LY2940680

A Smo antagonist

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库存: 现货

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5mg

￥1075.00

860.00

- +
10mg

￥1912.00

1530.00

- +
50mg

￥4212.00

3370.00

- +
200mg

￥12787.00

10230.00

- +

已选 0 种 0 瓶

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货号: ajci15608
CAS: 1258861-20-9
别名: 4-氟-N-甲基-N-[1-[4-(1-甲基-1H-吡唑-5-基)-1-酞嗪基]-4-哌啶基]-2-(三氟甲基)苯甲酰胺,LY2940680
分子式: C26H24F4N6O
分子量: 512.5
纯度: >98%
溶解度: ≥ 51.3mg/mL in DMSO with ultrasonic and warming
储存: Store at -20°C
库存: 现货

Background

LY2940680 is a selective inhibitor of Smo receptor and thus inhibits Hh signaling pathway [1].

Smoothened(Smo) receptor is a member of class F G protein-coupled receptors, which plays an important role in the main transducer of the Hedgehog (Hh) signaling pathway that implicated in a wide range of developmental and adult processes [2].

LY2940680 is a potent Smo receptor inhibitor that binds mostly to extracelluar loops and has a different functioning site with the reported Smo receptor inhibitor SANT-1 which binds to 7TM [2]. 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 [3].

Many studies have shown that Hh signaling pathway plays a pivotal role in CSCs and Hh inhibition caused many aspects of transformation attributed to CSCs. In patients with basal cell carcinoma and medulloblastoma, LY2940680 showed good efficacy as a monotherapy [1].

参考文献:
[1].? Justilien, V. and A.P. Fields, Molecular pathways: novel approaches for improved therapeutic targeting of Hedgehog signaling in cancer stem cells. Clin Cancer Res, 2015. 21(3): p. 505-13.
[2].? Hoch, L., et al., MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor. Faseb j, 2015. 29(5): p. 1817-29.
[3].? Redmond, E.M., et al., Investigational Notch and Hedgehog inhibitors--therapies for cardiovascular disease. Expert Opin Investig Drugs, 2011. 20(12): p. 1649-64.