| Bioactivity | PK 130 is a 2-nitroimidazole derivative that demonstrated potent hypoxic cellular radiosensitization in vitro as assessed by aerobic and hypoxic radiosensitivity of Chinese hamster V79 cells. PK 130 and PK 110 were more potent than SR-2508 at the same concentrations at 0.1 and 1.0 mM. The relative radiosensitization produced by PK 130 and PK 110 at 0.1 mM was comparable to that of 1.0 mM SR-2508. However, at 0.1 mM, the therapeutic effects of PK 130 and PK 110 were only modestly aerobic radiosensitizing. The relative radiosensitization of PK 130 and PK 110 at 0.1 mM was further enhanced by the reduction of glutathione (GSH) levels (less than 5% of control levels) by L-cysteine sulfoxide (BSO). The results of this study encourage the in vivo tumor radiosensitization evaluation of PK 130 and PK 110. |
| CAS | 140448-29-9 |
| Formula | C15H16N4O5 |
| Molar Mass | 332.31 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. 4-FLUOROBENZYLAMINE AND PHENYLALANINE METHYL ESTER CONJUGATES OF 2-NITROIMIDAZOLE: EVALUATION AS HYPOXIC CELL RADIOSENSITIZERS |