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GNF-2
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| Category | SARS-CoV |
| CAS | 778270-11-4 |
| Description | GNF-2 is a Bcr-Abl inhibitor that binds to the myristoyl binding pocket, an allosteric site distant from the active site, stabilizing the inactive form of the kinase. Thus, it can selectively inhibit Bcr-Abl phosphorylation (IC50 = 267 nM) without affecting native c-Abl or a panel of 63 additional kinases. |
Product Information
| Synonyms | GNF2; GNF-2; GNF 2. |
| Molecular Weight | 374.32 |
| Molecular Formula | C18H13F3N4O2 |
| Canonical SMILES | C1=CC(=CC(=C1)C(=O)N)C2=CC(=NC=N2)NC3=CC=C(C=C3)OC(F)(F)F |
| InChI | InChI=1S/C18H13F3N4O2/c19-18(20,21)27-14-6-4-13(5-7-14)25-16-9-15(23-10-24-16)11-2-1-3-12(8-11)17(22)26/h1-10H,(H2,22,26)(H,23,24,25) |
| InChIKey | WEVYNIUIFUYDGI-UHFFFAOYSA-N |
| Boiling Point | 536.4±50.0 °C at 760 mmHg |
| Flash Point | 278.2±30.1 °C |
| Purity | 98.73% |
| Density | 1.4±0.1 g/cm3 |
| Solubility | In vitro: 10 mM in DMSO |
| Appearance | White to off-white (Solid) |
| Storage | Powder: -20°C: 3 years 4°C: 2 years In solvent: -80°C: 6 months -20°C: 1 month |
| Complexity | 498 |
| Exact Mass | 374.09906016 |
| Index Of Refraction | 1.611 |
| 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). 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. |
| 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. GNF-2 prevents the LPS-induced increases of N.Oc/B.Pm, the percentage of Oc.S/BS, and the percentage of ES/BS. |
| PSA | 90.13000 |
| Target | Bcr-Abl; SARS-CoV |
| Vapor Pressure | 0.0±1.4 mmHg at 25°C |
| XLogP3-AA | 3.8 |
