品牌	貨號	產(chǎn)品規(guī)格	價格(RMB)	庫存（上海）	北京	武漢	南京
源葉(MedMol)	S80215-5mg	98%	￥700.00元	6	-	-	-
源葉(MedMol)	S80215-10mg	98%	￥1200.00元	2	-	-	-
源葉(MedMol)	S80215-50mg	98%	￥3900.00元	1	-	-	-

產(chǎn)品介紹

LGK974 (WNT974) is an orally bioavailable and specific Porcupine (PORCN) inhibitor with an IC50 of 0.1 nM

產(chǎn)品描述： LGK974 (WNT974) is an orally bioavailable and specific Porcupine (PORCN) inhibitor with an IC50 of 0.1 nM

靶點： Porcupine

體外研究：
LGK974 effectively displaces [3H]-GNF-1331 with an IC50 of 1 nM in the PORCN radioligand binding assay. LGK974 potently reduces Wnt-dependent AXIN2 mRNA levels in HN30 cells with an IC50 of 0.3 nM.

體內(nèi)研究：
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.

參考文獻：
1. Liu J, et al. 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. 2. Tammela T, et al. A Wnt-producing niche drives proliferative potential and progression in lung adenocarcinoma. Nature. 2017 May 18;545(7654):355-359.

溶解性： soluble in DMSO

保存條件： -20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.522 ml	12.612 ml	25.224 ml
5 mM	0.504 ml	2.522 ml	5.045 ml
10 mM	0.252 ml	1.261 ml	2.522 ml
50 mM	0.05 ml	0.252 ml	0.504 ml

注意：

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參考文獻

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