| CAS NO: | 1254473-64-7 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 444.31 |
|---|---|
| Formula | C21H19Cl2N5O2 |
| CAS No. | 1254473-64-7 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 88 mg/mL (198.1 mM) |
| Water:<1 mg/mL | |
| Ethanol: 57 mg/mL (128.3 mM) | |
| Solubility (In vivo) | 2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5mg/mL |
| Synonyms | LY 2874455; LY-2874455; LY2874455 Chemical Name: (R,E)-2-(4-(2-(5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazol-3-yl)vinyl)-1H-pyrazol-1-yl)ethanol. InChi Key: GKJCVYLDJWTWQU-CXLRFSCWSA-N InChi Code: InChI=1S/C21H19Cl2N5O2/c1-13(21-17(22)10-24-11-18(21)23)30-15-3-5-20-16(8-15)19(26-27-20)4-2-14-9-25-28(12-14)6-7-29/h2-5,8-13,29H,6-7H2,1H3,(H,26,27)/b4-2+/t13-/m1/s1 SMILES Code: C[C@H](C1=C(Cl)C=NC=C1Cl)OC2=CC3=C(NN=C3/C=C/C4=CN(CCO)N=C4)C=C2 |
| In Vitro | In vitro activity: In RT-112 cells, HUVECs, KATO-III cells, and SNU-16 cells, LY2874455 inhibits FGF/FGFR-mediated signaling activities. LY2874455 shows FGFR-dependent antiproliferative effects in KMS-11, OPM-2, SNU-16 and KATO-III cells. Kinase Assay: Biochemical filter-binding assays for detection of FGFR phosphorylation activities; Reaction mixtures contains 8 mM Tris-HCl (pH 7.5), 10 mmol/L HEPES, 5 mM dithiothreitol, 10 μM ATP, 0.5 μCi 33P-ATP, 10 mM MnCl2, 150 mM NaCl, 0.01% Triton X-100, 4% dimethyl sulfoxide, 0.05 mg/mL poly(Glu:Tyr) (4:1, average molecular weight of 20–50 kDa), and 7.5, 7.5, and 16 ng of FGFR1, FGFR3, and FGFR4, respectively, and are incubated at room temperature for 30 minutes followed by termination with 10% H3PO4. The reaction mixtures are transferred to 96-well MAFB filter plates that are washed 3 times with 0.5% H3PO4. After air-drying, the plates are read with a Trilux reader. Cell Assay: Cells (2,000 per well) are first grown in RPMI for 6 hours and treated with LY2874455 at 37 ℃ for 3 days. The cells are stained at 37℃ for 4 hours and then solubilized at 37℃ for 1 hour. Finally, the plate is read at 570 nm using a plate reader (Spectra Max Gemini XS). |
|---|---|
| In Vivo | LY2874455 exhibits a potent inhibition of FGF-induced Erk phosphorylation in the heart tissues of mice with TED50 and TED90 values of 1.3 and 3.2 mg/kg, respectively. In mice bearing RT-112, OPM-2 (DSMZ), SNU-16, or NCI-H460 xenograft, LY2874455 (3 mg/kg p.o.) results in dose-dependent inhibition of the tumor growth. |
| Animal model | Mice xenograft bearing RT-112, OPM-2 (DSMZ), SNU-16, or NCI-H460 |
| Formulation & Dosage | Dissolved in 10% Acacia; 3 mg/kg; p.o. |
| References | Mol Cancer Ther. 2011 Nov;10(11):2200-10. |
Inhibition of FGF/FGFR- and VEGF/VEGFR2-mediated signaling activities in cells by LY2874455. Mol Cancer Ther. 2011 Nov;10(11):2200-10. |
Effects of LY2874455 on blood pressure in rats. Mol Cancer Ther. 2011 Nov;10(11):2200-10. |
Efficacy of LY2874455 in different tumor xenograft models. Mol Cancer Ther. 2011 Nov;10(11):2200-10. |
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