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Table 1 Characteristics of novel PI3K inhibitors

From: Recent advances in the use of PI3K inhibitors for glioblastoma multiforme: current preclinical and clinical development

Classification Drug name IC50 (nM) IC50 to GBM cells (μM) References
p110α p110β p110δ p110γ mTORC1/2
Pan-PI3K inhibitors Pictilisib (GDC-0941) 3 33 3 75 580 0.95 (U-87 MG) [63, 130]
Taselisib (GDC-0032) 0.29 9.1 0.12 0.97 1200 N/A [131]
Buparlisib (BKM120) 52 166 116 262 4600 1.28 ± 0.33 (p53 wt cells) 2.08 ± 0.69 (p53 mutant/deleted cells) [35, 36]
Pilaralisib (XL147, SAR245408) 39 383 36 23 >15,000 24.0 (U-87 MG) >30.0 (U-251 and U-373 MG) [43]
Copanlisib (BAY 80–6946) 0.5 3.7 0.7 6.4 45 ~0.1 (U-87 MG) [73, 132]
Sonolisib (PX-866) 0.1 >300 2.9 N/A N/A N/A [52]
ZSTK474 16 44 4.6 49 >10,000 7.0 (U-87 MG) 1.1 (U-251 MG) [68, 133]
AMG 511 4 6 2 1 N/A N/A [70]
Isoform-selective inhibitors Alpelisib (BYL719) 5 1200 290 250 >9100 N/A [75]
Idelalisib (CAL-101, GS-1101) 820 565 2.5 89 >1000 39.11 (U-87 MG) [19, 134]
AMG319 3300 2700 18 850 N/A N/A [135]
AZD6482 870 10 80 1090 N/A N/A [136]
CH5132799 14 120 500 36 1600 N/A [137]
AS-605240 60 270 300 8 N/A N/A [138]
MLN1117 (INK1117) 15 4500 1900 13,390 1670 N/A [139]
Dual PI3K/mTOR inhibitors Dactolisib (NVP-BEZ235) 4 75 7 5 6 0.04–0.1 [89, 140]
NVP-BGT226 4 63 N/A 38 N/A N/A [141]
Omipalisib (GSK2126458, GSK458) 0.019 0.13 0.024 0.06 0.18/0.3 N/A [142]
GSK1059615 0.4 0.6 2 5 12 N/A [143]
Voxtalisib (XL765, SAR245409) 39 113 41 9 160/910 2.6 (U-87 MG) 19.6 (U-251 MG) >30 (U-373 MG) [100]
Apitolisib (GDC-0980) 5 27 7 14 17 N/A [144]
GDC-0084 (RG7666) 2 46 3 10 70 0.74 (U-87 MG) [104]
VS-5584 (SB2343) 16 68 42 25 37 0.18 (U-87 MG) [145]
PF-04691502 1.8 2.1 1.6 1.9 16 N/A [146]
Gedatolisib (PF-05212384, PKI-587) 0.4 N/A N/A 5.4 1.6 N/A [147]
PKI-402 2 7 14 16 3 0.077 (U-87 MG) [148]
  1. N/A, not available