Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Anticancer agent 82 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type III intermediate filament protein vimentin ( VIM ), to induce hyperphosphorylation of Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Anticancer agent 82 shows better oral bioavailability and pharmacokinetic profiles than FiVe1 [1].
Pack Size | Availability | Price/USD | Quantity |
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100 mg | 6-8 weeks | $ 1,360.00 |
Description | Anticancer agent 82 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type III intermediate filament protein vimentin ( VIM ), to induce hyperphosphorylation of Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Anticancer agent 82 shows better oral bioavailability and pharmacokinetic profiles than FiVe1 [1]. |
In vitro | Anticancer agent 82 (compound 4e) (0-10 mM; 72 h) inhibits a marked improvement in potency with an IC 50 value of 44 nM against HT-1080 fibrosarcoma, better than than FiVe1 (IC 50 =1.6 μM, HT-1080) [1]. Anticancer agent 82 (0.1 μM; 24 h) induces phosphorylation of VIM at Ser56 [1]. Anticancer agent 82 (100 μM; sampled at 0, 5, 15, 30, 45, and 60 min) exhibits poor stability with 0.0% remaining after 60 min of incubation in mouse liver microsome [1]. Cell Viability Assay [1] Cell Line: HT-1080, RD, and MCF-7 cells Concentration: 0-10 mM Incubation Time: 72 hours Result: Inhibited HT-1080, RD, and MCF-7 cells with IC 50 s of 44 nM, 61 nM, and 49 nM, respectively. |
In vivo | Anticancer agent 82 (compound 4e), administered orally at a dose of 10 mg/kg, demonstrated superior oral pharmacokinetic properties compared to Five1 [1]. Detailed pharmacokinetic analysis in mice [1] revealed that when given orally, compound 4e resulted in an area under the curve (AUC) from time zero to the last measurable concentration (0-last) of 371.33 ng·h/mL, an AUC from time zero to infinity (0-inf) of 534.33 ng·h/mL, a half-life (T 1/2) of 4.68 hours, time to maximum concentration (T max) of 0.67 hours, time of the last measurable concentration (T last) of 8 hours, and a maximum concentration (C max) of 154.67 ng/mL. In comparison, Five1, also given orally but at a 25 mg/kg dose, showed an AUC (0-last) of 309.78 ng·h/mL, AUC (0-inf) of 339.21 ng·h/mL, T 1/2 of 4.57 hours, T max of 0.5 hours, T last of 18 hours, and C max of 110.43 ng/mL. |
Molecular Weight | 389.28 |
Formula | C19H18Cl2N4O |
CAS No. | 2319587-80-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Anticancer agent 82 2319587-80-7 inhibitor inhibit