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VU6015929

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Chemical Structure| 2442597-56-8 同义名 : -
CAS号 : 2442597-56-8
货号 : A1219698
分子式 : C24H19F4N5O2
纯度 : 97%
分子量 : 485.434
MDL号 : N/A
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(216.3 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 Receptor tyrosine kinases (RTKs) are a group of cell surface receptors essential for cell survival, proliferation, differentiation, and metabolism. Discoidin domain receptors (DDR) 1 and 2 are the members of the RTKs family that can be activated by collagens. VU6015929 is a potent inhibitor of both DDR1 and DDR2 with IC50 values of 4.67±1.6 and 7.39±11.6nM, respectively. In mesangial cells expressing Hu-DDR1b, VU6015929 showed no cytotoxicity at 10M after 24h incubation. Treatment with VU6015929 at 4-100nM dose-dependently blocked collagen I-induced DDR1 auto-phosphorylation in serum-starved HEK293 cells expressing full-length human DDR1 cDNA with an IC50 value of 0.7078±0.3533nM. Also in serum-starved DDR1-null mesangial cells reconstituted with human full length DDR1 cDNA, incubation with VU6015929 for 24h significantly inhibited collagen IV production in a DDR1-dependent manner as compared to the vehicle-treated group. In a rat study (0.5 mg/kg, i.v.; 3 mg/kg, p.o.), VU6015929 showed an in vivo clearance of 34.2mL/min/kg, an ~3h half-life, a volume of distribution at 4.3L/kg at steady state, and 12.5% oral bioavailability[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.06mL

0.41mL

0.21mL

10.30mL

2.06mL

1.03mL

20.60mL

4.12mL

2.06mL
参考文献

[1]Jeffries DE, Borza CM, Blobaum AL, Pozzi A, Lindsley CW. Discovery of VU6015929: A Selective Discoidin Domain Receptor 1/2 (DDR1/2) Inhibitor to Explore the Role of DDR1 in Antifibrotic Therapy. ACS Med Chem Lett. 2019;11(1):29-33.