Borussertib, CAS 1800070-77-2

Formulation: A solid

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

Purity: ≥98%

Formula Markup: C36H32N6O3

CAS Number: 1800070-77-2

Notes: Borussertib is a covalent and allosteric Akt1 and Akt2 inhibitor (Kis = 2 and 6 nM, respectively).{67797} 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 (Item No. 16292), prevents tumor growth in three patient-derived xenografts (PDX) mouse models of K-Ras-mutant colorectal cancer.{67798}

• SKU: CAY33387-1
• Manufacturer: Cayman Chemical
• Manufacturer SKU: 33387-1
• Package Unit: 1 mg
• Quantity Unit: STK