Ipatasertib-NH2

Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) is a ligand for target protein AKT for PROTAC, binds to lenalidomide, a ligand of ubiquitin E3 ligase cereblon (CRBN), via a ten-hydrocarbon linker to form INY-03-041 (HY-133120) to degrade AKT.

Product information

CAS Number: 1001382-14-4

Molecular Weight: 415.92

Formula: C21H26ClN5O2

Synonym:

GDC-0068-NH2

RG7440-NH2

Chemical Name: (2S)-3-amino-2-(4-chlorophenyl)-1-{4-[(5R, 7R)-7-hydroxy-5-methyl-5H, 6H, 7H-cyclopenta[d]pyrimidin-4-yl]piperazin-1-yl}propan-1-one

Smiles: C[C@@H]1C[C@@H](O)C2=NC=NC(=C21)N1CCN(CC1)C(=O)[C@H](CN)C1=CC=C(Cl)C=C1

InChiKey: FKWGZLUCQAOQDJ-KBRIMQKVSA-N

InChi: InChI=1S/C21H26ClN5O2/c1-13-10-17(28)19-18(13)20(25-12-24-19)26-6-8-27(9-7-26)21(29)16(11-23)14-2-4-15(22)5-3-14/h2-5,12-13,16-17,28H,6-11,23H2,1H3/t13-,16-,17-/m1/s1

Technical Data

Appearance: Solid Power

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

Solubility: Soluble in DMSO.

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: ≥360 days 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:

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.

References:

1. You I, et al. Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling. Cell Chem Biol. 2020 Jan 16;27(1):66-73.e7.

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