2. TGF-beta/Smad
  3. TGF-β Receptor
  4. AZ12799734

AZ12799734 是一种选择性的、具有口服活性的 TGFBR1 激酶抑制剂， IC50 为 47 nM。 AZ12799734 也是一种 BMP 和 TGFβ 抑制剂。

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AZ12799734 Chemical Structure

AZ12799734 Chemical Structure

CAS No. : 1117684-36-2

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规格 价格 是否有货 数量
1 mg ￥636
In-stock
5 mg ￥1400
In-stock
10 mg ￥2250
In-stock
25 mg ￥4950
In-stock
50 mg ￥8000
In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

AZ12799734 相关抗体

Top Publications Citing Use of Products

查看 TGF-β Receptor 亚型特异性产品:

查看所有亚型
ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AZ12799734 is a selective, orally active TGFBR1 kinase inhibitor with an IC50 of 47 nM. AZ12799734 is also a pan BMP and TGFβ inhibitor[1].

IC50 & Target

TGFBR1

47 nM (IC50)

ALK6

0.017 μM (Kd)

ALK5

0.74 μM (Kd)

ALK4

1 μM (Kd)

ACVR1

6.2 μM (Kd)

ALK1

7.1 μM (Kd)

BMPR1A

40 μM (Kd)

BMP

 

体外研究
(In Vitro)

AZ12799734 inhibits ligand activated SMAD3/4 transcription[1].
AZ12799734 (10 nM; 24 h) inhibits phosphorylation of both SMAD1 and SMAD2[1].
AZ12799734 (500 nM; 36 h) inhibits TGFβ-induced migration in HaCaT epithelial cells[1].

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

AZ12799734 相关抗体:

Western Blot Analysis[1]

Cell Line: HaCaT cells and NIH3T3 cells
Concentration: 10 nM
Incubation Time: 10 days (HaCaT) or 24 h (NIH3T3)
Result: Blocked TGFβ-mediated induction of SMAD2 phosphorylation. Inhibited phosphorylation of both SMAD1 and SMAD2.

Cell Migration Assay [1]

Cell Line: HaCaT epithelial cells
Concentration: 500 nM
Incubation Time: 36 h
Result: A dose-dependent decrease in TGFβ-induced migration was observed.
体内研究
(In Vivo)

AZ12799734 (0-400 mg/kg/day; p.o.; 3-7 days) induces histopathologic heart valve lesions in rat[2].
AZ12799734 (50 mg/kg; p.o.; once) shows total and free pharmacokinetic (PK) levels in the nude mouse with time over in vitro IC50 of 0.01885 μM[1].

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

Animal Model: Ten-week-old female HsdHan:WIST rats[2]
Dosage: 200 and 400 mg/kg/day
Administration: Oral, 3-7 days
Result: Hemorrhage into the heart valves was evident at low magnification and the normal architecture of the leaflet was replaced by hemorrhage.
Increased valvular interstitial cells in size and number and shows increased cytoplasm, an enlarged round to spindeloid nucleus, and frequently undergoing mitosis.
Animal Model: Female BALB/c mice[1]
Dosage: 50 mg/kg
Administration: Oral administration (Pharmacokinetic Analysis)
Result: Showed total and free pharmacokinetic (PK) levels with time over in vitro IC50 of 0.01885 μM.
分子量

370.43

Formula

C18H18N4O3S
CAS 号
性状

固体

颜色

White to off-white

运输条件

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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 125 mg/mL (337.45 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6996 mL 13.4978 mL 26.9957 mL
5 mM 0.5399 mL 2.6996 mL 5.3991 mL
查看完整储备液配制表

* 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 (protect from light)。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

AZ12799734 相关分类

完整储备液配制表

* 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 (protect from light)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6996 mL 13.4978 mL 26.9957 mL 67.4891 mL
5 mM 0.5399 mL 2.6996 mL 5.3991 mL 13.4978 mL
10 mM 0.2700 mL 1.3498 mL 2.6996 mL 6.7489 mL
15 mM 0.1800 mL 0.8999 mL 1.7997 mL 4.4993 mL
20 mM 0.1350 mL 0.6749 mL 1.3498 mL 3.3745 mL
25 mM 0.1080 mL 0.5399 mL 1.0798 mL 2.6996 mL
30 mM 0.0900 mL 0.4499 mL 0.8999 mL 2.2496 mL
40 mM 0.0675 mL 0.3374 mL 0.6749 mL 1.6872 mL
50 mM 0.0540 mL 0.2700 mL 0.5399 mL 1.3498 mL
60 mM 0.0450 mL 0.2250 mL 0.4499 mL 1.1248 mL
80 mM 0.0337 mL 0.1687 mL 0.3374 mL 0.8436 mL
100 mM 0.0270 mL 0.1350 mL 0.2700 mL 0.6749 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZ127997341117684-36-2AZ 12799734AZ-12799734TGF-β ReceptorTransforming growth factor beta receptorsHaCaTSMAD1SMAD2SMAD3/4TGFBR1BMPheart valve lesionsInhibitorinhibitorinhibit

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产品名称：
AZ12799734
目录号：
HY-123900
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