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Taladegib(LY2940680)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Taladegib(LY2940680)图片
CAS NO:1258861-20-9
规格:≥98%
包装与价格:
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

产品介绍
理化性质和储存条件
Molecular Weight (MW)512.5
FormulaC26H24F4N6O
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 infoChemical 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
SynonymsLY2940680, LY 2940680, LY-2940680
实验参考方法
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 VivoLY2940680 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
ReferencesExpert Opin Investig Drugs. 2011 Dec;20(12):1649-64.