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.
| Molecular Weight | 540.65 |
| Formula | C23H32N4O7S2 |
| CAS Number | 133711-99-6 |
| Form | Solid |
| Solubility (25°C) | DMSO 115 mg/mL (ultrasonic) Water 100 mg/mL (ultrasonic) |
| Storage | 4°C, protect from light, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Topoisomerase Products |
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| F14512
F14512 is a polyamine-containing inhibitor of DNA topoisomerase II with a broad spectrum of antitumor activities. |
| ICRF-193
ICRF-193 is an TopoII inhibitor. |
| Topoisomerase II inhibitor 15
Topoisomerase II inhibitor 15 is a Topoisomerase II inhibitor. |
| Topoisomerase II inhibitor 13
Topoisomerase II inhibitor 13 is a topoisomerase II (Topo II) inhibitor. |
| ICRF-196
ICRF-196 is an racemic mixture of the (S,S)- and (R,R)-isomers of ICRF-193. |
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