ABC1183,99.19%

产品编号:Bellancom-100950| CAS NO:1042735-18-1| 分子式:C18H14N4OS| 分子量:334.39

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-100950
900.00 杭州 北京(现货)
Bellancom-100950
1440.00 杭州 北京(现货)
Bellancom-100950
3000.00 杭州 北京(现货)
Bellancom-100950
4800.00 杭州 北京(现货)
Bellancom-100950
7680.00 杭州 北京(现货)

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ABC1183

产品介绍 ABC1183 是一种具有口服活性的选择性 GSK3CDK9 双重抑制剂。ABC1183 作用于 GSK3β, GSK3α 和 CDK9/cyclin T1 的 IC50 值分别是 657 nM、327 nM、321 nM。ABC1183 具有抗炎作用,抗肿瘤活性。
生物活性

ABC1183 is an orally active selective dual GSK3 and CDK9 inhibitor. ABC1183 inhibits GSK3β, GSK3α and CDK9/cyclin T1 with the IC50 values of 657 nM, 327 nM and 321 nM, respectively. ABC1183 has anti-inflammatory and anti-tumor activities.

体外研究

ABC1183 (3 μM, 24 h) can block cell cycle progression and thus affect cell proliferation.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis

Cell Line: LNCaP human prostate cancer cells
Concentration: 3 μM
Incubation Time: 24 hours
Result: Significantly reduced cells in the G1 and S phases and increased cells in the G2/M and sub-G1 cycle phases.
体内研究
(In Vivo)

ABC1183 (oral gavage, 5 or 50 mg/kg) inhibits tumor proliferation through negative regulation of cell growth and pro-inflammatory signalling in male C57BL/6 mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6 mice with melanoma B16
Dosage: 5 mg/kg
Administration: Oral gavage; 5 times per week; 22 days
Result: Reduced tumor size and no observed toxicity.
Decreased the expression levels of GSK3 α /β, pSer21/9 and GS pSer641 but no change of total GS expression.
Animal Model: Male C57BL/6 mice infected crohn’s disease
Dosage: 50 mg/kg
Administration: Oral gavage; everyday; 3 days
Result: Reduced TNF-α by 65%, IL-6 by 30% and IL-1β by 45%.
Animal Model: Male C57BL/6 mice with ulcerative colitis
Dosage: 50 mg/kg
Administration: Oral gavage; once daily; 6 days
Result: Increased the expression of the anti-inflammatory factor IL-10, while decreasing the pro-inflammatory factor IL-6.
体内研究

ABC1183 (oral gavage, 5 or 50 mg/kg) inhibits tumor proliferation through negative regulation of cell growth and pro-inflammatory signalling in male C57BL/6 mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6 mice with melanoma B16
Dosage: 5 mg/kg
Administration: Oral gavage; 5 times per week; 22 days
Result: Reduced tumor size and no observed toxicity.
Decreased the expression levels of GSK3 α /β, pSer21/9 and GS pSer641 but no change of total GS expression.
Animal Model: Male C57BL/6 mice infected crohn’s disease
Dosage: 50 mg/kg
Administration: Oral gavage; everyday; 3 days
Result: Reduced TNF-α by 65%, IL-6 by 30% and IL-1β by 45%.
Animal Model: Male C57BL/6 mice with ulcerative colitis
Dosage: 50 mg/kg
Administration: Oral gavage; once daily; 6 days
Result: Increased the expression of the anti-inflammatory factor IL-10, while decreasing the pro-inflammatory factor IL-6.
体内研究

ABC1183 (oral gavage, 5 or 50 mg/kg) inhibits tumor proliferation through negative regulation of cell growth and pro-inflammatory signalling in male C57BL/6 mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6 mice with melanoma B16
Dosage: 5 mg/kg
Administration: Oral gavage; 5 times per week; 22 days
Result: Reduced tumor size and no observed toxicity.
Decreased the expression levels of GSK3 α /β, pSer21/9 and GS pSer641 but no change of total GS expression.
Animal Model: Male C57BL/6 mice infected crohn’s disease
Dosage: 50 mg/kg
Administration: Oral gavage; everyday; 3 days
Result: Reduced TNF-α by 65%, IL-6 by 30% and IL-1β by 45%.
Animal Model: Male C57BL/6 mice with ulcerative colitis
Dosage: 50 mg/kg
Administration: Oral gavage; once daily; 6 days
Result: Increased the expression of the anti-inflammatory factor IL-10, while decreasing the pro-inflammatory factor IL-6.
性状Solid
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (373.82 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9905 mL 14.9526 mL 29.9052 mL
5 mM 0.5981 mL 2.9905 mL 5.9810 mL
10 mM 0.2991 mL 1.4953 mL 2.9905 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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