NEO2734 EP31670|cas:2081072-29-7|西域试剂

NEO2734 EP31670,99.79%

产品编号：Bellancom-136938| CAS NO：2081072-29-7| 分子式：C₂₂H₂₄F₃N₃O₃| 分子量：435.44

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-136938	￥3500.00	杭州北京（现货）
Bellancom-136938	￥5800.00	杭州北京（现货）
Bellancom-136938	￥0.00	杭州北京（现货）
Bellancom-136938	￥0.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

NEO2734 EP31670

产品介绍

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 IC₅₀ values of <30 nM for both p300/CBP and BET bromodomains. NEO2734 is active in SPOP mutant and wild-type prostate cancer.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line:	NUT carcinoma patient cell lines (TC-797 and PER-403).
Concentration:	1 μM.
Incubation Time:	6 h.
Result:	Results in greater loss of MYC protein.

体内研究
(In Vivo)

NEO2734 (5, 8, 10 mg/kg, orally) inhibits growth and prolongs survival in pre-clinical xenograft models.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mice (PER-403 and 14169 models).
Dosage:	5, 8, 10 mg/kg
Administration:	Orally, once daily for 28 days.
Result:	Two of the three mice treated with NEO2734 were alive by day 100. Provided markedly improved survival compared with EP, i-BET-762, and even iBET-762+EP by day 100 following initiation of treatment.

体内研究

NEO2734 (5, 8, 10 mg/kg, orally) inhibits growth and prolongs survival in pre-clinical xenograft models.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mice (PER-403 and 14169 models).
Dosage:	5, 8, 10 mg/kg
Administration:	Orally, once daily for 28 days.
Result:	Two of the three mice treated with NEO2734 were alive by day 100. Provided markedly improved survival compared with EP, i-BET-762, and even iBET-762+EP by day 100 following initiation of treatment.

体内研究

NEO2734 (5, 8, 10 mg/kg, orally) inhibits growth and prolongs survival in pre-clinical xenograft models.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mice (PER-403 and 14169 models).
Dosage:	5, 8, 10 mg/kg
Administration:	Orally, once daily for 28 days.
Result:	Two of the three mice treated with NEO2734 were alive by day 100. Provided markedly improved survival compared with EP, i-BET-762, and even iBET-762+EP by day 100 following initiation of treatment.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (229.65 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2965 mL	11.4826 mL	22.9653 mL
5 mM	0.4593 mL	2.2965 mL	4.5931 mL
10 mM	0.2297 mL	1.1483 mL	2.2965 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制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

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.74 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.74 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.74 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。