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LY2940680 Sale

(Synonyms: 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) 目录号 : GC15683

A Smo antagonist

LY2940680 Chemical Structure

Cas No.:1258861-20-9

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5mg
¥882.00
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10mg
¥1,586.00
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50mg
¥3,528.00
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200mg
¥10,773.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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].

References:
[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.

Chemical Properties

Cas No. 1258861-20-9 SDF
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
化学名 4-fluoro-N-methyl-N-[1-[4-(2-methylpyrazol-3-yl)phthalazin-1-yl]piperidin-4-yl]-2-(trifluoromethyl)benzamide
Canonical SMILES CN1C(=CC=N1)C2=NN=C(C3=CC=CC=C32)N4CCC(CC4)N(C)C(=O)C5=C(C=C(C=C5)F)C(F)(F)F
分子式 C26H24F4N6O 分子量 512.5
溶解度 ≥ 51.3mg/mL in DMSO with ultrasonic and warming 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 1.9512 mL 9.7561 mL 19.5122 mL
5 mM 0.3902 mL 1.9512 mL 3.9024 mL
10 mM 0.1951 mL 0.9756 mL 1.9512 mL
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