853929-59-6
中文名稱
2-[4-[[3-(4-Bromophenyl)-1-oxo-2-propenyl]amino]-3-fluorophenyl]-5-benzoxazoleaceticacid
英文名稱
2-[4-[[3-(4-Bromophenyl)-1-oxo-2-propenyl]amino]-3-fluorophenyl]-5-benzoxazoleaceticacid
CAS
853929-59-6
分子式
C24H16BrFN2O4
分子量
495.3
MOL 文件
853929-59-6.mol
更新日期
2024/12/08 19:10:50
853929-59-6 結(jié)構(gòu)式
基本信息
中文別名
化合物 T16380 英文別名
OGT 21152-[4-[[3-(4-Bromophenyl)-1-oxo-2-propenyl]amino]-3-fluorophenyl]-5-benzoxazoleaceticacid
(E)-2-(2-(4-(3-(4-Bromophenyl)acrylamido)-3-fluorophenyl)benzo[d]oxazol-5-yl)acetic acid
5-Benzoxazoleacetic acid, 2-[4-[[3-(4-bromophenyl)-1-oxo-2-propen-1-yl]amino]-3-fluorophenyl]-
所屬類別
有機(jī)原料：雜環(huán)化合物物理化學(xué)性質(zhì)
沸點(diǎn)685.9±55.0 °C(Predicted)
密度1.574±0.06 g/cm3(Predicted)
儲(chǔ)存條件Store at RT
溶解度Soluble to 10 mM in DMSO
酸度系數(shù)(pKa)3.85±0.30(Predicted)
形態(tài)粉末
顏色White to yellow
常見問題列表
生物活性
OGT 2115 是一種有效的，細(xì)胞可滲透且口服活性的乙酰肝素酶 (heparanase) 抑制劑，IC50 為 0.4 μM。OGT 2115 具有抗血管生成特性 (IC50 為 1 μM)。OGT 2115 還抑制硫酸乙酰肝素的降解活性。靶點(diǎn)
IC50: 0.4 μM (Heparanase)
體外研究
Heparanase InhibitorOGT 2115 can suppress metastasis induced by endoplasmic reticulum (ER) stress in breast cancer cells, although not significantly. However, compared with the control group, the number and rate of migrated cells are significantly reduced following the exposure of the cells to Tunicamycin + OGT 2115. OGT 2115 significantly inhibits the invasion and migration induced by Adriamycin. Furthermore, the MTT assay results show that OGT 2115 does not decrease the anti-proliferative effect of Adriamycin.
體內(nèi)研究
When administered to mice, OGT 2115 (Compound 12d) shows a plasma concentration of ~10x the heparanase IC 50 following oral dosing at 20 mg/kg.