[CAS NO. 2375555-66-9] FKBP12PROTACRC32
PRODUCTS SPECIFICATIONS [2375555-66-9]
DESCRIPTION [2375555-66-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 1426.69 |
| Molecular Formula | C75H107N7O20 |
| 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 |
Summary
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
DMSO : 10 mg/mL ( 7.01 mM ; Need ultrasonic)
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 | --- | --- | --- |
-
1.