[CAS NO. 2375555-66-9]  FKBP12PROTACRC32

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PRODUCTS SPECIFICATIONS [2375555-66-9]

Catelog
HY-130835
Brand
MCE
CAS
2375555-66-9

DESCRIPTION [2375555-66-9]

Overview

MDL-
Molecular Weight1426.69
Molecular FormulaC75H107N7O20
SMILESC/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

For research use only. We do not sell to patients.

Summary

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) [1] .


IC50 & Target

Cereblon


In Vitro

FKBP12 PROTAC RC32 (RC32; 0.1-1000 nM; for 12 hours) results in 50% protein degradation (DC 50 ) of ~0.3 nM after only 12 hours of treatment [1] .

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

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 (DC 50 ) 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] .

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

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.

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 10 mg/mL ( 7.01 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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 --- --- ---
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: 1 mg/mL (0.70 mM); Suspended solution; Need ultrasonic

* All of the co-solvents are available by MCE.