|S1548||Dapagliflozin||<1 mg/mL||82 mg/mL||17 mg/mL|
|S2760||Canagliflozin||<1 mg/mL||88 mg/mL||<1 mg/mL|
|S8022||Empagliflozin (BI 10773)||<1 mg/mL||90 mg/mL||<1 mg/mL|
|S8103||Sotagliflozin (LX4211)||<1 mg/mL||84 mg/mL||17 mg/mL|
|S8558||Tofogliflozin(CSG 452)||4 mg/mL||84 mg/mL||84 mg/mL|
|S8637||Ipragliflozin (ASP1941)||<1 mg/mL||80 mg/mL||80 mg/mL|
|S2342||Phloretin||<1 mg/mL||54 mg/mL||54 mg/mL|
|S2343||Phlorizin||<1 mg/mL||87 mg/mL||9 mg/mL|
Dapagliflozin is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.
(B) Clonogenic survival of prostate cancer cells treated with Canagliflozin, Dapagliflozin or Salicylate and expressed relative to the vehicle controls.
Canagliflozin is a highly potent and selective SGLT2 inhibitor for hSGLT2 with IC50 of 2.2 nM in a cell-free assay, exhibits 413-fold selectivity over hSGLT1.
Canagliflozin dose-dependently increases pAMPK and pACC in PC3 cells after 30 min
Empagliflozin (BI-10773) is a potent and selective SGLT-2 inhibitor with IC50 of 3.1 nM, exhibits >300-fold selectivity over SGLT-1, 4, 5 and 6. Phase 3.
Sotagliflozin (LX4211) is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively. Phase 3.
Tofogliflozin is a novel sodium-glucose co-transporter 2(SGLT2) inhibitor with IC50 values of 2.9 nM and 8444 nM for hSGLT2 and Hsglt1, respectively.
Ipragliflozin (ASP1941) is a highly selective sodium-glucose cotransporter 2 (SGLT2) inhibitor with an IC50 value of 7.4 nM for hSGLT2 and a 254-fold selectivity versus SGLT1.
Phloretin is a dihydrochalcone found in apple tree leaves, which shows beneficial effects on diabetes.
Specificity of FDG uptake in BJAB, OCI-LY3 and SU-DHL-6 cells. Cells were incubated without inhibitors or with 2 mM 2-DG, 5 μM cytochalasin B or 10 μM phloretin for 24 h or with 50 μM CoCl2 for 30 min and 100 kBq of FDG for 30 min. Cell-bound radioactivity was normalized to protein concentration determined from a parallel sample and expressed as % of untreated control, mean ± standard deviation from fourfold determinations; Asterisks indicates significant decrease or increase (p < 0.05, Student’s t test)
Phlorizin is a dihydrochalcone found in the bark of pear (Pyrus communis), apple, cherry and other fruit trees.
The survival of cells treated with PQ in the presence or absence of STF-31 (d), phlorizin (e), or AA (f) was determined as explained