SIRT6 activator 12q

CAS: 2601734-99-8 货号: S647275 分子式: C31H22N2O2 分子量: 454.52
有货
级别和纯度: ≥98%
别名
SIRT6 激活剂 12q
储存条件
-20°C储存
运输条件
超低温运输
★
规格
库存
价格
数量
5mg
S647275-5mg
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¥1,200.90
10mg
S647275-10mg
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¥2,000.90
25mg
S647275-25mg
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¥3,900.90
50mg
S647275-50mg
期货 Stock Image
¥6,000.90
100mg
S647275-100mg
期货 Stock Image
¥9,000.90
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为什么选择此级别

提供 ≥98% 纯度,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


SIRT6 activator 12q is potent, selective and orally active SIRT6 activator with IC 50 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

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: PANC-1, BXPC-3, MIAPaCa-2, and AsPC-1 cells Concentration: 0-100 µM Incubation Time: 72 h Result: Showed antiproliferative activity with IC 50 s of 4.43, 8.27, 7.10, 9.66 µM for PANC-1, BXPC-3, MIAPaCa-2, and AsPC-1 cells, respectively. Cell Cycle AnalysisCell Line: PANC-1, BXPC-3 cells Concentration: 10, 25, 50 µM Incubation Time: 48 h Result: Induced cell cycle arrest at G2 phase in a dose-dependent manner. Apoptosis AnalysisCell Line: PANC-1, BXPC-3 cells Concentration: 10, 25, 50 µM Incubation Time: 48 h Result: Induced apoptosis by increased Annexin V+ populations in a concentration-dependent manner. Western Blot AnalysisCell Line: PANC-1, BXPC-3 cells Concentration: 12.5, 25, 50 µM Incubation Time: 72 h Result: Decreased the protein levels 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 T 1/2 (h) 7.52 ± 1.44 9.06 ± 0.21 T max (h) 2.00 ± 0.00 0.08 ± 0.00 C max (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 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/c female nude mice (human pancreatic tumor xenograft model of PANC-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.

Form:Solid

IC50& Target:SIRT1 171.2 μM (IC 50 ) SIRT2 >200 μM (IC 50 ) SIRT3 >200 μM (IC 50 ) SIRT5 >200 μM (IC 50 ) SIRT6 0.58 μM (IC 50 )

规格

别名
SIRT6 激活剂 12q
规格或纯度
≥98%
英文名称
SIRT6 activator 12q
生化机理
SIRT6 激活剂 12q 是一种强效、选择性和口服活性 SIRT6 激活剂,其对 SIRT1、SIRT2、SIRT3、SIRT5 和 SIRT6 的 IC 50 值分别为 171.20、>200、>200、>200 和 0.58 μM。SIRT6 激活剂 12q 可抑制细胞生长和迁移。SIRT6 激活剂
储存条件
-20°C储存
运输条件
超低温运输
纯度
≥98%
名称和识别符
分子类型
小分子
Smiles
O=C(C1=CC(C2=CC3=C(C=CC=C3)O2)=NC4=C1C=CC=C4)NC(C5=CC=CC=C5)C6=CC=CC=C6
分子量
454.52

技术文档

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高级数据

化学和物理性质
溶解性
DMSO : 25 mg/mL (55.00 mM; ultrasonic and warming and heat to 70°C)
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