XY028-140 is a PROTAC connected by ligands for Cereblon and CDK. XY028-140 inhibits both CDK4/6 expression and CDK4/6 activity in cancer cells^[1].

A375 melanoma and T47D breast cancer cells are treated with 0.3 or 1 µΜ XY028-140 for 24 hours. XY028-140 inhibits both CDK4/6 expression and CDK4/6 activity^[1].
T47D breast cancer cells are treated with 0.03, 0.1, 0.3, 1, or 3 µΜ XY028-140 for 11 days. XY028-140 inhibits cancer cell proliferation in breast cancer cells^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

760.80

C₃₉H₄₀N₁₀O₇

2229974-83-6

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 5.56 mg/mL (7.31 mM; ultrasonic and warming and heat to 60°C)

*

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: 0.56 mg/mL (0.74 mM); Suspended solution; Need ultrasonic

  此方案可获得 0.56 mg/mL (0.74 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 5.6 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

• [1]. Jian Jin, et al. Compositions and methods for treating cdk4/6-mediated cancer. WO2018106870A1.

  [2]. Xuewei Wu, et al. Distinct CDK6 complexes determine tumor cell response to CDK4/6 inhibitors and degraders. Nat Cancer 2, 429-443 (2021).