BETd-260 (ZBC 260) is aPROTACconnected by ligands forCereblonandBET, with as low as 30 pM againstBRD4protein in RS4;11 leukemia cell line^[1]. BETd-260 potently suppresses cell viability and robustly inducesapoptosisin hepatocellular carcinoma (HCC) cells^[2].

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^[1].
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^[2].

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^[1].

798.89

Solid

C₄₃H₄₆N₁₀O₆

2093388-62-4

Room temperature in continental US; may vary elsewhere.

-80°C, protect from light, stored under nitrogen

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

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℃, 6 months (protect from light, stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用。

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。