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Chemical Structure| 1429617-90-2 同义名 : DDR1-IN-2
CAS号 : 1429617-90-2
货号 : A431837
分子式 : C30H29F3N6O
纯度 : 99%+
分子量 : 546.586
MDL号 : MFCD30185014
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(109.77 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.83mL

0.37mL

0.18mL

9.15mL

1.83mL

0.91mL

18.30mL

3.66mL

1.83mL
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.