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CAS No.: 2442597-56-8

VU6015929 Catalog No. CSN25299

VU6015929 is a potent, selective and orally active dual discoidin domain receptor 1/2 (DDR1/2) inhibitor with IC50 values of 4.67 nM and 7.39 nM, respectively and potently blocks collagen-induced DDR1 activation and collagen-IV production.

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400-920-2911

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400-920-2911

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实验方案

技术信息

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].
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.

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
- 2.0600 mL
- 10.3001 mL
- 20.6001 mL
- 5 mM
- 0.4120 mL
- 2.0600 mL
- 4.1200 mL
- 10 mM
- 0.2060 mL
- 1.0300 mL
- 2.0600 mL

技术信息

CAS号

2442597-56-8

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H19F4N5O2

运输

蓝冰

分子量

485.43

别名

溶解度

DMSO	98.0 mg/mL (201.9 mM)
Water	Insoluble
Ethanol	12.0 mg/mL (24.7 mM)

动物实验配方

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