DDR1-IN-4;2-(4-Bromo-2-oxo-1'-(1H-pyrazolo[4,3-b]pyridine-5-carbonyl)spiro[indoline-3,4'-piperidin]-1-yl)-N-(2,2,2-trifluoroethyl)acetamide;2-[4-bromanyl-2-oxidanylidene-1'-(1~{H}-pyrazolo[4,3-b]pyridin-5-ylcarbonyl)spiro[indole-3,4'-piperidine]-1-yl]-~{N}-[2,2,2-tris(fluoranyl)ethyl]ethanamide;DDR1 inhibitor 2.45;BDBM438155;US10618897, Example 23;BrC1=C2C(=CC=C1)N(C(C21CCN(CC1)C(=O)C1=CC=C2C(=N1)C=NN2)=O)CC(=O)NCC(F)(F)F;D6Z
DDR1-IN-4 (Compound 2.45) is a selective and potent Discoidin Domain Receptor 1 (DDR1) autophosphorylation inhibitor, with IC 50 values of 29 nM and 1.9 μM for DDR1 and DDR2, respectively.
性状
Solid
IC50 & Target[1][2]
DDR1 29 nM (IC50) DDR2 1900 nM (IC50
体外研究(In Vitro)
DDR1-IN-4 (Compound 2.45) shows a clear dose-dependent inhibition of DDR1 phosphorylation in HT1080 cells overexpressing DDR1, with greater than 70% inhibition of phosphorylation at a concentration of 1 μM, and retaining selectivity over inhibition of DDR2. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
DDR1-IN-4 (Compound 2.45, ip, 90 mg/kg) preserves renal function and reduces tissue damage in Col4a3 mice (the preclinical mouse model of Alport syndrome) when employing a therapeutic dosing regime, indicating the real therapeutic value of selectively inhibiting DDR1 phosphorylation in vivo. has not independently confirmed the accuracy of these methods. They are for reference only.
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
参考文献
[1]. Hans Richter, et al. DNA-Encoded Library-Derived DDR1 Inhibitor Prevents Fibrosis and Renal Function Loss in a Genetic Mouse Model of Alport Syndrome. ACS Chem Biol. 2019 Jan 18;14(1):37-49.
溶解度数据
In Vitro: DMSO : 250 mg/mL (442.21 mM; Need ultrasonic)配制储备液