维莫德吉|T2590

Vismodegib
879085-55-9

￥575 5mg 起订

￥897 10mg 起订

￥2260 50mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 维莫德吉

英文名称：: Vismodegib

CAS号：: 879085-55-9

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.99%

产品类别：: 抑制剂

货号：: T2590

Product Introduction

Bioactivity

名称	Vismodegib
描述	Vismodegib (GDC-0449) is a hedgehog pathway inhibitor (IC50: 3 nM). It also inhibits P-gp (IC50: 3.0 μM), ABCG2 (IC50: 1.4 μM).
细胞实验	MDCKII cells were plated into 24-well plates at a density of 3 x 10^5 cells per well and were allowed to attach. The medium was then changed to that containing different drugs (50 μM VP, 50 μM indomethacin, or 20 μM Vismodegib) in DMSO or DMSO alone as control, and nonfluorescent calcein-AM was added to a final concentration of 1.0 μM and incubated at 37°C for 2 hours. Cells were then washed twice with Ca2+, Mg2+-containing Hank's balanced salt solution buffer and lysed by shaking in 0.01% Triton X-100 in PBS buffer for 1 hour at room temperature or overnight at 4°C. The lysate was then transferred into 96-well plates, and the fluorescence signal caused by the cell-derived calcein was quantified spectrophotometrically with a SpectraMax M5 Multi-Detection Reader using an excitation wavelength of 495 nm and an emission wavelength of 515 nm. All manipulations were performed in the dark. All readings are expressed as mean ± SEM normalized to the control [2].
动物实验	Female CD-1 nude mice (weighing 25–28 g) were administered oral doses of 5, 15, 50, and 100 mg/kg (free base equivalent) of vismodegib hydrochloride salt in 0.5% methylcellulose/0.2% Tween 80 (MCT). Blood samples (～1 mL) were collected up to 24 hours postdose via cardiac puncture (terminal collection) into tubes containing potassium ethylenediaminetetraacetic acid (K2EDTA) anticoagulant. Immediately on the collection, the blood was mixed with K2EDTA and stored on ice. Within 30 minutes, blood samples were centrifuged at approximately 1000 to 1500 × g for 5 minutes at 4°C, and plasma was harvested. The plasma samples were stored at ?80°C until analysis. Concentrations of vismodegib were determined by LC/MS/MS as described previously [4].
体外活性	Vismodegib (GDC-0449) 是针对两种ABC转运蛋白，ABCG2/BCRP 和 ABCB1/Pgp 的强效抑制剂，并对 ABCC1/MRP1 表现出温和的抑制作用。在过表达ABCG2 的HEK293细胞中，Vismodegib 增加了荧光ABCG2底物BODIPY-prazosin的保留，并使这些细胞重新对抗肿瘤药物mitoxantrone敏感。此外，Vismodegib 还使过表达ABCG2的人类非小细胞肺癌细胞 NCI-H460/par 和 NCI-H460/MX20 对mitoxantrone、topotecan 或 SN-38 重新敏感。Vismodegib 抑制ABCG2 和 Pgp 的IC(50) 值分别约为1.4 μM 和约3.0 μM [2]。在对顺铂敏感和耐药的细胞中，GDC-0449 均抑制了细胞生长。在这两种细胞类型中，GDC-0449 增加了[Ca(2+)](cyto) 并减少了内质网中的[Ca(2+)](ER) [3]。
体内活性	经口给予vismodegib在Ptch(+/-)同种异体移植的小脑髓质瘤模型中，当剂量≥25 mg/kg时可引起肿瘤退缩。在两种配体依赖的CRC模型D5123和1040830中，vismodegib剂量高达92 mg/kg并每日两次给药时可抑制肿瘤生长。通过分析Hh通路活性和PK/PD建模显示，vismodegib在这两种模型中抑制Gli1的IC(50)相似（分别为0.165 μmol/L ±11.5%和0.267 μmol/L ±4.83%）。该路径调控与疗效的关联通过一个整合的PK/PD模型揭示，其中vismodegib活性> 50%与Hh路径>80%的抑制呈陡峭关系[4]。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 50 mg/mL (118.68 mM) Ethanol : Insoluble H2O : Insoluble
关键字	GDC0449 \| Hedgehog \| Inhibitor \| RG3616 \| Vismodegib \| inhibit \| RG-3616 \| Autophagy \| GDC 0449
相关产品	Guanidine hydrochloride \| Naringin \| Valproic Acid \| Taurine \| Gefitinib \| Aceglutamide \| Hydroxychloroquine \| Curcumin \| Stavudine \| Salicylic acid \| Paeonol \| Sodium 4-phenylbutyrate
相关库	抑制剂库 \| 抗癌上市药物库 \| EMA 上市药物库 \| 抗衰老化合物库 \| 离子通道库 \| FDA 上市药物库 \| 抗癌临床化合物库

维莫德吉|||RG 3616|||GDC-0449|||Erivedge|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子