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CereblonE3 泛素连接酶配体 (Pomalidomide；HY-10984)。
| 生物活性 | FKBP12PROTACRC32 (RC32) is a potentFKBP12degrader based onPROTACtechnology. FKBP12PROTACRC32 contains conjugation of Rapamycin (HY-10219) and a ligand for anCereblonE3 ubiquitin ligase (Pomalidomide; HY-10984)[1]. |
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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].
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. |
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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].
| 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. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 10 mg/mL(7.01 mM;Need ultrasonic) 配制储备液 | 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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。 *以上所有助溶剂都可在本网站选购。
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