FKBP12 PROTAC RC32(Synonyms: RC32)

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FKBP12 PROTAC RC32 (Synonyms: RC32) 纯度: 95.23%

FKBP12 PROTAC RC32 (RC32) 是基于 PROTAC 的有效 FKBP12 降解剂。FKBP12 PROTAC RC32 包含雷帕霉素 (Rapamycin；HY-10219) 和Cereblon E3 泛素连接酶配体 (Pomalidomide；HY-10984)。

FKBP12 PROTAC RC32(Synonyms: RC32)

FKBP12 PROTAC RC32 Chemical Structure

CAS No. : 2375555-66-9

规格 价格 是否有货 数量
5 mg ￥6500 In-stock
10 mg ￥11500 In-stock
25 mg ￥22000 In-stock
50 mg ￥36000 In-stock
100 mg ￥58000 In-stock
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500 mg   询价  

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生物活性

FKBP12 PROTAC RC32 (RC32) is a potent FKBP12 degrader based on PROTAC technology. FKBP12 PROTAC RC32 contains conjugation of Rapamycin (HY-10219) and a ligand for an Cereblon E3 ubiquitin ligase (Pomalidomide; HY-10984)[1].

IC50 & Target[1]

Cereblon

 

体外研究
(In Vitro)

FKBP12 PROTAC RC32 (RC32; 0.1-1000 nM; for 12 hours) results in 50% protein degradation (DC50) of ~0.3 nM after only 12 hours of treatment[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.

Western Blot Analysis[1]

Cell Line: Jurkat cells
Concentration: 0.1, 1, 10, 100, 1000 nM
Incubation Time: For 12 hours
Result: Resulted in 50% protein degradation (DC50) of ~0.3 nM after only 12 h of treatment.

体内研究
(In Vivo)

RC32 (RC32; i.p.; 30 mg/kg; twice a day; 1 day) degrades the FKBP12 protein in most of the organs of treated mice, except for the brain after only 1 day of treatment in mice[1].
RC32 (orally; 60 mg/kg; twice a day; for 1 day) significantly degrades FKBP12 in mice[1].
RC32 (i.p.; 8 mg/kg; twice a day; for 2 days) efficiently degrades the FKBP12 protein in most of the organs examined in Bama pigs (20 kg) [1].
RC32 (i.p.; 8 mg/kg; twice a day; for 3 days) efficiently degrades FKBP12 in the heart, liver, kidney, spleen, lung, and stomach of rhesus monkeys[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.

Animal Model: Male and female mice[1]
Dosage: 30 mg/kg
Administration: IP; twice a day; 1 day
Result: Degraded the FKBP12 protein in most of the organs of treated mice after only 1 day of treatment.

分子量

1426.69

Formula

C75H107N7O20
CAS 号

2375555-66-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 10 mg/mL (7.01 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.7009 mL 3.5046 mL 7.0092 mL
5 mM 0.1402 mL 0.7009 mL 1.4018 mL
10 mM — — —

*

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: 1 mg/mL (0.70 mM); Suspended solution; Need ultrasonic

    此方案可获得 1 mg/mL (0.70 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 10.0 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

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. A chemical approach for global protein knockdown from mice to non-human primates. Cell Discov. 2019 Feb 5;5:10.

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