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NEO2734 {[allProObj[0].p_purity_real_show]}

货号:A1359463 同义名: EP31670

NEO2734是一种口服的双重 p300/CBP 和 BET 溴结构域抑制剂,IC50 值均小于 30 nM。

NEO2734 化学结构 CAS号:2081072-29-7
NEO2734 化学结构
CAS号:2081072-29-7
NEO2734 3D分子结构
CAS号:2081072-29-7
NEO2734 化学结构 CAS号:2081072-29-7
NEO2734 3D分子结构 CAS号:2081072-29-7
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NEO2734 纯度/质量文件 产品仅供科研

货号:A1359463 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 +++

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 +

BRD4BD1, 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 +++

BRD3BD2, IC50: 98 nM

BRD4BD2, 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。

NEO2734 生物活性

靶点
  • p300/CBP

    p300/CBP, IC50:<30 nM

  • BET

    BET, IC50:<30 nM

描述 NEO2734 (EP31670) is an orally active inhibitor selectively targeting both p300/CBP and BET bromodomains, displaying IC50 values of less than 30 nM for each[1]. NEO2734 is effective in both SPOP mutant and wild-type prostate cancer[2].
体内研究

NEO2734 (5, 8, 10 mg/kg, orally) suppresses tumor growth and extends survival in preclinical xenograft models[1].

体外研究

NEO2734 (1 μM) promotes differentiation and induces G1-phase cell cycle arrest[1].

NEO2734 (1 μM) quickly triggers squamous differentiation in NMC cell lines, including the expression of the terminal squamous differentiation markers involucrin and keratins[1].

NEO2734 is effective against both hotspot mutant (F133V) and non-hotspot mutant (Q165P) prostate cancer (PCa) cells in vitro andin vivo[2].

NEO2734 细胞实验

Cell Line
Concentration Treated Time Description References
KG1 100 nM 48 hours NEO2734 significantly downregulated the expression of c-Myc and Bcl2. Hemasphere. 2021 Jul 8;5(8):e610.
KN473 60 µM 72 hours Evaluate the antitumor activity of NEO2734 on UPS cells, results showed over 40% of viable cells remained at higher doses Transl Oncol. 2025 Feb;52:102236.
IB119 25 µM 72 hours Evaluate the antitumor activity of NEO2734 on UPS cells, results showed over 40% of viable cells remained at higher doses Transl Oncol. 2025 Feb;52:102236.
DLBCL cell lines 157 nM (median IC50) 72 hours Evaluate the antiproliferative activity of NEO2734 in DLBCL cell lines, showing higher sensitivity in ABC-DLBCL than GCB-DLBCL Blood Adv. 2020 Sep 8;4(17):4124-4135.
Primary AML cells 6-175 nM 4 days NEO2734 significantly eliminated primary AML cells and reduced cell survival by inducing apoptosis. Hemasphere. 2021 Jul 8;5(8):e610.
KG1a 27-125 nM 96 hours NEO2734 significantly reduced the viability of AML cell lines and induced apoptosis. Hemasphere. 2021 Jul 8;5(8):e610.
MV4;11 100 nM 2 and 5 hours NEO2734 significantly downregulated the expression of c-Myc but had minimal effect on Bcl2, though it reduced MCL1 expression. Hemasphere. 2021 Jul 8;5(8):e610.
THP1 100 nM 2 and 5 hours NEO2734 significantly downregulated the expression of c-Myc and Bcl2. Hemasphere. 2021 Jul 8;5(8):e610.
HL60 27-125 nM 96 hours NEO2734 significantly reduced the viability of AML cell lines and induced apoptosis. Hemasphere. 2021 Jul 8;5(8):e610.
C4-2 cells 2 μM 72 hours To evaluate the inhibitory effect of NEO2734 on the growth of SPOP mutant C4-2 cells. Results showed that F133V mutant cells were resistant to JQ1 but sensitive to NEO2734. EMBO Mol Med. 2019 Nov 7;11(11):e10659.
DU145 cells 2 μM 72 hours To evaluate the inhibitory effect of NEO2734 on the growth of SPOP Q165P mutant DU145 cells. Results showed that NEO2734 significantly inhibited cell growth, with superior effect compared to the combination of JQ1 and CPI-637. EMBO Mol Med. 2019 Nov 7;11(11):e10659.
SNU-407 0.036 µM 72 hours To evaluate the inhibitory effect of NEO2734 on the growth of SNU-407 cells, results showed that NEO2734 significantly inhibited cell growth with an IC50 of 0.036 µM. Front Oncol. 2022 Oct 12;12:1018775.
NCI-H508 0.059 µM 72 hours To evaluate the inhibitory effect of NEO2734 on the growth of NCI-H508 cells, results showed that NEO2734 significantly inhibited cell growth with an IC50 of 0.059 µM. Front Oncol. 2022 Oct 12;12:1018775.
DLD-1 10 µM 48 hours To evaluate the effect of NEO2734 on apoptosis in DLD-1 cells, results showed that NEO2734 induced cleavage of caspase-3, indicating activation of apoptosis. Front Oncol. 2022 Oct 12;12:1018775.
RKO 10 µM 48 hours To evaluate the effect of NEO2734 on apoptosis in RKO cells, results showed that NEO2734 induced cleavage of caspase-3, indicating activation of apoptosis. Front Oncol. 2022 Oct 12;12:1018775.
LOVO 1 µM 48 hours To evaluate the effect of NEO2734 on apoptosis in LOVO cells, results showed that NEO2734 induced cleavage of caspase-3, indicating activation of apoptosis. Front Oncol. 2022 Oct 12;12:1018775.
HCT116 10 µM 24 hours To evaluate the effect of NEO2734 on apoptosis in HCT116 cells, results showed that NEO2734 significantly increased the proportion of Annexin V-positive cells, indicating induction of apoptosis. Front Oncol. 2022 Oct 12;12:1018775.
JR588 0.2863 µM 72 hours Evaluate the antitumor activity of NEO2734 on UPS cells, results showed NEO2734 decreased cell viability through regulation of E2F targets and cell cycle Transl Oncol. 2025 Feb;52:102236.
IB106 1.088 µM 72 hours Evaluate the antitumor activity of NEO2734 on UPS cells, results showed NEO2734 decreased cell viability through regulation of E2F targets and cell cycle Transl Oncol. 2025 Feb;52:102236.

NEO2734 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
SCID (CB17) mice MV4;11 tumor xenograft model Oral 10 mg/kg Once daily for 11 consecutive days NEO2734 significantly inhibited tumor growth of MV4;11 cells. Hemasphere. 2021 Jul 8;5(8):e610.
SCID mice SPOP Q165P mutant PDX model Intraperitoneal injection 30 mg/kg 5 days per week for 3 consecutive weeks To evaluate the inhibitory effect of NEO2734 on the growth of SPOP Q165P mutant PDX tumors. Results showed that NEO2734 significantly suppressed tumor growth, with superior effect compared to the combination of JQ1 and CPI-637. EMBO Mol Med. 2019 Nov 7;11(11):e10659.
Nude mice HCT116 xenograft model Oral gavage 30 mg/kg Administered on days 1, 5, and 9, for a total of 9 days To evaluate the antitumor effect of NEO2734 in the HCT116 xenograft model, results showed that NEO2734 significantly inhibited tumor growth and induced tumor cell apoptosis. Front Oncol. 2022 Oct 12;12:1018775.
Rag2-/- γc-/- mice JR588 and KN473 PDX models Oral 10 mg/kg Once daily (5 days-on/2 days-off) Evaluate the antitumor activity of NEO2734 in vivo, results showed NEO2734 significantly inhibited tumor growth in JR588 PDX model Transl Oncol. 2025 Feb;52:102236.
Mice 22Rv1 xenograft model Intraperitoneal injection 10 mg/kg 5 days per week for 21 days Evaluate the effect of NEO2734 alone or in combination with ENZ on 22Rv1 xenograft tumor growth, results showed combination therapy significantly inhibited tumor growth Cancer Res. 2023 Oct 2;83(19):3192-3204
NOD-SCID mice TMD8 xenograft model Oral 10 mg/kg Once daily, 6 days per week Evaluate the antitumor activity of NEO2734 in a DLBCL xenograft model, showing significant tumor growth inhibition Blood Adv. 2020 Sep 8;4(17):4124-4135.

NEO2734 参考文献

[1]Chevaun D Morrison-Smit, et al. Combined Targeting of the BRD4-NUT-p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734. Mol Cancer Ther. 2020 Jul;19(7):1406-1414.

[2]Yuqian Yan, et al. The novel BET-CBP/p300 dual inhibitor NEO2734 is active in SPOP mutant and wild-type prostate cancer. EMBO Mol Med. 2019 Nov 7;11(11):e10659.

NEO2734 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.30mL

0.46mL

0.23mL

11.48mL

2.30mL

1.15mL

22.97mL

4.59mL

2.30mL

NEO2734 技术信息

CAS号2081072-29-7
分子式C22H24F3N3O3
分子量 435.44
SMILES Code O=C1C(C)=CC(C2=CC=C3N=C(C4CCOCC4)N(CCOC(F)(F)F)C3=C2)=CN1C
MDL No. MFCD32857168
别名 EP31670
运输蓝冰
InChI Key KPWWFNXRLAAREN-UHFFFAOYSA-N
Pubchem ID 126582741
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(241.14 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

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
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方案 三
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