NEO2734|2081072-29-7|-陌孚医药/Medlife

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NEO2734

目录号: PL13479 纯度: ≥99%

CAS No. :2081072-29-7

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中文名称	NEO2734
英文名称	NEO2734
英文别名	EP31670;NEO2734;s9648;CN1C(C(=CC(=C1)C1=CC2=C(N=C(N2CCOC(F)(F)F)C2CCOCC2)C=C1)C)=O
Cas No.	2081072-29-7
分子式	C₂₂H₂₄F₃N₃O₃
分子量	435.44
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

NEO2734 (EP31670) 是具有口服活性的 p300/CBP 和 BET bromodomain 的选择性抑制剂，其IC₅₀ 值均 <30 nM。NEO2734 在 SPOP 突变型和野生型前列腺癌模型中均有活性。

生物活性

NEO2734 (EP31670) is an orally active dual p300/CBP and BET bromodomain selective inhibitor, with IC 50 values of <30 nM for both p300/CBP and BET bromodomains. NEO2734 is active in SPOP mutant and wild-type prostate cancer.

性状

Solid

体外研究(In Vitro)

NEO2734 (1 μM) induces differentiation and G1-phase cell cycle arrest.
NEO2734 (1 μM) rapidly induces squamous differentiation in NMC cell lines, and expression of the terminal squamous differentiation marker, involucrin, or keratins.
NEO2734 is active in both hotspot mutant (F133V) and non-hotspot mutant (Q165P) PCa cells in vitro and in vivo. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

NEO2734 (5, 8, 10 mg/kg, orally) inhibits growth and prolongs survival in pre-clinical xenograft models.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mice (PER-403 and 14169 mo

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : 100 mg/mL (229.65 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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