SKLB1002 is a potent and ATP-competitive VEGFR2 inhibitor with IC50 of 32 nM.
| Cell Experiment | |
|---|---|
| Cell lines | HUVECs, L-02, B16-F10, HepG2, and SW620 cells. |
| Preparation method | Cell proliferation Using MTT assay to measure cell proliferation . Various cells including HUVECs, L-02, B16-F10, HepG2, and SW620 are treated with indicated concentrations of SKLB1002 for 24 hours. Vandetanib and sunitinib serve as positive controls. Each assay is replicated 3 times. |
| Concentrations | ~40 μM |
| Incubation time | 24 hours |
| Animal Experiment | |
|---|---|
| Animal models | Mice bearing SW620 or HepG2 tumors |
| Formulation | 35% (v/v) polyethylene glycol solution containing 5% (v/v) DMSO |
| Dosages | ~100 mg/kg daily |
| Administration | i.p. |
| Molecular Weight | 320.39 |
| Formula | C13H12N4O2S2 |
| CAS Number | 1225451-84-2 |
| Solubility (25°C) | DMSO |
| 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.
[3] Wen Nie, et al. Synergic antitumor effect of SKLB1002 and local hyperthermia in 4T1 and CT26
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