|4-乙基-N-(3-((4-甲基哌嗪-1-基)甲基)-5-(三氟甲基)苯基)-3-(吡唑并[1,5-a]嘧啶-6-基炔基)苯甲酰胺|CsnPharm

CAS No.: 1429617-90-2

7rh Catalog No. CSN21975

Synonyms: DDR1-IN-2;7RH

DDR1-IN-2 is an inhibitor of discoidin domain receptor 1 (DDR1) with IC50 of 13.1 nM, the IC50 of DDR2 is 203 nM.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述DDR1-IN-2 is a selective DDR1 inhibitor with IC50 value of 6.8nM in an enzymatic activity assay. It exhibited less inhibitory effect on DDR2 with IC50 value of 101.4nM. DDR1-IN-2 dose-dependently inhibited phosphorylation of DDR1 in NCI-H23 non-small cell lung cancer cells (NSCLC) expressing high level of DDR1 at doses of 0.5, 1 and 2μM. The inactivation of DDR1 by DDR1-IN-2 induced significant decrease of total protein levels of Bcl-xL and MMP-2. It suppressed the growth of A549, NCI-H23 and NCI-H460 human NSCLC cells with IC50 values of 2.7, 2.1 and 3.0μM, respectively, while the value in K562 human CML cells was approximately 0.038μM. Also it inhibited colony formation by NCI-H23 NSCLC cells with IC50 values of 0.56 and 3.29 μM, respectively. DDR1-IN-2 potently inhibited cell-matrix adhesion by ~17%, ~40% or ~88% at 5.0, 10.0 or 20.0 μM for 2 hours, respectively, as well as inhibited the invasiveness of NCI-H23 cells by ~30%, ~37% or ~82% at 1.0, 2.0 or 5.0 μM for 24 hours, respectively. DDR1-IN-2 possessed good PK profiles with oral bioavailability of 67.4%^[2].
作用机制DDR1-IN-2 tightly binds to the ATP-binding site of DDR1. It inhibited DDR1 in a competitive manner.^[2]
参考文献

[1] Gao M, Duan L, et al. Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors. J Med Chem. 2013 Apr 25;56(8):3281-95.
[2] Gao M, Duan L, Luo J, Zhang L, Lu X, Zhang Y, Zhang Z, Tu Z, Xu Y, Ren X, Ding K. Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors. J Med Chem. 2013 Apr 25;56(8):3281-95. doi: 10.1021/jm301824k. Epub 2013 Apr 10. PMID: 23521020.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8295 mL
- 9.1477 mL
- 18.2954 mL
- 5 mM
- 0.3659 mL
- 1.8295 mL
- 3.6591 mL
- 10 mM
- 0.1830 mL
- 0.9148 mL
- 1.8295 mL

技术信息

CAS号

1429617-90-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H29F3N6O

运输

蓝冰

分子量

546.59

别名

DDR1-IN-2;7RH

溶解度

DMSO	60.0 mg/mL (109.8 mM) warming

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

7rh Catalog No. CSN21975

靶点选择性

请登录您的专属账户

确认信息