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基本描述
| 规格或纯度 | 99% |
|---|---|
| 英文名称 | ZW4864 free base |
| 生化机理 | 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 K i value of 0.76 μM and an IC 50 value of 0.87 μM. |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
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 K i value of 0.76 μM and an IC 50 value of 0.87 μM In Vitro ZW4864 (10~40 μM; 24 hours; SW480 and MBA-MD-231 cells) (free base) decreases the expression levels of Axin2 and cyclin D1 proteins. ZW4864 (10~40 μM; 72 hours; MDA-MB231, MCF10A and MDA-MB-468 cells) (free base) selectively triggeres rapid apoptosis of triple-negative breast cancer cells with hyperactive β-catenin signaling while sparing normal mammary epithelial MCF10A cells. ZW4864 (10~40 μM; 24 hours; SW480 and MBA-MD-231 cells) (free base) suppresses 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. ZW4864 (free base) binds with β-catenin and selectively disrupts the protein?protein interaction (PPI) between B-cell lymphoma 9 (BCL9) and β-catenin while sparing the β-catenin/E-cadherin PPI. ZW4864 (free base) dose-dependently suppresses β-catenin signaling activation, downregulates oncogenic β-catenin target genes, and abrogates invasiveness of β-catenin-dependent cancer cells. ZW4864 (free base) suppresses TOPFlash luciferase activities in β-catenin expressing HEK293 cells in a dose-dependent manner with an IC 50 of 11 μM. ZW4864 (free base) also dose-dependently suppresses the TOPFlash luciferase activities in SW480 and Wnt 3a-activated MDA-MB-468 cells with the IC 50 s of 7.0 and 6.3 μM, respectively. ZW4864 (free base) selectively suppresses transactivation of β-catenin signaling. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell 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 AnalysisCell 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-PCRCell Line: SW480 and MBA-MD-231 cells Concentration: 10~40 μM 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. In Vivo ZW4864 (20 mg/kg; p.o.) (free base) exhibits good pharmacokinetic properties with an oral bioavailability (F) of 83 % . ZW4864 (90 mg/kg; p.o.) (free base) shows a variation in tumor growth in mice . ZW4864 (free base) shows good pharmacokinetic properties and effectively suppresses β-catenin target gene expression in the patient-derived xenograft mouse model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Form:Solid IC50& Target:IC50: 0.87 μM (β catenin/BCL9 PPI),Ki: 0.76 μM (β catenin/BCL9 PPI) |
名称和标识符
| Canonical SMILES | O=C([C@H]1CN(C2=CC=CC(OC(C)(C)C(N3CCNCC3)=O)=C2)CCC1)N(C4CC4)CC5=CC=C(C6=CNN=C6)C=C5 |
|---|---|
| 分子量 | 570.72 |
化学和物理性质
| 溶解性 | DMSO : 100 mg/mL (175.22 mM; Need ultrasonic) |
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