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Taladegib

Taladegib (LY2940680) 是smoothened 受体拮抗剂。

CAS号

1258861-20-9

分子式

C26H24F4N6O

主要靶点

Smo|Hedgehog/Smoothened

仅限科研使用

Cat No : CM06472

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Synonyms

LY2940680

验证数据展示

  • CAS No.: 1258861-20-9

    Taladegib
    CAS#: 1258861-20-9

产品信息

Taladegib is an orally bioavailable small molecule antagonist of the Hedgehog (Hh)-ligand cell surface receptor smoothened (Smo) with potential antineoplastic activity.

CAS号 1258861-20-9
分子式 C26H24F4N6O
主要靶点 Smo|Hedgehog/Smoothened
主要通路 G蛋白偶联受体|干细胞
分子量 512.5
纯度 98.75%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 LY2940680

体内活性

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. [2]

体外活性

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. [1]

溶解度

DMSO:5.64 mg/mL (11 mM)

参考文献

1.Redmond EM et al. Expert Opin Investig Drugs, 2011, 20(12),1649-1664.
2.Mark H. Bender, Cancer Research, 2011, Volume 71, Issue 8, Supplement1

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