Table 2.

mTOR/PI3K dual inhibitors in vitro kinase IC₅₀ (nM)

	PI103 [15,16]	PI540 [16,55]	PI620 [16,55]	NVPBEZ235 [19]	GSK2126458 [22]	SF1126†	NVPBBD130 [41]	PKI402 [45]
mTOR	20/83*	61	231	20.7	0.180/0.300*	1060	n.d./7.7#	3
PI3Kα	2/8	10	7	4	0.019	356	72/71	2
PI3Kβ	3/88	35	63	75	0.13	736	2340/2336	7
PI3Kγ	15/150	331	672	5	0.06	1774	382/350	16
PI3Kδ	3/48	4	8	7	0.024	3225	201/201	14
DNA-PK	23/2	525	147	n.d.	0.28	357	n.d.	n.d.
Chemical structure
Inventor	Astellas	Piramed	Piramed	Novartis	GlaxoSmithKline	Semafore	Novartis	Wyeth

n.d., not determined.

^*IC₅₀ for mTORC1 and mTORC2, respectively.

^#Values obtained in TSC1 null mouse embryonic fibroblasts using phospho-S6 as output.

^†See: http://www.semaforepharma.com/semaforeposterkinase.pdf