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).

Product information

CAS Number: 2375555-66-9

Molecular Weight: 1426.69

Formula: C75H107N7O20

Chemical Name: (1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-12-[(2R)-1-[(1S,3R,4R)-4-{2-[(1-{2-[2-(2-{[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]amino}ethoxy)ethoxy]ethyl}-1H-1,2,3-triazol-4-yl)methoxy]ethoxy}-1-hydrogenio-3-methoxycyclohexyl]propan-2-yl]-9,32-dihydrogenio-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.0⁴,⁹]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone

Smiles: CC1=CC=CC=C[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)C(C)=C[C@@H](C)C(=O)C[C@H](OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@]2(O)O[C@H](C[C@@H]1OC)CC[C@H]2C)[C@H](C)C[C@H]1C[C@@H](OC)[C@@H](CC1)OCCOCC1=CN(CCOCCOCCNC2=CC=CC3=C2C(=O)N(C2CCC(=O)NC2=O)C3=O)N=N1 |c:1,t:3,5,20|

InChiKey: XCSUEITWRRFFMN-LPIXFUNRSA-N

InChi: InChI=1S/C75H107N7O20/c1-45-17-12-11-13-18-46(2)61(94-8)41-54-24-22-51(7)75(93,102-54)69(87)73(91)81-29-15-14-21-58(81)74(92)101-62(42-59(83)47(3)38-50(6)67(86)68(96-10)66(85)49(5)37-45)48(4)39-52-23-26-60(63(40-52)95-9)100-36-35-99-44-53-43-80(79-78-53)30-32-98-34-33-97-31-28-76-56-20-16-19-55-65(56)72(90)82(71(55)89)57-25-27-64(84)77-70(57)88/h11-13,16-20,38,43,45,47-49,51-52,54,57-58,60-63,67-68,76,86,93H,14-15,21-37,39-42,44H2,1-10H3,(H,77,84,88)/b13-11-,17-12-,46-18-,50-38-/t45-,47-,48-,49-,51-,52+,54+,57?,58+,60-,61+,62+,63-,67-,68+,75-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

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. RC32 (orally; 60 mg/kg; twice a day; for 1 day) significantly degrades FKBP12 in mice. 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) . 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.

Products are for research use only. Not for human use.