Table 4. IC50 determination of TSC2 deficient cells, cells with TSC2 add back and control vector.
IC50 in nM | |||||||
inhibitor | target | SNU-878 | + TSC2 | + control | SNU-886 | + TSC2 | + control |
Rapamycin | mTORC1 | NR | NR | NR | NR | NR | NR |
WYE-125132 | mTORC1/2 | 55 | 20 | 15 | 55 | 36 | 13 |
AZD8055 | mTORC1/2 | 38 | 24 | 13 | 52 | 41 | 32 |
Torin1 | mTORC1/2 | 300 | 1076 | 205 | 120 | 660 | 140 |
Torin2 | mTORC1/2/PI3Ks/DNA-PK | 12 | 10 | 8 | 9 | 9 | 8 |
INK 128 | mTORC1/2 | 23 | 140 | 12 | 30 | 119 | 16 |
CGP60474 | CDKs, mTOR | 50 | 62 | 64 | 36 | 36 | 24 |
Flavopiridol | pan-CDKs | 172 | 163 | 201 | 121 | 145 | 109 |
BMS-387032 | CDKs | 949 | 1047 | 754 | 978 | 1113 | 1261 |
GSK2126458 | PI3K | 25 | 5 | 14 | 10 | 6 | 5 |
GSK461364 | PLK | 33 | 24 | 21 | 5 | 5 | 7 |
HMN-214 | PLK | 171 | 177 | 100 | 193 | 268 | 204 |
WZ3105 | CLK2/CNSK1E/ FLT3/ ULK1 | 1515 | 1072 | 1152 | 1254 | 1137 | 1050 |
AZD7762 | CHKs | 25 | 40 | 37 | 71 | 58 | 57 |
MK 1775 | Wee1 | 86 | 135 | 110 | 354 | 250 | 112 |
NVP-AUY922 | HSP90 | 12 | ND | ND | 10 | 16 | 7 |
Ganetespib | HSP90 | 14 | 59 | 10 | 35 | 24 | 10 |
IC50 in nM | |||||||
inhibitor | target | SNU-398 | + TSC2 | + control | |||
Rapamycin | mTORC1 | NR | NR | NR | |||
WYE-125132 | mTORC1/2 | 58 | 80 | 25 | |||
AZD8055 | mTORC1/2 | 73 | 109 | 55 | |||
Torin1 | mTORC1/2 | 340 | 679 | 184 | |||
Torin2 | mTORC1/2/PI3Ks/DNA-PK | 19 | 16 | 10 | |||
INK 128 | mTORC1/2 | 67 | 576 | 59 | |||
CGP60474 | CDKs, mTOR | 24 | 33 | 30 | |||
Flavopiridol | pan-CDKs | 68 | 88 | 75 | |||
BMS-387032 | CDKs | 95 | 96 | 85 | |||
GSK2126458 | PI3K | 103 | 122 | 73 | |||
GSK461364 | PLK | 6 | 3 | 4 | |||
HMN-214 | PLK | 223 | 192 | 173 | |||
WZ3105 | CLK2/CNSK1E/ FLT3/ ULK1 | 60 | 68 | 84 | |||
AZD7762 | CHKs | 124 | 107 | 154 | |||
MK 1775 | Wee1 | 144 | 122 | 55 | |||
NVP-AUY922 | HSP90 | 10 | ND | ND | |||
Ganetespib | HSP90 | 9 | 11 | 9 |