中文名 | GNF-2 |
英文名 | GNF-2 |
别名 | 化合物GNF-2 BCR-ABL抑制剂(GNF-2) 3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺 |
英文别名 | GNF-2 Bcr-abl Inhibitor 3-(6-(4-(TRIFLUOROMETHOXY)PHENYLAMINO)PYRIMIDIN-4-YL)BENZAMIDE 3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide Benzamide, 3-[6-[[4-(trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]- 3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide GNF-2 GNF-2 3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide |
CAS | 778270-11-4 |
EINECS | 200-256-5 |
化学式 | C18H13F3N4O2 |
分子量 | 374.32 |
溶解度 | H2O: <2 mg/mL |
存储条件 | 2-8°C |
外观 | 白色固体 |
颜色 | off-white |
MDL号 | MFCD09265253 |
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. |
危险品标志 | Xi - 刺激性物品 |
风险术语 | 36/37/38 - 刺激眼睛、呼吸系统和皮肤。 |
安全术语 | 26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.672 ml | 13.358 ml | 26.715 ml |
5 mM | 0.534 ml | 2.672 ml | 5.343 ml |
10 mM | 0.267 ml | 1.336 ml | 2.672 ml |
5 mM | 0.053 ml | 0.267 ml | 0.534 ml |
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