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LGK-974

LGK-974 Structure
LGK-974
LGK-974 Property
  • Melting point 176 - 180°C
  • Boiling point 650.9±55.0 °C(Predicted)
  • Density 1.268±0.06 g/cm3(Predicted)
  • storage temp. Refrigerator
  • solubility Chloroform (Slightly), Methanol (Slightly)
  • pka 12.24±0.70(Predicted)
  • form Solid
  • color White to Off-White
  • FDA UNII U27F40013Q
  • UNSPSC Code 12352200
  • NACRES NA.77
Safety
  • HS Code  :2933399990
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal word
  • Hazard statements
  • Precautionary statements
LGK-974 Price More Price(1)
  • Brand: Sigma-Aldrich(India)
  • Product number: 5.31091
  • Product name : Porcn Inhibitor IV, LGK974 - CAS 1243244-14-5 - Calbiochem
  • Purity: A cell-permeable inhibitor of Wnt secretion from L-cell Wnt1/2/3/3a/6/7a/9a transfectants (IC?? from 50 pM to 1.1 nM).
  • Packaging: 5MG
  • Price: ₹20010
  • Updated: 2022/06/14
  • Buy: Buy

LGK-974 Chemical Properties,Usage,Production

  • Description Porcupine (PORCN) is a membrane bound O-acyltransferase that mediates palmitoylation of Wnt family proteins. This step is required for secretion and biologic activity of Wnt proteins, which have roles in embryonic development and cancer. LGK974 is a potent and specific small molecule inhibitor of PORCN (IC50 = 0.4 nM). It greatly reduces Wnt secretion without decreasing its synthesis and without increasing cytotoxicity. LGK974 is orally bioavailable in mice and induces tumor regression in mouse breast tumors produced by mammary tumor virus-driven Wnt1 signaling. It also blocks carcinogenesis in other Wnt-related tumors at doses that have limited impact on stem cell renewal.
  • Uses LGK 974 is a potent and specific small molecule Porcupine (PORCN) inhibitor.
  • Definition ChEBI: LGK974 is a carboxamide, the structure of which is that of acetamide substituted on carbon by a 2',3-dimethyl-2,4'-bipyridin-5-yl group and on nitrogen by a 5-(pyrazin-2-yl)pyridin-2-yl group. It is a highly potent, selective and orally bioavailable Porcupine inhibitor (a Wnt signalling inhibitor). It has a role as a Wnt signalling inhibitor. It is a member of bipyridines, a member of pyrazines, a member of pyridines and a secondary carboxamide. It is functionally related to an acetamide.
  • in vivo

    LGK974, a drug that targets Porcupine, a Wnt-specific acyltransferase. LGK974 potently inhibits Wnt signaling, has strong efficacy in rodent tumor models, and is well-tolerated. Toxicology studies are performed on nontumor bearing rats at 3 and 20 mg/kg. At the efficacious dose of 3 mg/kg per day for 14 d, LGK974 is well-tolerated without abnormal histopathological findings in Wnt-dependent tissues, including the intestine, stomach, and skin. When rats are administrated a very high dose of 20 mg/kg per day for 14 d, loss of intestinal epithelium is observed, consistent with the concept that Wnt is required for intestinal tissue homeostasis[1].

  • target PORCN
  • References [1] liu j, pan s, hsieh mh, ng n, sun f, wang t, kasibhatla s, schuller ag, li ag, cheng d, li j, tompkins c, pferdekamper a, steffy a, cheng j, kowal c, phung v, guo g, wang y, graham mp, flynn s, brenner jc, li c, villarroel mc, schultz pg, wu x, mcnamara p, sellers wr, petruzzelli l, boral al, seidel hm, mclaughlin me, che j, carey te, vanasse g, harris jl. targeting wnt-driven cancer through the inhibition of porcupine by lgk974. proc natl acad sci u s a. 2013 dec 10;110(50):20224-9.
LGK-974 Preparation Products And Raw materials
Raw materials
Preparation Products
LGK-974 Suppliers
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LGK-974 Spectrum
1243244-14-5, LGK-974Related Search:
  • Inhibitors
  • 抑制剂
  • 化工试剂
  • 合成有机化合物配体
  • 细胞生物学试剂
  • 小分子抑制剂
  • 小分子抑制剂，天然产物
  • 243244-14-5
  • 化合物LGK-974,10 MM DMSO 溶液
  • 乙酰胺杂质LGK(乙酰胺杂质43)
  • 2-(2',3-二甲基-[2,4'-联吡啶]-5-基)-N-(5-(吡嗪-2-基)吡啶-2-基)乙酰胺
  • 7'-二氯荧光素二乙酸酯
  • NOVARTIS诺华
  • MK-0991, L-743872
  • 2-(2,3-二甲基-[2,4-联吡啶]-5-基)-N-(5-(吡嗪-2-基)吡啶-2-基)醋胺石
  • PORCUPINE抑制剂(LGK974)
  • 2',3-二甲基-N-[5-(2-吡嗪基)-2-吡啶基]-[2,4'-联吡啶]-5-乙酰胺
  • 1243244-14-5
  • Porcn Inhibitor IV, LGK974
  • LGK974, 10 mM in DMSO
  • Acotiamide Impurity LGK or Acotiamide Impurity 43
  • 2 ', 3-dimethyl-N - [5- (2-pyrazinyl) -2-pyridyl] - [2,4' - bipyridine] -5-acetamide
  • Acotiamide Impurity LGK（Acotiamide Impurity 43）
  • CS-1102
  • LGK974; LGK-974
  • 2-(2',3-Dimethyl-2,4'-bipyridin-5-yl)-N-[5-(2-pyrazinyl)-2-pyridi nyl]acetamide
  • 2-(2',3-Dimethyl-[2,4'-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide hydrochloride
  • LGK974; LGK 974; NVP-LGK974
  • WNT-974
  • LGK974 (WNT974)
  • LGK-974 USP/EP/BP
  • 2-[5-methyl-6-(2-methylpyridin-4-yl)pyridin-3-yl]-N-(5-pyrazin-2-ylpyridin-2-yl)acetamide
  • 7'-Dichlorodihydrofluorescein diacetate
  • LGK-974 2',3-Dimethyl-N-[5-(2-pyrazinyl)-2-pyridinyl]-[2,4'-bipyridine]-5-acetamide
  • NVP-LGK974
  • [2,4'-Bipyridine]-5-acetamide, 2',3-dimethyl-N-[5-(2-pyrazinyl)-2-pyridinyl]-
  • 2',3-Dimethyl-N-[5-(2-pyrazinyl)-2-pyridinyl]-[2,4'-bipyridine]-5-acetamide
  • 2-(2',3-diMethyl-[2,4'-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetaMide
  • LGK-974
  • 2-[5-Methyl-6-(2-methyl-4-pyridyl)-3-pyridyl]-N-(5-pyrazin-2-yl-2-pyridyl)acetamide
  • LGK974(NVP-LGK974)

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