2095849-04-8
中文名稱(chēng)
CSF1R-IN-1
英文名稱(chēng)
CSF1R-IN-1
CAS
2095849-04-8
分子式
C25H20F3N5O2
分子量
479.45
MOL 文件
2095849-04-8.mol
2095849-04-8 結(jié)構(gòu)式
基本信息
中文別名
化合物CSF1R-IN-1 英文別名
CSF1R-IN-1CSF1R-IN-22
3-Pyridinecarboxamide, 5-(1-methyl-1H-pyrazol-4-yl)-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]-
物理化學(xué)性質(zhì)
沸點(diǎn)528.3±50.0 °C(Predicted)
密度1.34±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)11.58±0.70(Predicted)
形態(tài)Solid
顏色White to off-white
常見(jiàn)問(wèn)題列表
生物活性
CSF1R-IN-1是 CSF1R 的抑制劑，IC50 為0.5 nM。靶點(diǎn)
IC50: 0.5 nM (CSF1R)
體外研究
CSF1R is thought to play an important role in recruitment and differentiation of tumor-associated macrophages (TAMs). CSF1R-IN-1 (compound 22) shows good intestinal permeability in a Caco2 assay.
體內(nèi)研究
CSF1R-IN-1 has favorable pharmacokinetics when dosed orally to mice. It appears suitable for in vivo pharmacology testing in the appropriate preclinical tumor model to demonstrate proof of concept..
| Animal Model: | Male CD-1 mice, 25-35 grams (8-11 weeks old) |
| Dosage: | 2 mg/kg IV or 10 mg/kg orally (Per Os) |
| Administration: | i.v. or oral |
| Result: | I.V.: C max =3.55, T 1/2 =0.87 P.O.: C max =4.6, T 1/2 =1.8, Bioavailability=64% |