778270-11-4
778270-11-4 結(jié)構(gòu)式
基本信息
3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺
CS-569
GNF2
GNF 2
GNF 2, >=98%
GNF-2 USP/EP/BP
Bcr-abl Inhibitor
Bcr-abl Inhibitor - CAS 778270-11-4 - Calbiochem
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]-
安全數(shù)據(jù)
常見(jiàn)問(wèn)題列表
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Bcr-Abl
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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. |
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. |