Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 4-[(3R)-3-methyl-4-morpholinyl]-6-[(2R)-2-(trifluoromethyl)-1-piperidinyl]-2(1H)-pyridinone
Purity: ≥98%
Formula Markup: C16H22F3N3O2
Formula Weight: 345.4
CAS Number: 2126737-28-6
Notes: SB-02024 is an inhibitor of vacuolar protein sorting 34 (VPS34; IC50 = 5 nM).{67895} It selectively binds to VPS34 (Kd = 0.0011 µM) over eight other PI3K kinases (Kds = 1.2693->30 µM), mTOR (Kd = 1.0199 µM), a panel of 468 kinases at 1 µM, and an additional panel of 97 kinases at 1 µM.{67896} SB-02024 (0.7 µM) inhibits autophagic flux in H1299 cells. In vivo, SB-02024 (20 mg/kg) enhances increases in survival when used in combination with an antibody targeting programmed cell death protein 1 (PD-1) or PD-1 ligand (PD-L1) in B16/F10 murine melanoma and CT26 murine colorectal cancer models.{67897} SB-02024 (20 mg/kg) also enhances increases in survival and decreases in tumor volume when used in combination with the STING agonist ADU-S100 (Item No. 27901) in a B16/F10 murine melanoma model.{67895}
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