|
|
| Product Name: | NSC-12 | | Synonyms: | NSC-12;NSC 12;NSC12;CS-2161;CS-2338;21-Norchol-5-ene-3,20,23-triol, 24,24,24-trifluoro-23-(trifluoromethyl)-, (3β,20S)-;NSC12，NSC 172285 | | CAS: | 102586-30-1 | | MF: | C24H34F6O3 | | MW: | 484.52 | | EINECS: | | | Product Categories: | | | Mol File: | 102586-30-1.mol |  |
| | NSC-12 Chemical Properties |
| Boiling point | 521.8±45.0 °C(Predicted) | | density | 1.31±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMF: 2 mg/ml; DMSO: 0.1 mg/ml; Ethanol: 20 mg/ml; Ethanol:PBS (pH 7.2)(1:2): 0.33 mg/ml | | form | A crystalline solid | | pka | 9.50±0.29(Predicted) |
| | NSC-12 Usage And Synthesis |
| Biological Activity | NSC12 (NSC 172285) is an orally available inhibitor of FGF2/FGFR interaction with potential antitumor activity. | | in vitro | NSC-12 can inhibit FGF-dependent tumor growth, angiogenesis and metastasis. It did not affect FGF2/heparin interaction, but inhibited FGF2 binding to immobilized receptors (IC50 ~30 μM), it disrupted FGF2 interaction with FGFR1, and had no effect on the interaction activity of growth factors with heparin or HSPGs . | | in vivo | Administered by injection and oral route, NSC-12 inhibits FGFR activation, tumor growth, angiogenesis and metastasis in FGF-dependent mouse and human tumor models. In animal models, it significantly reduced tumor weight, tumor cell FGFR1 phosphorylation levels and proliferation, and tumor CD31+ cardiovascular formation. | | target | | Target | Value | FGF3
(Cell-free assay) | 15.9 μM(Kd) | FGF8b
(Cell-free assay) | 18.9 μM(Kd) | FGF22
(Cell-free assay) | 26.8 μM(Kd) | FGF20
(Cell-free assay) | 29.4 μM(Kd) | FGF2/FGFR
(Cell-free assay) | 30 μM |
|
| | NSC-12 Preparation Products And Raw materials |
|