ZW4864 free base

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ZW4864 (free base) 是一种具有口服活性和选择性的 β catenin/ B-Cell lymphoma 9 蛋白-蛋白相互作用 (β catenin/BCL9 PPI) 抑制剂。ZW4864 (free base) 抑制 β catenin/BCL9 PPI 的 Ki 值为 0.76 μM，IC50 值为 0.87 μM。

ZW4864 (free base) is an orally active and selective β catenin/B-Cell lymphoma 9 protein?protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 (free base) inhibits β catenin/BCL9 PPI with a Ki value of 0.76 μM and an IC50 value of 0.87 μM.

Western Blot Analysis Cell Line:SW480 and MBA-MD-231 cells Concentration:10~40 μM Incubation Time:24 hours Result:Decreased the expression levels of Axin2 and cyclin D1 proteins.Apoptosis Analysis Cell Line:MDA-MB231, MCF10A and MDA-MB-468 cells Concentration:10~40 μM Incubation Time:72 hours Result:Selectively triggered rapid apoptosis of triple-negative breast cancer cells with hyperactive β-catenin signaling while sparing normal mammary epithelial MCF10A cells.RT-PCR Cell Line:SW480 and MBA-MD-231 cells Concentration:10~40 μ Incubation Time:24 hours Result:Suppressed the transcription of β-catenin target genes in a concentration-dependent manner without affecting the expression of HPRT, a house-keeper gene, in both SW480 and Wnt 3a-activated MDA-MB-231 cells.

Animal Model:C57BL/6 mice Dosage:20 mg/kg (Pharmacokinetic Analysis)Administration:P.o.Result:Exhibited good pharmacokinetic properties with an oral bioavailability (F) of 83%.Animal Model:Mice Dosage:90 mg/kg Administration:P.o.Result:Showed a variation in tumor growth in mice.

——

Wnt/Notch/Hedgehog

Wnt/beta/catenin

Wnt/beta-catenin

——

——

2632259-92-6

570.72

C33H42N6O3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (175.22 mM; 超声助溶 )

CC(C)(Oc1cccc(c1)N1CCC[C@H](C1)C(=O)N(Cc1ccc(cc1)-c1cn[nH]c1)C1CC1)C(=O)N1CCNCC1

——

(-20℃)

With Ice Pack

≥ 2 years