3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺
![3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺,778270-11-4,结构式](https://www.chemicalbook.com/CAS/GIF/778270-11-4.gif)
- CAS号:778270-11-4
- 英文名:GNF-2
- 中文名:3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺
- CBNumber:CB4973102
- 分子式:C18H13F3N4O2
- 分子量:374.32
- MOL File:778270-11-4.mol
- 储存条件 :2-8°C
- 溶解度 :H2O: <2mg/mL
- 形态 :White solid
- 颜色 :off-white
3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺性质、用途与生产工艺
- 生物活性 GNF-2 是一种具有高度选择性、变构的、非 ATP 竞争性 Bcr-Abl 抑制剂。 GNF-2 抑制 Ba/F3.p210 增殖， IC50 为 138 nM。
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靶点
Bcr-Abl
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体外研究
GNF-2 selectively inhibits Bcr-abl-dependent cell proliferation. GNF-2 (0.005-10 μM; 48 hours) specifically inhibits the proliferation of the Bcr-abl-expressing cells with an IC 50 of 138 nM and not show any cytotoxic effects on the nontransformed cells at concentrations of up to 10 μM. GNF-2 (0.005-10 μM; 48 hours) causes a dose-dependent growth inhibition of the Bcr-abl-positive cell lines with IC 50 values of 273 nM (K562) and 268 nM (SUP-B15). GNF-2 (0.005-10 μM; 48 hours) inhibits E255V and Y253H mutant Bcr-abl cell growth (IC 50 values of 268 and 194 nM, respectively).
GNF-2 (1-10 μM; 48 hours) induces apoptosis of Bcr-abl-transformed cells.
GNF-2 (0.1-10 μM; 90 minutes) inhibits the cellular tyrosine phosphorylation of Bcr-abl in a dose-dependent manner with an IC 50 of 267 nM.
Cell Proliferation Assay
Cell Line: Ba/F3.p210, Ba/F3.p210 E255V and Ba/F3.p185 Y253H cells Concentration: 0.005, 0.01, 0.1, 1, 10 μM Incubation Time: 48 hours Result: Inhibited Bcr-abl-transformed cells proliferation. Apoptosis Analysis
Cell Line: Ba/F3.p210 and Ba/F3.p210 E255V cells Concentration: 1, 10 μM Incubation Time: 48 hours Result: Increased number of Ba/F3.p210 cells undergoing apoptosis at 1 μM for 48 h.
Ba/F3.p210 E255V underwent apoptotic death after 48 h incubation in the presence of 1 μM or higher concentration.Western Blot Analysis
Cell Line: Ba/F3.p210 and Ba/F3.p210 E255V cells Concentration: 0.1, 1, 10 μM Incubation Time: 90 minutes Result: Decreased the autophosphorylation levels at a concentration of 1 μM and were barely detectable at 10 μM, whereas the level of total Bcr-abl remained unchanged.
Induced a significant decrease in the levels of p-Stat5 (at Y694) at 1 μM in Ba/F3.p210 and Ba/F3.p210 E255V cells. -
体内研究
GNF-2 (10 mg/kg; i.p. for 8 days) protects LPS (5 mg/kg) induced bone erosion in mice. GNF-2 protects the LPS induced bone loss and abrogates the LPS-induced decreases of bone volume/tissue volume (BV/TV) of LPS-treated mice.
GNF-2 prevents the LPS-induced increases of N.Oc/B.Pm, the percentage of Oc.S/BS, and the percentage of ES/BS.
Animal Model: Eight-week-old C57/BL6 mice were administered i.p. injections of LPS (5 mg/kg) Dosage: 10 mg/kg Administration: I.p. injections for 8 days; 1 day before and every day after the LPS injection Result: Prevented inflammatory bone destruction in vivo.
- 更新日期：2024/11/08
- 产品编号：HY-11007
- 产品名称：GNF-2
- CAS编号：
- 包装：1 mg
- 价格：293元
- 更新日期：2024/11/08
- 产品编号：HY-11007
- 产品名称：3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺 GNF-2
- CAS编号：778270-11-4
- 包装：5mg
- 价格：700元
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5726
- 优势度：77
