GNF-2

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的变构非 ATP 竞争性 Bcr-Abl 抑制剂，对 Bcr-abl 转化细胞显示出独特的抗增殖活性。

A potent, allosteric, non-ATP competitive Bcr-Abl inhibitor that shows exclusive antiproliferative activity toward Bcr-abl-transformed cells; causes growth inhibition of Bcr-Abl positive cell lines with IC50s of 273 nM (K562) and 268 nM (SUP-B15); inhibits mutant Bcr-Abl E255V, Y253H cell growth.

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 IC50 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 IC50 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 (IC50 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 IC50 of 267 nM. Cell Proliferation Assay Cell Line:Ba/F3.p210, Ba/F3.p210E255V and Ba/F3.p185Y253H 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.p210E255V 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.p210E255V 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.p210E255V 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.p210E255V 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.

GNF 2 | GNF2

Angiogenesis

Bcr-Abl

Bcr-Abl(K562cellline)|Bcr-Abl(SUP-B15cellline)

Cancer

——

778270-11-4

374.3166

C18H13F3N4O2

>98% (HPLC)

DMSO: ≥ 45 mg/mL

O=C(N)C1=CC=CC(C2=NC=NC(NC3=CC=C(OC(F)(F)F)C=C3)=C2)=C1

Benzamide, 3-[6-[[4-(trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]-

(-20℃)

With Ice Pack

≥ 2 years