| CAS NO: | 1258861-20-9 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| Molecular Weight (MW) | 512.5 |
|---|---|
| Formula | C26H24F4N6O |
| CAS No. | 1258861-20-9 (free base); |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 5 mg/mL (9.8 mM) |
| Water:<1 mg/mL | |
| Ethanol: 2 mg/mL (3.9 mM) | |
| Other info | Chemical Name: 4-fluoro-N-methyl-N-(1-(4-(1-methyl-1H-pyrazol-5-yl)phthalazin-1-yl)piperidin-4-yl)-2-(trifluoromethyl)benzamide InChi Key: SZBGQDXLNMELTB-UHFFFAOYSA-N InChi Code: InChI=1S/C26H24F4N6O/c1-34(25(37)20-8-7-16(27)15-21(20)26(28,29)30)17-10-13-36(14-11-17)24-19-6-4-3-5-18(19)23(32-33-24)22-9-12-31-35(22)2/h3-9,12,15,17H,10-11,13-14H2,1-2H3 SMILES Code: O=C(N(C)C1CCN(C2=NN=C(C3=CC=NN3C)C4=C2C=CC=C4)CC1)C5=CC=C(F)C=C5C(F)(F)F |
| Synonyms | LY2940680, LY 2940680, LY-2940680 |
| In Vitro | In vitro activity: LY2940680 inhibits cancer growth in cell lines containing a mutation in the gene encoding Smoothened that researchers had previously observed in patient with cancer who developed resistance to vismodegib. Kinase Assay: Taladegib, a small-molecule antagonist of the smoothened receptor, shows a slight inhibitory effect on cell proliferation without differences between mucin- (IC50: Taladegib=49.8±4.5 μM) and mixed- Cholangiocarcinoma (CCA) (IC50: Taladegib=61.2±21.1 μM). Cell Assay: When tested with cell lines containing a mutation in the gene encoding Smoothened that researchers had previously observed in patient with cancer who developed resistance to vismodegib, LY2940680 inhibited cell proliferation. |
|---|---|
| In Vivo | LY2940680 has excellent pharmacokinetic properties in rodent and non-rodent species. LY2940680 administrated orally treats Ptch+/- p53-/- transgenic mice which spontaneously develop medulloblastoma, produces remarkable efficacy and significantly improves their survival. LY2940680 reveals rapid kinetics of anti-tumor activity through magnetic resonance imaging of these mice, and LY2940680 induces Caspase-3 activity and reduces proliferation by immunohistochemistry analysis of medulloblastoma tumors. LY2940680 inhibits Hh regulated gene expression in the subcutaneous xenograft tumor stroma and produces significant anti-tumor activity. |
| Animal model | Mice |
| Formulation & Dosage | Oral |
| References | Expert Opin Investig Drugs. 2011 Dec;20(12):1649-64. |
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