CAS
2765081-21-6
Formulation
A solid
Purity
≥98%
MW
811,1
Shipment
-20
Long Term Storage
-20
Shelf Life
1460
Description
A non-covalent inhibitor of GTP-bound Ras; binds to PPIase A (Kd = 55.3 nM) to form a binary complex that then binds to wild-type K-Ras, K-Ras(G12V), and K-Ras(G12D) (Kds = 131, 364, and 154 nM, respectively); forms a trimeric complex with PPIAse A and a K-Ras, H-Ras, N-Ras, or mutant Ras variant and disrupts the protein-protein interaction between these Ras variants and the B-RAF Ras-binding domain (IC50s = 28-220 nM); induces apoptosis in 28 K-Ras(G12X) and five N-Ras(Q61X) mutant cancer cell lines from 1-100 nM; inhibits intratumoral ERK phosphorylation and reduces tumor volume in Capan-2 and NCI H441 PDAC mouse xenograft models at 25 mg/kg; reduces tumor growth in 29 NSCLC, 22 PDAC, and 23 colorectal cancer K-Ras(G12X) mutant mouse xenograft models at 25 mg/kg
ESCLUSIVAMENTE PER USO DI RICERCA (RUO) e non per uso terapeutico o diagnostico su uomini o animali. Il prodotto NON è un Dispositivo Medico o un Diagnostico in Vitro.
PRODUCT FOR RESEARCH USE ONLY (RUO) and not for therapeutic or diagnostic use on humans or animals. The product is NOT a Medical Device or an In-Vitro Diagnostic (IVD).