INY-03-041

INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor GDC-0068 conjugated to Lenalidomide. INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0 nM, 6.8 nM and 3.5 nM, respectively.

Product information

CAS Number: 2503017-97-6

Molecular Weight: 798.41

Formula: C44H56ClN7O5

Chemical Name: 3-[7-[10-[[(2S)-2-(4-chlorophenyl)-3-[4-[(5R, 7R)-7-hydroxy-5-methyl-6, 7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]piperazin-1-yl]-3-oxopropyl]amino]decyl]-3-oxo-1H-isoindol-2-yl]piperidine-2, 6-dione

Smiles: C[C@@H]1C[C@@H](O)C2=NC=NC(=C21)N1CCN(CC1)C(=O)[C@H](CNCCCCCCCCCCC1=CC=CC2=C1CN(C1CCC(=O)NC1=O)C2=O)C1=CC=C(Cl)C=C1

InChiKey: GQGZWBDNMCIYSF-OZDCPDTESA-N

InChi: InChI=1S/C44H56ClN7O5/c1-29-25-37(53)40-39(29)41(48-28-47-40)50-21-23-51(24-22-50)43(56)34(31-14-16-32(45)17-15-31)26-46-20-9-7-5-3-2-4-6-8-11-30-12-10-13-33-35(30)27-52(44(33)57)36-18-19-38(54)49-42(36)55/h10,12-17,28-29,34,36-37,46,53H,2-9,11,18-27H2,1H3,(H,49,54,55)/t29-,34-,36?,37-/m1/s1

Technical Data

Appearance: Solid Power

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

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:

INY-03-041 (10-1000 nM; 2-24 hours; MDA-MB-468 cells) treatment induces potent degradation of all three AKT isoforms in a dose-dependent manner after a 12-h treatment, with maximal degradation observed between 100 and 250 nM. At concentrations of 500 nM and greater, AKT degradation is diminished. Treatment with 250 nM of INY-03-041 over time reveals partial degradation of all AKT isoforms within 4 h and progressive loss of AKT abundance out to 24 h. INY-03-041 exhibits potent in vitro inhibition of S6K1 (IC50 =37.3 nM) and PKG1 (IC50 = 33.2 nM). INY-03-041 displays enhanced anti-proliferative effects compared with GDC-0068 in MDA-MB-468 and HCC1937 cells.

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