标签归档：tgfbr

AZ12601011

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

AZ12601011  纯度: 99.25%

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 ALK4，TGFBR1 和 ALK7 来抑制 SMAD2 的磷酸化。AZ12601011 抑制乳腺肿瘤的生长。

AZ12601011

AZ12601011 Chemical Structure

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3850 In-stock
5 mg ￥3500 In-stock
10 mg ￥5800 In-stock
50 mg ￥15500 In-stock
100 mg ￥21500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

AZ12601011 相关产品

•相关化合物库:

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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 [1].

IC50 & Target[1]

ALK4

 

ALK7

 

体外研究
(In Vitro)

AZ12601011 (0.01-10 μM; for 20 minutes) completely inhibits Phosphorylation of SMAD2 [1].
AZ12601011 (0.01 µM-10 µM) inhibits the activity of ALK4, ALK7 and TGFBR1 [1].
AZ12601011 inhibits 4T1 cells growth in vitro (IC50=0.4µM) [1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

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[1].

上海金畔生物科技有限公司 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[1]
Dosage: 50mg/kg
Administration: Oral gavage; twice daily; for 25 days
Result: Inhibited tumour growth and metastasis in vivo.

分子量

313.36

Formula

C19H15N5
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
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。
参考文献

  • [1]. Spender LC, et al. Preclinical Evaluation of AZ12601011 and AZ12799734, Inhibitors of Transforming Growth Factor βSuperfamily Type 1 Receptors. Mol Pharmacol. 2019 Feb;95(2):222-234.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

TGFBR1-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

TGFBR1-IN-1 

TGFBR1-IN-1 是一种有效的选择性 ALK5 抑制剂，IC50 为 10-100 nM。详细信息请参考专利文献 WO2018004290A1 中的化合物 33。

TGFBR1-IN-1

TGFBR1-IN-1 Chemical Structure

CAS No. : 2170830-26-7

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

TGFBR1-IN-1 is an ALK5 inhibitor extracted from patent WO2018004290A1, Compound 33, has an IC50 of 10-100 nM[1].

IC50 & Target[1]

ALK5

10-100 nM (IC50)

体外研究
(In Vitro)

Transforming Growth Factor-β (TGF-β) signaling regulates various cellular responses such as cell proliferation, differentiation, cell migration and cell death. TGF-β has at least three isoforms TGF-β1, TGF-β2 and TGF-β3. TGF-β1 is two well-conserved single membrane serine/threonine kinase type I (ALK5). ALK5 inhibitos can be used for treating fibrotic disease, tumor, inflammatory disease, and autoimmune disease[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

427.48

Formula

C23H17N5O2S
CAS 号

2170830-26-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Novel pyrazole derivative as alk5 inhibitor and uses thereof. WO2018004290A1.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务