3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺
中文名称:
3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺
中文同义词:
3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺;BCR-ABL抑制剂(GNF-2)
英文名称:
GNF-2
英文同义词:
3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide GNF-2;GNF-2 3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide;GNF 2, >=98%;3-(6-(4-(TRIFLUOROMETHOXY)PHENYLAMINO)PYRIMIDIN-4-YL)BENZAMIDE;Benzamide, 3-[6-[[4-(trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]-;GNF-2;Bcr-abl Inhibitor;3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide
CAS号:
778270-11-4
分子式:
C18H13F3N4O2
分子量:
374.32
EINECS号:
200-256-5
相关类别:
小分子抑制剂;小分子抑制剂，天然产物;血管生成;细胞生物学试剂;Inhibitors
Mol文件:
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
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。
靶点
Bcr-Abl
Bcr-Abl
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.
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.
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.
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.
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
危险类别码
36/37/38
安全说明
26
WGK Germany
3
