AZ12601011,99.88%

产品编号:Bellancom-122856| 分子式:C19H15N5| 分子量:313.36

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-122856
3500.00 杭州 北京(现货)
Bellancom-122856
5800.00 杭州 北京(现货)
Bellancom-122856
15500.00 杭州 北京(现货)
Bellancom-122856
21500.00 杭州 北京(现货)

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AZ12601011

产品介绍 AZ12601011 是一种具有口服活性的,选择性 TGFBR1 激酶抑制剂,IC50 为 18 nM,Kd 为 2.9 nM。AZ12601011 通过选择性的抑制 ALK4TGFBR1ALK7 来抑制 SMAD2 的磷酸化。AZ12601011 抑制乳腺肿瘤的生长。
生物活性

AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .

体外研究

AZ12601011 (0.01-10 μM; for 20 minutes) completely inhibits Phosphorylation of SMAD2 .
AZ12601011 (0.01 µM-10 µM) inhibits the activity of ALK4, ALK7 and TGFBR1 .
AZ12601011 inhibits 4T1 cells growth in vitro (IC50=0.4µM) .

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

Western Blot Analysis

Cell Line: NIH3T3, HaCaT, C2C12, T47D cells
Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM
Incubation Time: 20 minutes
Result: Completely inhibited Phosphorylation of SMAD2.
体内研究
(In Vivo)

AZ12601011 (50mg/kg; oral gavage; twice daily; for 25 days) inhibits tumour growth and metastasis in vivo.

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

Animal Model: Female BALB/c mice at greater than 18g with tumour
Dosage: 50mg/kg
Administration: Oral gavage; twice daily; for 25 days
Result: Inhibited tumour growth and metastasis in vivo.
体内研究

AZ12601011 (50mg/kg; oral gavage; twice daily; for 25 days) inhibits tumour growth and metastasis in vivo.

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

Animal Model: Female BALB/c mice at greater than 18g with tumour
Dosage: 50mg/kg
Administration: Oral gavage; twice daily; for 25 days
Result: Inhibited tumour growth and metastasis in vivo.
体内研究

AZ12601011 (50mg/kg; oral gavage; twice daily; for 25 days) inhibits tumour growth and metastasis in vivo.

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

Animal Model: Female BALB/c mice at greater than 18g with tumour
Dosage: 50mg/kg
Administration: Oral gavage; twice daily; for 25 days
Result: Inhibited tumour growth and metastasis in vivo.
性状Solid
溶解性数据
In Vitro: 

DMSO : 5 mg/mL (15.96 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1912 mL 15.9561 mL 31.9122 mL
5 mM 0.6382 mL 3.1912 mL 6.3824 mL
10 mM 0.3191 mL 1.5956 mL 3.1912 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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