AZ12601011

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AZ12601011

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

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，K_d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 aK_dof 2.9 nM. AZ12601011 inhibits phosphorylation ofSMAD2via selectively inhibitingALK4,TGFBR1, andALK7. 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].

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].

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

性状

Solid

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℃, 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。