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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。 | |||||||||||||||||||
| 靶点 | 
 | 
| 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]. | 
| 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. | 
| 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. | 
| 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 | |
| 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 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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			沪ICP备2024050318号-1
			沪公网安备 31011702889066号
			
			沪ICP备2024050318号-1