Vimseltinib
产品说明书
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同义名 : | DCC-3014 |
| CAS号 : | 1628606-05-2 | |
| 货号 : | A1365584 | |
| 分子式 : | C23H25N7O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 431.49 | |
| MDL号 : | MFCD32858282 | |
| 存储条件： |
Pure form Keep in dark place, inert atmosphere, room temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | DCC-3014 (Vimseltinib) is a potent, selective, orally active inhibitor of colony-stimulating factor 1 receptor (CSF1R/c-Fms), inhibits CSF1R (Colony-stimulating factor 1 receptor) phosphorylated juxtamembrane domain (JMD) with IC50 of 2.8 nM, 100-fold less potency against fully phosphorylated CSF1R (IC50=290 nM). Vimseltinib significantly inhibited CSF1-stimulated expression of cFOS mRNA for > 24 hours post dose after single doses of 3.75 to 30 mg/kg in mouse spleens. In a PC3 prostate cancer peritibial implant xenograft model in nude mice, mice were treated with vimseltinib at 10 mg/kg, administered either once or twice daily on days 0 through 32 (until the average vehicle primary tumor reached 1,000 mm3 in size). Both regimens led to statistically significant protection from bone degradation. Vimseltinib treatment led to a statistically significant 68% decrease in liver CD68+ macrophages when dosed at 15 mg/kg/day in rats. CD68+ macrophages were also reduced in the colon[1]. In addition, DCC-3014 combined with the anti-PDL1 inhibitor avelumab would be safe and tolerable, decrease immunosuppressive myeloid cells, and increase cytotoxic T cells[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.32mL 0.46mL 0.23mL |
11.59mL 2.32mL 1.16mL |
23.18mL 4.64mL 2.32mL |
| 参考文献 |
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