FKBP12 PROTAC RC32

Modify Date: 2024-01-14 17:29:08

FKBP12 PROTAC RC32 Structure
FKBP12 PROTAC RC32 structure
Common Name FKBP12 PROTAC RC32
CAS Number 2375555-66-9 Molecular Weight 1426.69
Density N/A Boiling Point N/A
Molecular Formula C75H107N7O20 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of FKBP12 PROTAC RC32


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 E3 ubiquitin ligase (Pomalidomide; HY-10984)[1].

 Names

Name FKBP12 PROTAC RC32

 FKBP12 PROTAC RC32 Biological Activity

Description 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 E3 ubiquitin ligase (Pomalidomide; HY-10984)[1].
Related Catalog
Target

Cereblon

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.
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.
References

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

 Chemical & Physical Properties

Molecular Formula C75H107N7O20
Molecular Weight 1426.69
Storage condition -20°C