dBET1|cas:1799711-21-9|西域试剂

dBET1,98.86%

产品编号：Bellancom-101838| CAS NO：1799711-21-9| 分子式：C₃₈H₃₇ClN₈O₇S| 分子量：785.27

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-101838	￥820.00	杭州北京（现货）
Bellancom-101838	￥1320.00	杭州北京（现货）
Bellancom-101838	￥2350.00	杭州北京（现货）
Bellancom-101838	￥5020.00	杭州北京（现货）
Bellancom-101838	￥8500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

dBET1

产品介绍

dBET1 是由Cereblon配体和BRD4配体相连的PROTAC，其 EC₅₀ 值为 430 nM。dBET1 是一种由 BRD4 抑制剂 JQ1 (HY-13030) 与 NSC 527179 (HY-14658) 衍生物通过 linker 产生的 PROTAC，能够在低纳摩尔浓度下诱导 BRD4 降解。

生物活性

dBET1 is a PROTAC connected by ligands for Cereblon and BRD4 with an EC₅₀ of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to NSC 527179 (HY-14658) with a linker.

体外研究

Treatment with dBET1 down regulates MYC and PIM1 transcription. Degradation of BRD4 by dBET1 is associated with a more potent apoptotic consequence in MV4;11 cell line. Significantly increased apoptosis after only 4 h of dBET1 treatment is enhanced at 8 h. dBET1 also induces a potent and superior inhibitory effect on MV4;11 cell proliferation at 24 hours (measured by ATP content, IC₅₀= 0.14 μM, compare to IC₅₀= 1.1 μM with JQ1).

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

体内研究

Administration of dBET1 attenuates tumor progression as determined by serial volumetric measurement, and decreases tumor weight assessed post-mortem. Acute pharmacodynamic degradation of BRD4 is observed four hours after a first or second daily treatment with dBET1 (50 mg/kg IP). A statistically significant destabilization of BRD4, down regulation of MYC and inhibition of proliferation is observed with dBET1 compare to vehicle control in excised tumors. Two weeks of dBET1 is well tolerated by mice without a meaningful effect on weight, white blood count, hematocrit or platelet count.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 43.33 mg/mL (55.18 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.2734 mL	6.3672 mL	12.7345 mL
5 mM	0.2547 mL	1.2734 mL	2.5469 mL
10 mM	0.1273 mL	0.6367 mL	1.2734 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 90% corn oil
Solubility: ≥ 3 mg/mL (3.82 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (3.82 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 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。