BETd-260 ZBC 260|cas:2093388-62-4|西域试剂

BETd-260 ZBC 260,99.59%

产品编号：Bellancom-101519| CAS NO：2093388-62-4| 分子式：C₄₃H₄₆N₁₀O₆| 分子量：798.89

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货号	价格	库存与货期
Bellancom-101519	￥4500.00	杭州北京（现货）
Bellancom-101519	￥7500.00	杭州北京（现货）
Bellancom-101519	￥15000.00	杭州北京（现货）
Bellancom-101519	￥24000.00	杭州北京（现货）

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BETd-260 ZBC 260

产品介绍

BETd-260 (ZBC 260) 是由Cereblon配体和BET配体相连的PROTAC，在白血病细胞 RS4;11 中，在 30 pM 的低浓度下，能够降低 BRD4 蛋白活性。BETd-260能显著抑制肝细胞癌 HCC 细胞的活性并诱导细胞凋亡 (apoptosis)。

生物活性

BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line. BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells.

体外研究

BETd-260 (ZBC260; Compound 23) is capable of inducing degradation of BRD2, BRD3, and BRD4 proteins at 30–100 pM in the RS4;11 leukemia cells. BETd-260 shows inhibitory activity against the growth of RS4;11 leukemia cells and MOLM-13 cells with IC₅₀s of 51 pM and 2.2 nM, respectively, and induces apoptosis in both RS4;11 and MOLM-13 cell lines at 3-10 nM.
BETd-260 reciprocally modulates the expression of several apoptotic genes in HCC cells, i.e., suppressing the expression of anti-apoptotic Mcl-1, Bcl-2, c-Myc, and XIAP, whereas increasing the expression of pro-apoptotic Bad.

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

体内研究

BETd-260 (5 mg/kg, i.v., every other day, thrice a week for 3 weeks) causes rapid tumor regression with a maximum of >90% regression in mice bearing RS4;11 xenograft tumors, and with no body weight loss or other signs of toxicity in mice. BETd-260 (5 mg/kg, i.v.) degrades the BRD2, BRD3, and BRD4 proteins for more than 24 h, with robust cleavage of PARP and caspase-3, and strong down-regulation of c-Myc protein in RS4;11 xenograft mice model.

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 : 25 mg/mL (31.29 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.2517 mL	6.2587 mL	12.5174 mL
5 mM	0.2503 mL	1.2517 mL	2.5035 mL
10 mM	0.1252 mL	0.6259 mL	1.2517 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 (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 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: ≥ 0.83 mg/mL (1.04 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (1.04 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 8.3 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% corn oil
Solubility: ≥ 0.83 mg/mL (1.04 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (1.04 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 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。