Zamaporvint,1900754-56-4

价格￥2400 - 3800

品牌MedChemExpress(MCE)
产地美国
货号HY-153855
更新日期2025年12月05日

MedChemExpress LLC

品牌商

14 年钻石会员

规格：	10 mM * 1 mL	产品价格：	￥2640.0
规格：	5 mg	产品价格：	￥2400.0
规格：	10 mg	产品价格：	￥3800.0

Zamaporvint

CAS No. : 1900754-56-4

MCE 国际站：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 CL_int 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 ligand–dependent SNU-1411, AsPC1, and HPAFII models, and no effected tumor growth in the Wnt ligand–independent 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)	C_max (p.o., μM)	C_{24 h} (p.o., μM)	AUC_inf (p.o., μM.h)	Cl (mL/min/kg)	V_ss (L/kg)	F (p.o., %)	T_1/2 (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