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SIRT6 activator 12q is potent, selective and orally active SIRT6 activator with IC50 values of 171.20, >200, >200, >200, 0.58 μM for SIRT1, SIRT2, SIRT3, SIRT5, SIRT6, respectively. SIRT6 activator 12q inhibits cell growth and migration. SIRT6 activator 12q induces Apoptosis and cell cycle arrest at G2 phase. SIRT6 activator 12q shows anticancer activity[1]. | [in vivo]
SIRT6 activator 12q (100, 150 mg/kg; p.o.; daily for 30 days) inhibites the tumer growth in a dose-dependent manner in mouse[1].
Pharmacokinetic Parameters of SIRT6 activator 12q in Male Sprague-Dawley rats[1].
| PK parameter | 10 mg/kg p.o. | 2 mg/kg i.v. | | CL (L/h/kg) | | 0.6 ± 0.08 | | Vss (L/kg) | | 1112.8 ± 322.84 | | T1/2 (h) | 7.52 ± 1.44 | 9.06 ± 0.21 | | Tmax (h) | 2.00 ± 0.00 | 0.08 ± 0.00 | | Cmax (ng/mL) | 98.45 ± 3.62 | 5123.70 ± 905.5 | | AUC(0-t)(h·ng/mL) | 704.67 ± 80.47 | 3326.13 ± 476.4 | | AUC(0-∞)(h·ng/mL) | 755.57 ± 80.74 | 3381.49 ± 468.48 | | F (%) | 4.24 ± 0.48 | |
Male Sprague-Dawley rats, 2 mg/kg iv; 10 mg/kg po [1]| Animal Model: | BALB/c female nude mice (human pancreatic tumor xenograft model of PANC-1)[1] | | Dosage: | 100, 150 mg/kg | | Administration: | P.o.; daily for 30 days | | Result: | Inhibited tumer growth in a dose-dependent manner, and a tumor inhibition rate of 90.25% at a dose of 150 mg/kg. |
| [IC 50]
SIRT6: 0.58 μM (EC1.5) | [References]
[1] Chen X, et al. Discovery of Potent Small-Molecule SIRT6 Activators: Structure-Activity Relationship and Anti-Pancreatic Ductal Adenocarcinoma Activity. J Med Chem. 2020 Sep 24;63(18):10474-10495. DOI:10.1021/acs.jmedchem.0c01183 |
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