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Vismodegib

产品编号 T2590 CAS 879085-55-9

别名: Erivedge, GDC-0449, RG 3616, 维莫德吉

Vismodegib (GDC-0449) 是一种刺猬抑制剂，IC50值为 3 nM。它还可抑制 P-gp 和ABCG2的活性，IC50值分别为 3.0 μM 和 1.4 μM。

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Vismodegib, CAS 879085-55-9

规格	价格/CNY	货期
5 mg	￥ 575	现货
10 mg	￥ 897	现货
50 mg	￥ 2,260	现货
100 mg	￥ 3,331	现货
200 mg	￥ 4,195	现货
1 mL * 10 mM (in DMSO)	￥ 575	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	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).
靶点活性	Hedgehog:3 nM (cell free), P-gp:3.0 μM, ABCG2:1.4 μM
体外活性	Vismodegib (GDC-0449) is a potent inhibitor of two ABC transporters, ABCG2/BCRP and ABCB1/Pgp, and is a mild inhibitor of ABCC1/MRP1. In ABCG2-overexpressing HEK293 cells, Vismodegib increased retention of the fluorescent ABCG2 substrate BODIPY-prazosin and resensitized these cells to mitoxantrone, an antineoplastic ABCG2 substrate. Vismodegib also resensitized human non-small cell lung carcinoma cells NCI-H460/par and NCI-H460/MX20, which overexpress ABCG2 in response to mitoxantrone, to mitoxantrone, and to topotecan or SN-38. The IC(50) values of Vismodegib for inhibition of ABCG2 and Pgp were approximately 1.4 and approximately 3.0 μM, respectively [2]. GDC-0449 inhibited cell growth in cisplatin-na?ve and -resistant cells. In both cell types, GDC-0449 increased [Ca(2+)](cyto) and reduced endoplasmatic [Ca(2+)](ER) [3].
体内活性	Oral dosing of vismodegib caused tumor regressions in the Ptch(+/-) allograft model of medulloblastoma at doses ≥25 mg/kg and tumor growth inhibition at doses up to 92 mg/kg dosed twice daily in two ligand-dependent CRC models, D5123, and 1040830. Analysis of Hh pathway activity and PK/PD modeling reveals that vismodegib inhibits Gli1 with a similar IC(50) in both the medulloblastoma and D5123 models (0.165 μmol/L ±11.5% and 0.267 μmol/L ±4.83%, respectively). Pathway modulation was linked to efficacy using an integrated PK/PD model revealing a steep relationship where > 50% of the activity of vismodegib is associated with >80% repression of the Hh pathway [4].
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].

别名	Erivedge, GDC-0449, RG 3616, 维莫德吉
化合物与蛋白结合的复合物	Vismodegib binds to the catalytical domain of human Ubiquitin-Specific Protease 28
分子量	421.3
分子式	C19H14Cl2N2O3S
CAS No.	879085-55-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 78 mg/mL (185.1 mM)

Ethanol: Insoluble

H2O: Insoluble

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3736 mL	11.868 mL	23.7361 mL	59.3401 mL
	5 mM	0.4747 mL	2.3736 mL	4.7472 mL	11.868 mL
	10 mM	0.2374 mL	1.1868 mL	2.3736 mL	5.934 mL
	20 mM	0.1187 mL	0.5934 mL	1.1868 mL	2.967 mL
	50 mM	0.0475 mL	0.2374 mL	0.4747 mL	1.1868 mL
	100 mM	0.0237 mL	0.1187 mL	0.2374 mL	0.5934 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Scales SJ, et al. Mechanisms of Hedgehog pathway activation in cancer and implications for therapy. Trends Pharmacol Sci. 2009 Jun;30(6):303-12. 2. Zhang Y, et al. Hedgehog pathway inhibitor HhAntag691 is a potent inhibitor of ABCG2/BCRP and ABCB1/Pgp. Neoplasia. 2009 Jan;11(1):96-101. 3. Tian F, et al. The hedgehog pathway inhibitor GDC-0449 alters intracellular Ca2+ homeostasis and inhibits cell growth in cisplatin-resistant lung cancer cells. Anticancer Res. 2012 Jan;32(1):89-94. 4. Wong H, et al. Pharmacokinetic-pharmacodynamic analysis of vismodegib in preclinical models of mutational and ligand-dependent Hedgehog pathway activation. Clin Cancer Res. 2011 Jul 15;17(14):4682-92.

文献引用

1. Hu A, Zhang J Z, Wang J, et al. Cholesterylation of Smoothened is a calcium-accelerated autoreaction involving an intramolecular ester intermediate. Cell Research. 2022, 32(3): 288-301. 2. Wu Q, Huang Q, Jiang Y, et al. Remodeling Chondroitin-6-Sulfate–Mediated Immune Exclusion Enhances Anti–PD-1 Response in Colorectal Cancer with Microsatellite Stability. Cancer Immunology Research. 2021 3. Wu Q, Huang Q, Jiang Y, et al. Remodeling Chondroitin-6-Sulfate–Mediated Immune Exclusion Enhances Anti–PD-1 Response in Colorectal Cancer with Microsatellite Stability. Cancer Immunology Research. 2021 4. Wu H, Zhang L, Chen B, et al.B13, a well-tolerated inhibitor of hedgehog pathway, exhibited potent anti-tumor effects against colorectal carcinoma in vitro and in vivo.Bioorganic Chemistry.2023: 106488.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Vismodegib 879085-55-9 Autophagy GPCR/G Protein Membrane transporter/Ion channel Stem Cells Hedgehog/Smoothened ABC GDC0449 Hedgehog Inhibitor RG3616 inhibit Erivedge RG-3616 GDC-0449 RG 3616 GDC 0449 维莫德吉 inhibitor

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Vismodegib

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords