Table 1.
Preclinical evaluation of ATM, CHK2, ATR, or CHK1 inhibitors as radiosensitizing and/or chemosensitizing agents
| Target(s) | Agent | Combinations | Refs |
|---|---|---|---|
| ATM | CP466722 | Radiation | 227 |
| ATM | KU55933 | Camptothecin, doxorubicin, etoposide, or radiation | 223 |
| Radiation | 222 | ||
| ATM | KU59403 | Camptothecin, doxorubicin or etoposide | 225 |
| ATM | KU60019 | Radiation | 210 |
| 215 | |||
| 224 | |||
| Radiation and TMZ | 211 | ||
| ATM/ATR | Caffeine | Radiation | 226 |
| ATR | Compound 45 | Cisplatin or radiation | 230 |
| ATR | NU6027 | Camptothecin, cisplatin, doxorubicin, hydroxyurea, radiation, rucaparib or TMZ | 218 |
| ATR | VE-821 | Camptothecin or indotecan | 269 |
| Cisplatin, topotecan or veliparib | 279 | ||
| Radiation | 228 | ||
| ATR | VE-822 | Gemcitabine or radiation | 229 |
| Irinotecan | 269 | ||
| CHK1 | AR458323 | MK-1775 | 288 |
| CHK1 | CHIR-124 | Camptothecin or irinotecan | 219 |
| CHK1 | CCT244747 | Gemcitabine or irinotecan | 189 |
| CHK1 | GNE-783 | TMZ | 252 |
| CHK1 | GNE-900 | Gemcitabine, irinotecan or TMZ | 252 |
| CHK1 | LY2603618 | Gemcitabine | 221 |
| NU1025, olaparib, rucaparib or veliparib | 283 | ||
| CHK1 | SAR-020106 | Gemcitabine or irinotecan | 255 |
| 254 | |||
| Radiation | 217 | ||
| CHK1 | SB-218078 | Gemcitabine | 251 |
| PD-407824 | 251 | ||
| CHK1 | MK-8776 | Cytarabine, gemcitabine or hydroxyurea | 186 |
| Gemcitabine or hydroxyurea | 253 | ||
| MK-1775 | 290 | ||
| 190 | |||
| CHK1/2 | AZD7762 | Gemcitabine and/or MK-1775 | 291 |
| Olaparib, radiation and/or veliparib | 281 | ||
| NU1025, olaparib, radiation or veliparib | 283 | ||
| Gemcitabine | 261 | ||
| 263 | |||
| Gemcitabine, irinotecan, or topotecan | 264 | ||
| Gemcitabine and radiation | 235 | ||
| Olaparib | 282 | ||
| Olaparib and radiation | 285 | ||
| PD184352, PP2, saracatinib, or selumetinib | 287 | ||
| PD184352, radiation, saracatinib and/or selumetinib | 286 | ||
| Radiation | 234 | ||
| 216 | |||
| Veliparib | 278 | ||
| 5-FU and/or radiation | 232 | ||
| CHK1/2 | PF-00477736 | Carboplatin or gemcitabine | 182 |
| MK-1775 | 289 | ||
| CHK1/2 | V158411 | Several chemotherapeutic drugs including camptothecin or gemcitabine | 220 |
| CHK1/2 | XL-844 | Gemcitabine | 262 |
| Radiation | 233 | ||
| CHK1/WEE1 | PD-321852 | Gemcitabine | 265 |
| CHK1/WEE1 | PD-407824 | Gemcitabine | 251 |
| CHK1 and multiple other kinases | UCN-01 | Olaparib | 281 |
| NU1025, olaparib or veliparib | 283 | ||
| PD184352 or selumetinib | 286 | ||
| Dasatinib, PD184352, PP2 or selumetinib | 287 | ||
| Gemcitabine | 261 | ||
| Monastrol | 293 | ||
| Sagopilone | 292 | ||
| CHK2 | CCT241533 | Olaparib or rucaparib | 246 |
| CHK2 | PV1019 | Camptothecin, radiation or topotecan | 231 |
Abbreviation: 5-FU, 5-fluorouracil; TMZ, temozolomide