Shelf life (days): 1460.0
Formulation: A solid
Formal Name: (1a,5a,6a)-N-[(2R,14S,18S)-2-[5-(4-cyclopropyl-1-piperazinyl)-2-[(1S)- 1-methoxyethyl]-3-pyridinyl]-1- ethyl-18,19,20,21-tetrahydro-25,25-dimethyl-15,22-dioxo-17H-5,3-([4,2]-endo-thiazolopropano[1,3]-endo-pyridazinomethanoxypropano)-1H-indol-14-yl]-3-oxabicyclo[3.1.0]hexane-6-carboxamide
Purity: ≥98%
Formula Markup: C47H60N8O6S
Formula Weight: 865.1
CAS Number: 2765082-12-8
Notes: A wild-type and mutant Ras protein-protein interaction inhibitor; inhibits the interaction between wild-type K-Ras and seven activating mutation-containing K-Ras variants and C-RAF (EC50s = 5.06-34.5 nM) and the same K-Ras variants and cyclophilin A (EC50s = 1.27-9.12 nM) in BRET assays using U2OS cells expressing the human proteins; inhibits the protein-protein interactions between wild-type N-Ras, N-RasQ61K, N-RasQ61L, and N-RasQ61R and B-RAF (EC50s = 57.7, 53.9, 145, and 181 nM, respectively, in TR-FRET assays) and wild-type H-Ras and H-RasG13R and B-RAF (EC50s = 59.9 and 23.7 nM, respectively, in TR-FRET assays); has antiproliferative activity against a panel of 183 K-Ras-dependent cancer cell lines (median EC50 = 2.4 nM); reduces the proliferation of adagrasib-resistant NCI H358 cells at 10 nM; reduces tumor volumes in SW620 colon, HPAC pancreatic, and NCI H441 lung cancer mouse xenograft models at 10 mg/kg per day
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