Table 1 Characteristics of novel PI3K inhibitors

Pan-PI3K inhibitors

Pictilisib (GDC-0941)

33

3

75

580

0.95 (U-87 MG)

[63, 130]

Taselisib (GDC-0032)

9.1

0.12

0.97

1200

N/A

[131]

Buparlisib (BKM120)

166

116

262

4600

1.28 ± 0.33 (p53 wt cells)

2.08 ± 0.69 (p53 mutant/deleted cells)

[35, 36]

Pilaralisib (XL147, SAR245408)

383

36

23

>15,000

24.0 (U-87 MG)

>30.0 (U-251 and U-373 MG)

[43]

Copanlisib (BAY 80–6946)

3.7

0.7

6.4

45

~0.1 (U-87 MG)

[73, 132]

Sonolisib (PX-866)

>300

2.9

N/A

N/A

N/A

[52]

ZSTK474

44

4.6

49

>10,000

7.0 (U-87 MG)

1.1 (U-251 MG)

[68, 133]

AMG 511

6

2

1

N/A

N/A

[70]

Isoform-selective inhibitors

Alpelisib (BYL719)

1200

290

250

>9100

N/A

[75]

Idelalisib (CAL-101, GS-1101)

565

2.5

89

>1000

39.11 (U-87 MG)

[19, 134]

AMG319

2700

18

850

N/A

N/A

[135]

AZD6482

10

80

1090

N/A

N/A

[136]

CH5132799

120

500

36

1600

N/A

[137]

AS-605240

270

300

8

N/A

N/A

[138]

MLN1117 (INK1117)

4500

1900

13,390

1670

N/A

[139]

Dual PI3K/mTOR inhibitors

Dactolisib (NVP-BEZ235)

75

7

5

6

0.04–0.1

[89, 140]

NVP-BGT226

63

N/A

38

N/A

N/A

[141]

Omipalisib (GSK2126458, GSK458)

0.13

0.024

0.06

0.18/0.3

N/A

[142]

GSK1059615

0.6

2

5

12

N/A

[143]

Voxtalisib (XL765, SAR245409)

113

41

9

160/910

2.6 (U-87 MG)

19.6 (U-251 MG)

>30 (U-373 MG)

[100]

Apitolisib (GDC-0980)

27

7

14

17

N/A

[144]

GDC-0084 (RG7666)

46

3

10

70

0.74 (U-87 MG)

[104]

VS-5584 (SB2343)

68

42

25

37

0.18 (U-87 MG)

[145]

PF-04691502

2.1

1.6

1.9

16

N/A

[146]

Gedatolisib (PF-05212384, PKI-587)

N/A

N/A

5.4

1.6

N/A

[147]

PKI-402

7

14

16

3

0.077 (U-87 MG)

[148]