Borussertib

Borussertib is a covalent and allosteric Akt1 and Akt2 inhibitor (Kis = 2 and 6 nM, respectively). It is selective for Akt1 and Akt2 over Akt3 (Ki = 91 nM). Borussertib (5 µM) reduces viability in Ba/F3 cells expressing human Akt1 or Akt2 but not Ba/F3 cells expressing human Akt3. It decreases the levels of phosphorylated Akt1, Akt2, proline-rich Akt substrate 40 kDa (PRAS40), and ribosomal protein S6 in PANC-1 pancreatic cancer cells when used at concentrations ranging from 0.3 to 5 µM. In vivo, borussertib (20 mg/kg per day), in combination with the MEK1 and MEK2 inhibitor trametinib (Cay-16292), prevents tumor growth in three patient-derived xenografts (PDX) mouse models of K-Ras-mutant colorectal cancer.Formal Name: N-[3-[1-[[4-(5,6-dihydro-5-oxo-3-phenyl-1,6-naphthyridin-2-yl)phenyl]methyl]-4-piperidinyl]-2,3-dihydro-2-oxo-1H-benzimidazol-5-yl]-2-propenamide. CAS Number: 1800070-77-2. Molecular Formula: C36H32N6O3. Formula Weight: 596.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Slightly Soluble: 0.1-1 mg/ml. SMILES: O=C1NC=CC2=NC(C(C=C3)=CC=C3CN(CC4)CCC4N5C(NC6=CC=C(NC(C=C)=O)C=C65)=O)=C(C7=CC=CC=C7)C=C12. InChi Code: InChI=1S/C36H32N6O3/c1-2-33(43)38-26-12-13-31-32(20-26)42(36(45)40-31)27-15-18-41(19-16-27)22-23-8-10-25(11-9-23)34-28(24-6-4-3-5-7-24)21-29-30(39-34)14-17-37-35(29)44/h2-14,17,20-21,27H,1,15-16,18-19,22H2,(H,37,44)(H,38,43)(H,40,45). InChi Key: HXBRBOYWXDLHDC-UHFFFAOYSA-N.