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Zamaporvint
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Zamaporvint
CAS No. : 1900754-56-4
MCE 站:Zamaporvint
产品活性:Zamaporvint (RXC004) 是一种具有口服活性的选择性 Wnt 抑制剂。Zamaporvint 靶向膜结合邻酰基转移酶 Porcupine 并抑制 Wnt 配体棕榈酰化、分泌和通路激活。Zamaporvint 显示出良好的药代动力学特征,并在依赖 Wnt 配体的结直肠和胰腺细胞系中显示出强效的抗增殖作用。Zamaporvint 具有多种抗肿瘤机制,可用于癌症研究。是是
研究领域:Stem Cell/Wnt | Metabolic Enzyme/Protease
作用靶点:Wnt | Acyltransferase | Porcupine
In Vitro: Zamaporvint (300 nM, 48 h) treatment of L- wnt3a cells reduce the ability of conditioned medium to activate the β-catenin-responsive luciferase reporter gene in a concentration-dependent manner, with an IC50 of 64 pM, and the addition of recombinant Wnt3a restore the luciferase activity, suggesting no effect on downstream Wnt signaling.
The effect of Zamaporvint (100 nM, 24 hr) on proliferation reflects a concentration-dependent downregulation of c-Myc mRNA. Reduced the proportion of cells in S phase and strongly suppressed the expression of the mitotic marker phospho-histone-H3 in cells with abnormal upstream components of the Wnt pathway, indicative of cell cycle arrest, and was found to have reduced immunosuppression at the same dose as after administration Sexual support .
Zamaporvint (20 μM, 18 h) in plasma across species ranged from 2.5% to 7.5%, microsomal CLint values ranged from 3.9 to 31.6 μL/min?mg, with mouse having the lowest and dog the highest predicted clearances, rodents and humans display low clearance.
Zamaporvint (10 μM, 2 h) has good intrinsic permeability, showing some evidence of efflux in MDR1-MDCKII cells but not in Caco-2 cells.
In Vivo: Zamaporvint (1.5 mg/kg or 5 mg/kg orally twice daily, or 5 mg/kg Zamaporvint orally once daily, for 28 days) reduces in tumor growth, and inhibition of Wnt-responsive gene expression including cMyc, was observed in the Wnt liganddependent SNU-1411, AsPC1, and HPAFII models, and no effected tumor growth in the Wnt ligandindependent HCT116 xenograft mode.
Zamaporvint (1.5 mg/kg, 5 mg/kg, once daily) reduces Ki67-positive cells in the total tumor area, and its effect is more pronounced in differentiated tumor areas, and by inhibiting immune evasion in the B16F10 "cold" tumor model Antitumor effect .
Zamaporvint (1.5 or 5 mg/kg once daily) stimulates host tumor immunity, reduces resident myeloid-derived suppressor cells within B16F10 tumors and synergizing with anti-programmed cell death protein-1 (PD-1, HY-P73361) to increase CD8+/regulatory T cell ratios within CT26 tumors.
Pharmacokinetic Parameters of Zamaporvint in Mice.
species | Dose (i.v./p.o., mg/kg) | Cmax (p.o., μM) | C24 h (p.o., μM) | AUCinf (p.o., μM.h) | Cl (mL/min/kg) | Vss (L/kg) | F (p.o., %) | T1/2 (hr) |
mouse | 2/5 | 7.6 | 0.002 | 33.9 | 2.9 | 0.40 | 48 | 1.8 |
rat | 2/5 | 3.6 | 0.009 | 10.5 | 5.8 | 0.64 | 31 | 2.5 |
dog | 2/5 | 10.4 | 0.012 | 8.6 | 8.9 | 0.39 | 137 | 0.8 |
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