PROTAC CBP/P300 Degrader-1 is a potent PROTAC CBP/P300 degrader. PROTAC CBP/P300 Degrader-1 potently inhibited cell viability of multiple cancer cell lines^[1].

PROTAC CBP/P300 Degrader-1 shows LNCaP prostate cancer cell viability inhibition (IC₅₀=0.4 nM). PROTAC CBP/P300 Degrader-1 (10 nM) induces degradation of P300 (≥ 80%)^[1].
PROTAC CBP/P300 Degrader-1 potently inhibited cell viability of multiple cancel cell lines (IC₅₀s ranging from 0.1-141.4 nM for HEL, NOMO-1, MOLM-13, HL-60, MEG-01, MM.IS, MM.1R, NCL-H929, RPM-8226, AMO-1, WSU-DLCL2, Karpas-422, Pfeiffer, SU-DHL-1, LNCap clone FGC, VCap; 22RV1, NCI-H520, NCI-H703, LK-2, 上海金畔生物科技有限公司-7, and SK-BR-3 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.

893.98

C₄₆H₅₃F₂N₁₁O₆

2484739-48-0

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

In Vitro: 

DMSO : 173.33 mg/mL (193.89 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-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: 6.5 mg/mL (7.27 mM); Suspended solution; Need ultrasonic

  此方案可获得 6.5 mg/mL (7.27 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 65.0 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

• [1]. Jing Liu, et al. Cyclic-amp response element binding protein (cbp) and/or adenoviral e1a binding protein of 300 kda (p300) degradation compounds and methods of use. WO2020173440A1.