SW044248 is a cell permeable, indolotriazine-based compound that selectively inhibits topoisomerase 1 (Top 1), but not Top 2, catalyzed DNA decatenation in a manner distinct from that of camptothecin (Cat. Nos. 208925 & C9911). SW044248 is shown to exhibit antiproliferation efficacy against a subset of non-small-cell lung cancer (NSCLC) cultures (IC50 <5 μM), including HCC4017 (IC50 = 1.68 μM) as a result of DNA damage and apoptosis induction, while exhibiting little potency toward the non-cancerous HBEC30KT lung epithelial cells (IC50 >10 μM) derived from the same patient as HCC4017.
| Molecular Weight | 421.52 |
| Formula | C22H23N5O2S |
| CAS Number | 522650-83-5 |
| Form | Solid |
| Solubility (25°C) | DMSO: 5 mg/mL (warmed) |
| 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.
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| ICRF-196
ICRF-196 is an racemic mixture of the (S,S)- and (R,R)-isomers of ICRF-193. |
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