GNF-2


CAS No. : 778270-11-4

778270-11-4
Price and Availability of CAS No. : 778270-11-4
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Cat. No. : HY-11007
M.Wt: 374.32
Formula: C18H13F3N4O2
Purity: >98 %
Solubility: DMSO : ≥ 100 mg/mL (267.15 mM); H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
Introduction of 778270-11-4 :

GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM [1]. IC50 & Target: Bcr-Abl[1] In Vitro: 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)[1].
GNF-2 (1-10 μM; 48 hours) induces apoptosis of Bcr-abl-transformed cells[1].
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[1].
In Vivo: 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[2].
GNF-2 prevents the LPS-induced increases of N.Oc/B.Pm, the percentage of Oc.S/BS, and the percentage of ES/BS[2].

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