7311.

Nude mice

HepG2 xenograft model

Intraperitoneal injection

20 mg/kg

Every other day for 25 days

To evaluate the inhibitory effect of ARV-771 on HCC progression in vivo, results showed that ARV-771 significantly inhibited tumor growth.

Front Pharmacol. 2022 May 4;13:858901.

Nude mice

HeLa tumor model

Intravenous injection

3 mg/kg and 10 mg/kg

Every other day for 12 days

Evaluate the anti-tumor efficacy of ARV@PDSA in vivo, showing significant tumor growth inhibition, BRD4 degradation, and c-Myc downregulation.

Adv Sci (Weinh). 2023 Jun;10(16):e2207439.

ARV-771 动物研究

Dose

Mice: 10 mg/kg^[1] (s.c.)

Administration

s.c.

ARV-771 参考文献

ARV-771 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.01mL

0.20mL

0.10mL

5.07mL

1.01mL

0.51mL

10.14mL

2.03mL

1.01mL

ARV-771 技术信息

CAS号	1949837-12-0
分子式	C₄₉H₆₀ClN₉O₇S₂
分子量	986.64
SMILES Code	O=C([C@H]1N(C([C@H](C(C)(C)C)/N=C(O)/COCCCOCCNC(C[C@H]2C3=NN=C(C)N3C4=C(C(C)=C(C)S4)C(C5=CC=C(Cl)C=C5)=N2)=O)=O)C[C@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C
MDL No.	MFCD30738017

别名
运输	蓝冰
InChI Key	PQOGZKGXGLHDGS-QQRWPDCKSA-N
Pubchem ID	126619980

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 50 mg/mL(50.68 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

动物实验：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

方案一

方案二

方案三

ARV-771 {[allProObj[0].p_purity_real_show]}

ARV-771 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

ARV-771 质控信息

ARV-771 生物活性

ARV-771 细胞实验

ARV-771 动物实验

ARV-771 动物研究

ARV-771 参考文献

ARV-771 实验方案

ARV-771 技术信息

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ARV-771 {[allProObj[0].p_purity_real_show]}

ARV-771 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

ARV-771 质控信息

ARV-771 生物活性

ARV-771 细胞实验

ARV-771 动物实验

ARV-771 动物研究

ARV-771 参考文献

ARV-771 实验方案

ARV-771 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

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