2. Protein Tyrosine Kinase/RTK
  3. Discoidin Domain Receptor
  4. DDR-TRK-1

DDR-TRK-1 是圆盘状受体 1 (DDR1) 的一个选择性抑制剂，其 IC50 值为 9.4 nM。DDR-TRK-1 也抑制 TRK 激酶家族。

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DDR-TRK-1 Chemical Structure

DDR-TRK-1 Chemical Structure

CAS No. : 1934246-19-1

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规格 价格 是否有货 数量
1 mg ￥2207
1 周
5 mg   询价  
10 mg   询价  

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DDR-TRK-1 相关抗体

Top Publications Citing Use of Products

查看 Discoidin Domain Receptor 亚型特异性产品:

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DDR1 DDR2

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

DDR-TRK-1 is a selective Discoidin Domain Receptor 1 (DDR1) inhibitor, with an IC50 value of 9.4 nM. DDR-TRK-1 also inhibits TRK family.

IC50 & Target

IC50: 9.4 nM (DDR1)[1].
体外研究
(In Vitro)

DDR-TRK-1 is a promising candidate, with an IC50 value of 9.4 nM against DDR1. DDR-TRK-1 also exhibits reasonable pharmacokinetic (PK) properties, with an oral bioavailability of 66.8% and a T1/2 value of 1.25 h at an oral dose of 20 mg/kg in rats. However, the area under concentration−time curve (AUC) value of DDR-TRK-1 in mice is obviously higher than that in rats, suggesting its good absorption property in mice. The DDR1 inhibition of DDR1-IN-3 is further validated by determining its binding affinity with the DDR1 protein. It is shown that DDR-TRK-1 bounds tightly to DDR1, with a binding constant (Kd) value of 4.7 nM[1].

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

DDR-TRK-1 相关抗体:
体内研究
(In Vivo)

DDR-TRK-1 prevents these BLM-induced pathological changes in a dose-dependent manner. These results agree with the expression levels of fibrotic markers in lung tissue lysates, including fibronectin and α-smooth muscle actin (SMA). Further analyses also reveal that the administration of DDR-TRK-1 cause a dose-dependent suppression in the content of hydroxyproline, a unique amino acid found in collagen. The above data collectively indicate the promising therapeutic potential of DDR-TRK-1 against the BLM-induced pulmonary fibrosis[1].

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

492.50

Formula

C26H23F3N6O
CAS 号
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.
纯度 & 产品资料
参考文献
Cell Assay
[1]

Panc-1 cells are plated at low density in media in the presence or absence of controls or the indicated concentration of DDR-TRK-1 (0.016, 0.0625, 0.25, 1 μM). Colony formation is evaluated after 1.5-2 weeks by fixing and staining with crystal violet. The effect of DDR1-IN-3 on cell migration is determined through a ‘scratch’ assay. Panc-1 cells are grown to confluence in a 6 well dish. A scratch is made using a p20 pipette tip and cell migration into the wound is determined at 12, 24, 48, 60, and 72 hrs. The effect of control compounds or DDR-TRK-1 at the indicated concentrations is determined at each time point[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
To induce pulmonary damage, 6- to 8-week-old sex- and age-matched wild type or slie mice (at least five animals per group) are intranasally dropped with bleomycin at 5mg/kg BW. The inhibitors (e.g., DDR-TRK-1) are dissolved in water at a concentration of 5 mg/mL and given to the mice orally by gavage twice a day. Hydroxyproline accounts for 13.4% of the total amino acids of collagen; thus its content can be used to reflect the severity of fibrosis. A commercial hydroxyproline kit is used. Briefly, fresh lung tissues are weighted and hydrolyzed to release hydroxyproline. After a series of chemical reactions, a pink color solution is formed and then subjected to measurement of absorbance at 560 nm. The hydroxyproline content of each sample is calculated by comparing with the standards[1].

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

DDR-TRK-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

DDR-TRK-11934246-19-1Discoidin Domain ReceptorInhibitorinhibitorinhibit

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