Anticancer agent 82
Modify Date: 2024-01-12 11:23:37
Anticancer agent 82 structure
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Common Name | Anticancer agent 82 | ||
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| CAS Number | 2319587-80-7 | Molecular Weight | 389.28 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C19H18Cl2N4O | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Anticancer agent 82Anticancer 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]. |
| Name | Anticancer agent 82 |
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| 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]. |
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| Related Catalog | |
| Target |
vimentin (VIM)[1] |
| In Vitro | Anticancer agent 82 (compound 4e) (0-10 mM; 72 h) inhibits a marked improvement in potency with an IC50 value of 44 nM against HT-1080 fibrosarcoma, better than than FiVe1 (IC50=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 IC50s of 44 nM, 61 nM, and 49 nM, respectively. |
| In Vivo | Anticancer agent 82 (compound 4e) (10 mg/kg; p.o.; single dose) shows better oral pharmacokinetic properties than Five1[1]. Pharmacokinetic properties of Anticancer agent 82 in mice[1] Route Dose (mg/kg) AUC0-last (ng·h/mL) AUC0-inf (ng·h/mL) T1/2 (h) Tmax (h) Tlast (h) Cmax (ng/mL) 4e PO 10 371.33 534.33 4.68 0.67 8 154.67 4e IP 1 208.33 211.33 0.59 0.25 4 197.00 Five1 PO 25 309.78 339.21 4.57 0.5 18 110.43 |
| References |
| Molecular Formula | C19H18Cl2N4O |
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| Molecular Weight | 389.28 |