133711-99-6
133711-99-6 structure
- Name: Intoplicine dimesylate
- Chemical Name: Intoplicine methasulfonate
- CAS Number: 133711-99-6
- Molecular Formula: C23H32N4O7S2
- Molecular Weight: 540.65300
- Catalog: Signaling Pathways Cell Cycle/DNA Damage Topoisomerase
- Create Date: 2016-07-21 08:00:50
- Modify Date: 2024-01-12 08:54:32
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Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 105 /M) and thereby increases the length of linear DNA[1][2].
| Name | Intoplicine methasulfonate |
|---|
| Description | Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 105 /M) and thereby increases the length of linear DNA[1][2]. |
|---|---|
| Related Catalog | |
| Target |
Topoisomerase I Topoisomerase II |
| In Vitro | With 1-hour exposure to Intoplicine dimesylate at final concentrations of 2.5 micrograms/mL and 10.0 micrograms/mL, 26% and 54% of the assessable specimens shows positive in vitro responses, respectively[2]. With continuous exposure to Intoplicine dimesylate at concentrations of 0.25 micrograms/mL and 2.5 micrograms/mL, 16% and 71% of the assessable specimens showed positive responses, respectively[2]. Activity is seen against breast (71%), non-small-cell lung (69%), and ovarian (45%) cancer colony-forming units at a Intoplicine dimesylate concentration of 10.0 micrograms/mL after 1-hour exposure[2]. |
| In Vivo | At the highest non-toxic dose (HNTD) (6 mg/kg/injection, total dose, 36 mg/kg), intoplicine dimesylate shows highly active with a T/C of 0% and a corresponding total log cell kill of 3[3]. |
| References |
| Molecular Formula | C23H32N4O7S2 |
|---|---|
| Molecular Weight | 540.65300 |
| Exact Mass | 540.17100 |
| PSA | 192.91000 |
| LogP | 4.83840 |