1243244-14-5 Good S...

1243244-14-5 Good Supplier In China 1243244-14-5 on hot selling 1243244-14-5 LGK-974
1243244-14-5 Good Supplier In China 1243244-14-5 on hot selling 1243244-14-5 LGK-974

1243244-14-5 Good Supplier In China 1243244-14-5 on hot selling 1243244-14-5 LGK-974

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1 Gram

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  • Min.Order :1 Gram
  • Purity: 98%
  • Payment Terms : T/T,Other

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1243244-14-5 Good Supplier In China 1243244-14-5 on hot selling 1243244-14-5 LGK-974

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  • Appearance:Powder
  • Application:Scientific research
  • PackAge:As required
  • ProductionCapacity:1000|Gram|Week
  • Storage:keep sealed and keep from direct light
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1243244-14-5 Good Supplier In China on hot selling LGK-974

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.

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

Details:

Alternate Name 2-(2',3-dimethyl-[2,4'-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide
Appearance Crystalline solid
CAS # 1243244-14-5
Molecular Formula C??H??N?O
Molecular Weight 396.44
Purity ≥98% by HPLC
Solubility DMSO (~ 35 mg/ml)
SMILES CC1=C(N=CC(=C1)CC(=O)NC2=NC=C(C=C2)C3=NC=CN=C3)C4=CC(=NC=C4)C
InChi InChI=1S/C23H20N6O/c1-15-9-17(12-28-23(15)18-5-6-25-16(2)10-18)11-22(30)29-21-4-3-19(13-27-21)20-14-24-7-8-26-20/h3-10,12-14H,11H2,1-2H3,(H,27,29,30)
InChi Key XXYGTCZJJLTAGH-UHFFFAOYSA-N
PubChem CID 46926973
Handling Protect from air and light
Storage Conditions -20°C
Shipping Conditions Gel Pack
USAGE For Research Use Only! Not For Use in Humans.

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