FKBP12 PROTAC RC32 RC32,96.40%

产品编号:Bellancom-130835| CAS NO:2375555-66-9| 分子式:C75H107N7O20| 分子量:1426.69

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-130835
6500.00 杭州 北京(现货)
Bellancom-130835
11500.00 杭州 北京(现货)
Bellancom-130835
22000.00 杭州 北京(现货)
Bellancom-130835
36000.00 杭州 北京(现货)
Bellancom-130835
58000.00 杭州 北京(现货)

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FKBP12 PROTAC RC32 RC32

产品介绍 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)。
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).

体外研究

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.

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

Western Blot Analysis

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.
RC32 (orally; 60 mg/kg; twice a day; for 1 day) significantly degrades FKBP12 in mice.
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) .
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.

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

Animal Model: Male and female mice
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.
体内研究

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.
RC32 (orally; 60 mg/kg; twice a day; for 1 day) significantly degrades FKBP12 in mice.
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) .
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.

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

Animal Model: Male and female mice
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.
体内研究

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.
RC32 (orally; 60 mg/kg; twice a day; for 1 day) significantly degrades FKBP12 in mice.
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) .
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.

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

Animal Model: Male and female mice
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.
性状Solid
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 西域 网站选购。
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
参考文献

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