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FKBP12 PROTAC RC32 is a PROTAC-like degrader targeting FKBP12. It can degrade FKBP12 in organs after intraperitoneal administration.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $215 | In Stock |
Description | FKBP12 PROTAC RC32 is a PROTAC-like degrader targeting FKBP12. It can degrade FKBP12 in organs after intraperitoneal administration. |
In vitro | RC32 induced FKBP12 degradation in Hep3B and HuH7 with DC50 values at 0.9 and 0.4 nM. [2] RC32 demonstrated the ability for FKBP12 degradation resulted in 50% protein degradation (DC50) of ~0.3 nM after only 12 h of treatment in Jurkat cells. [3] |
In vivo | The FKBP12 protein in most of the organs of treated mice, except for the brain, was undetectable after only 1 day of treatment with RC32 (intraperitoneal (i.p.) injection, 30 mg/kg, twice a day). A significant degradation of FKBP12 also occurred in the eyes. RC32 had no effect on FKBP12 degradation in brain tissues. [3] When Bama pigs (20 kg) were given RC32 (8 mg/kg, twice a day) for 2 days, the FKBP12 protein was efficiently degraded in most of the organs examined. [3] After 3 days of administration (8 mg/kg, i.p., twice a day), FKBP12 in the heart, liver, kidney, spleen, lung, and stomach of monkeys was efficiently degraded by RC32. [3] |
Alias | RC32 |
Molecular Weight | 1426.69 |
Formula | C75H107N7O20 |
Cas No. | 2375555-66-9 |
Smiles | O=C1NC(C(N2C(C(C=CC=C3NCCOCCOCCN4C=C(COCCO[C@H]5CC[C@@H](C[C@H]([C@](OC([C@@]6([H])N(C(C([C@]7(O)O[C@@]8([H])CC[C@H]7C)=O)=O)CCCC6)=O)([H])CC([C@@H](/C=C(C)\[C@@H](O)[C@@H](OC)C([C@H](C)C[C@H](C)/C=C\C=C\C=C(C)/[C@@H](OC)C8)=O)C)=O)C)C[C@H]5OC)N=N4)=C3C2=O)=O)CC1)=O |
Relative Density. | 1.31 g/cm3 (Predicted) |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||
Solubility Information | DMSO: 5 mg/mL (3.50 mM), Sonication is recommended. | ||||||||||
Solution Preparation Table | |||||||||||
DMSO
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