9-Aminocamptothecin (9-amino-CPT) is a topoisomerase I inhibitor with potent anticancer activity. 9-Aminocamptothecin inhibits PC-3, PC-3M, DU145, and LNCaP cells with IC50 values of 34.1, 10, 6.5, and 8.9 nM, respectively after 96 h exposure.
9-Aminocamptothecin (9-amino-CPT) inhibits tumor growth at the lowest oral dose (0.35 mg/kg/day), whereas higher oral doses (0.75 and 1 mg/kg/day) and s.c. administration (4 mg/kg/week) causes tumor regression. 9-Aminocamptothecin (9-amino-CPT) is well tolerated at all doses, with no toxic death or weight loss of more than 10% observed in any group. 9-Aminocamptothecin (9-amino-CPT) induces complete remissions in 55 % of SCID mice engrafted with human myeloid leukemia.
| Molecular Weight | 363.37 |
| Formula | C20H17N3O4 |
| CAS Number | 91421-43-1 |
| Solubility (25°C) | DMSO 3 mg/mL (Need ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
[2] C H Takimoto, et al. Ann N Y Acad Sci. The clinical development of 9-aminocamptothecin
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