SIRT6 activator 12q,2601734-99

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SIRT6 activator 12q

CAS No. : 2601734-99-8

MCE 国际站：SIRT6 activator 12q

产品活性：SIRT6 activator 12q 是有效的、选择性的和具有口服活性的 SIRT6 激活剂，对 SIRT1、SIRT2、SIRT3、SIRT5、SIRT6 的 IC₅₀ 值分别为 171.20、>200、>200、>200、0.58 μM。SIRT6 activator 12q 抑制细胞生长和迁移。SIRT6 activator 12q 诱导细胞凋亡 (Apoptosis) 和细胞周期停滞在 G2 期。SIRT6 activator 12q 显示出抗癌活性。

研究领域：Apoptosis  |  Epigenetics  |  Cell Cycle/DNA Damage

作用靶点：Apoptosis  |  Sirtuin

In Vitro: SIRT6 activator 12q (compound12q) (2.5, 5, 10 µM; 14, 18 days) inhibits the colony formation of PANC-1, BXPC-3, MIAPaCa-2, and AsPC-1 cells in a dose-dependent manner.
SIRT6 activator 12q (10, 25, 50 µM; 48 h) induces apoptosis and cell cycle arrest at G2 phase in a dose-dependent manner.
SIRT6 activator 12q (12.5, 25, 50 µM; 48 h) decreases the protein expression of H3K9ac, H3K18ac, and H3K56ac in PANC-1 and BXPC-3 cells in a dose-dependent manner.

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.
Pharmacokinetic Parameters of SIRT6 activator 12q in Male Sprague-Dawley rats.

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

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