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。
| 生物活性 | AZ12601011 is an orally active, selectiveTGFBR1 kinaseinhibitor with anIC50of 18 nM and aKdof 2.9 nM. AZ12601011 inhibits phosphorylation ofSMAD2via selectively inhibitingALK4,TGFBR1, andALK7. AZ12601011 inhibits mammary tumor growth[1]. |
| IC50& Target[1] | |
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].
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. |
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体内研究
(In Vivo) | AZ12601011 (50mg/kg; oral gavage; twice daily; for 25 days) inhibits tumour growth and metastasis in vivo[1].
| 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. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 5 mg/mL(15.96 mM;Need ultrasonic) 配制储备液 | 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
