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  3. FKBP12 PROTAC RC32

FKBP12 PROTAC RC32 (Synonyms: RC32)

目录号: HY-130835
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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 E3 泛素连接酶配体 (Pomalidomide;HY-10984)。

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FKBP12 PROTAC RC32 Chemical Structure

FKBP12 PROTAC RC32 Chemical Structure

CAS No. : 2375555-66-9

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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].

IC50 & Target[1]

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.
Molecular Weight

1426.69

Formula

C₇₅H₁₀₇N₇O₂₀

CAS No.

2375555-66-9

SMILES

C/C([C@@H](OC)C[C@@]([H])(O[C@]1(C(C(N2[C@]([H])3CCCC2)=O)=O)O)CC[C@H]1C)=C\C=C\C=C\[C@@H](C)C[C@@H](C)C([C@H](OC)[C@H](O)/C(C)=C/[C@H](C(C[C@@H]([C@H](C)C[C@]4([H])CC[C@@H](OCCOCC5=CN(CCOCCOCCNC6=CC=CC(C(N7C8C(NC(CC8)=O)=O)=O)=C6C7=O)N=N5)[C@H](OC)C4)OC3=O)=O)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

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Keywords:

FKBP12 PROTAC RC32RC32RC 32RC-32PROTACProteolysis-targeting chimeraFKBP12degraderrapamycinpomalidomideInhibitorinhibitorinhibit

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产品名称:
FKBP12 PROTAC RC32
目录号:
HY-130835
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