FKBP12 PROTAC RC32 - CAS:2375555-66-9

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FKBP12 PROTAC RC32 (Synonyms:RC32)

目录号 : KM5862 CAS No. : 2375555-66-9 纯度 : 95%

Data Sheet 产品使用指南

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；) 和Cereblon E3 泛素连接酶配体 (Pomalidomide；)。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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Other Forms of Rapamycin:

Ginkgolide B In-stock
Isoginkgetin In-stock
Ginkgolic acid C17:1 In-stock
Ginkgolic Acid In-stock
Propargyl-PEG4-amine In-stock

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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 and a ligand for an Cereblon E3 ubiquitin ligase (Pomalidomide; ).

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.

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

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.

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.

分子量

1426.69

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。