Theaflavin 3,3'-digallate (TF3) is an antitumor agent. Theaflavin 3,3'-digallate inhibits HCT116 cell growth with an IC50 of 17.26 μM. Theaflavin 3,3'-digallate causes a rapid and sustained decrease in phospho-ERK1/2 and -MEK1/2 protein expression. TF-3 and EGCG have stronger inhibitory effects on Dnmt3a and Dnmt3b than on other methyltransferases. In addition, in silico analysis predicted that TF-3 would bind most specifically to the catalytic domain of Dnmt3a. Injection of TF-3 into control mice 6 weeks after OVX protected against bone loss, which was associated with a lower number of osteoclasts as compared to the numbers in vehicleinjected (saline) OVX mice, but TF-3 had a negligible effect on bone mass and osteoclast number in Dnmt3aRank−/− OVX mice compared to vehicle-injected Dnmt3aRank−/− OVX mice, indicating that, in osteoclasts, TF-3 exerts its effect specifically on Dnmt3a.
| Molecular Weight | 868.7 |
| Formula | C43H32O20 |
| CAS Number | 30462-35-2 |
| Solubility (25°C) | DMSO ≥ 20 mg/mL |
| Storage | -20°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.
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