SB-02024

SB-02024 is an inhibitor of vacuolar protein sorting 34 (VPS34, IC50 = 5 nM). 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. 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. 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 (Cay-27901) in a B16/F10 murine melanoma model.Formal Name: 4-[(3R)-3-methyl-4-morpholinyl]-6-[(2R)-2-(trifluoromethyl)-1-piperidinyl]-2(1H)-pyridinone. CAS Number: 2126737-28-6. Molecular Formula: C16H22F3N3O2. Formula Weight: 345.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Slightly soluble: 0.1-1 mg/ml, DMSO: Sparingly soluble: 1-10 mg/ml. SMILES: C[C@H](COCC1)N1C2=CC(NC(N(CCCC3)[C@H]3C(F)(F)F)=C2)=O. InChi Code: InChI=1S/C16H22F3N3O2/c1-11-10-24-7-6-21(11)12-8-14(20-15(23)9-12)22-5-3-2-4-13(22)16(17,18)19/h8-9,11,13H,2-7,10H2,1H3,(H,20,23)/t11-,13-/m1/s1. InChi Key: IARAUFAUVKBTEM-DGCLKSJQSA-N.