Ambeed 大中华区 CN | ZH

中文 - ZH English - EN

Ambeed.cn

搜索

关键字搜索批量搜索

首页 收藏 购物车0
首页 /
抑制剂/激动剂
细胞生物学 肿瘤
/
细胞培养
干细胞 肿瘤干细胞
/
类器官培养添加剂
Hedgehog
/ Vismodegib/维莫德吉

Vismodegib/维莫德吉 {[allProObj[0].p_purity_real_show]}

货号：A603143 同义名： GDC-0449

Vismodegib（GDC-0449）是一种口服活性的Hedgehog通路抑制剂，IC50为3 nM。Vismodegib还抑制P-gp和ABCG2，其IC50值分别为3.0 μM和1.4 μM。

Vismodegib/维莫德吉 化学结构 CAS号：879085-55-9
Vismodegib/维莫德吉 化学结构
CAS号：879085-55-9
Vismodegib/维莫德吉 3D分子结构
CAS号：879085-55-9
Vismodegib/维莫德吉 化学结构 CAS号：879085-55-9
Vismodegib/维莫德吉 3D分子结构 CAS号：879085-55-9
规格 价格 会员价 库存 数量
{[ item.pr_size ]}

{[ getRatePriceInt(item.pr_rmb, 1,1) ]}

{[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}

{[ getRatePriceInt(item.pr_rmb, 1,1) ]}

{[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} 		{[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]} 现货 1周 咨询 - +
购物车0 收藏 询单

Vismodegib/维莫德吉 纯度/质量文件 产品仅供科研

货号：A603143 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >

Vismodegib/维莫德吉 生物活性

描述 The Hedgehog (HH) signaling pathway is closely linked to developmental processes, organ patterning, tissue and stem cell maintenance, cell differentiation processes, cell proliferation, regenerative responses after injury and cancer formation[6]. Vismodegib (GDC-0449) is a potent inhibitor of two ABC transporters, ABCG2/BCRP and ABCB1/Pgp, with IC50 values of 1.4 and 3.0 µM, respectively. Additionally, vismodegib can also mildly inhibit ABCC1/MRP1 [7]. In vitro, vismodegib can inhibited cell viability and induce apoptosis in pancreatic cancer cell lines (AsPC-1, PANC-1 and MIA PaCa-2) at 72 hours with IC50 less than 10 μM. Vismodegib-induced apoptosis in cancer cell lines showed increased Fas expression and decreased expression of PDGFRa[8]. After exposed to 50 μM vismodegib for 2 days, survival fraction of HCC and H1339 cells reduced to 60% and 50%, respectively. Ca2+ imaging showed that vismodegib increased [Ca2+](cyto) and reduced endoplasmatic [Ca2+](ER)[1]. When the mouse model of nonalcoholic steatohepatitis was treated with vismodegib (25 mg/kg), TRAIL-mediated liver injury was significantly suppressed and serum ALT and hepatic TUNEL-positive cells were reduced[9].

Vismodegib/维莫德吉 细胞实验

Cell Line
Concentration Treated Time Description References
WM35 melanoma cells 0.5 µM 6 h Vismodegib failed to reduce GLI1 expression, suggesting a crucial role of SMO-independent oncogenic GLI activity in the control of IDO1 expression. Cell Commun Signal. 2025 Feb 17;23(1):91.
DAOY cells 500 nM 5.0 and 15 min To investigate the inhibitory effect of vismodegib on the Hedgehog signaling pathway and its impact on phosphorylation dynamics. Results showed that vismodegib treatment led to activation of Polo-like Kinase 1 and inhibition of Casein Kinase 2A1. Cell Commun Signal. 2020 Jun 23;18(1):99.
POP92 10 µM 7 days To evaluate the effect of Vismodegib on the growth of POP92 cells, results showed that Vismodegib significantly reduced the efficacy of UNC1999. Nat Commun. 2019 Mar 29;10(1):1436.
Mz-ChA-1 cells 10 μM 72 h To evaluate the effect of Vismodegib on cell proliferation, results showed that Vismodegib combined with Rapamycin significantly inhibited cell proliferation Br J Cancer. 2015 Mar 17;112(6):1042-51.
Sk-ChA-1 cells 10 μM 72 h To evaluate the effect of Vismodegib on cell proliferation, results showed that Vismodegib combined with Rapamycin significantly inhibited cell proliferation Br J Cancer. 2015 Mar 17;112(6):1042-51.
hepatoma cells 10 μM 36 h To evaluate the inhibitory effect of Vismodegib on the Hedgehog signaling pathway, results showed that Vismodegib could reverse the stimulatory effects of HMGCR on the stemness and metastasis of hepatoma cells. Genes Dis. 2024 Apr 3;11(5):101285.

Vismodegib/维莫德吉 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Colorectal cancer patient-derived xenograft model Oral gavage 300 mg/kg Once daily for 9 consecutive days, with a 2-day break, for a total of 21 to 25 days To evaluate the effect of UNC1999 on tumour growth, results showed that UNC1999 significantly reduced tumour volume and weight. Nat Commun. 2019 Mar 29;10(1):1436.
Nude mice Mz-ChA-1 xenograft model Oral 100 mg/kg Twice daily for 27 days To evaluate the inhibitory effect of Vismodegib combined with Rapamycin on tumor growth, results showed that the combination treatment significantly inhibited tumor growth Br J Cancer. 2015 Mar 17;112(6):1042-51.
BALB/c nude mice HCC metastatic model Intraperitoneal injection 20 mg/kg Once daily for 7 weeks To evaluate the inhibitory effect of Vismodegib on HCC metastasis, results showed that Vismodegib could suppress HMGCR overexpression-induced HCC metastasis. Genes Dis. 2024 Apr 3;11(5):101285.
Mice Math1-Cre/SmoM2 (M-Smo) mice Intraperitoneal injection 75 mg/kg or 100 mg/kg Once daily for 3 days, then every other day until symptomatic progression Vismodegib initially induced transient tumor regression, but after 2 weeks of treatment, tumor cells began to proliferate again, indicating early resistance to Vismodegib. Nat Commun. 2019 Dec 20;10(1):5829

Vismodegib/维莫德吉 动物研究

Dose Rat: 10 mg/kg - 300 mg/kg[3] (p.o.) Nude Mice: 5 mg/kg - 100 mg/kg[4] (p.o.)
Administration p.o.
Pharmacokinetics
Animal Mice[5] Rats[5] Dogs[5] Monkeys[5]
Dose 1 mg/kg (i.v.)
5 mg/kg (p.o.) 		1 mg/kg (i.v.)
5 mg/kg (p.o.) 		1 mg/kg (i.v.)
2 mg/kg (p.o.) 		1 mg/kg (i.v.)
5 mg/kg (p.o.)
Administration i.v.
p.o. 		i.v.
p.o. 		i.v.
p.o. 		i.v.
p.o.
MRT 1.22 h (i.v.) 1.89 ± 0.508 h (i.v.) 62.3 ± 30.0 h (i.v.) 0.855 ± 0.101 h (i.v.)
F 19.2% (p.o.) 52.9% (p.o.) 32.9% (p.o.) 13.4 ± 2.07% (p.o.)
T1/2 0.976 h (i.v.) 1.32 ± 0.258 h (i.v.) 41.8 ± 19.8 h (i.v.) 0.581 ± 0.0922 h (i.v.)
Tmax 1.00 h (p.o.) 0.667 ± 0.289 h (p.o.) 9.33 ± 12.7 h (p.o.) 2.00 ± 0.00 h (p.o.)
AUCinf 725 ng·h/ml (i.v.)
696 ng·h/ml (p.o.) 		3980 ± 1540 ng·h/ml (i.v.)
10500 ± 3150 ng·h/ml (p.o.) 		60000 ± 26800 ng·h/ml (i.v.)
39400 ± 5800 ng·h/ml (p.o.) 		957 ± 387 ng·h/ml (i.v.)
256 ± 112 ng·h/ml (p.o.)
CL 23.0 ml·min/kg (i.v.) 4.65 ± 1.81 ml·min/kg (i.v.) 0.338 ± 0.203 ml·min/kg (i.v.) 19.3 ± 6.93 ml·min/kg (i.v.)
Cmax 311 ng/ml (p.o.) 2760 ± 1020 ng/ml (p.o.) 591 ± 97.7 ng/ml (p.o.) 162 ± 121 ng/ml (p.o.)
Vss 1.68 L/kg (i.v.) 0.490 ± 0.0653 L/kg (i.v.) 1.03 ± 0.119 L/kg (i.v.) 0.984 ± 0.342 L/kg (i.v.)

Vismodegib/维莫德吉 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03498521 Cancer of Unknown Primary Site Phase 2 Recruiting April 16, 2022 -
NCT03297606 Lymphoma, Non-Hodgkin ... 展开 >> Multiple Myeloma Advanced Solid Tumors 收起 << Phase 2 Recruiting September 2021 Canada, British Columbia ... 展开 >> BCCA - Vancouver Cancer Centre Recruiting Vancouver, British Columbia, Canada, V5Z 4E6 Contact: Daniel John Renouf    604 877-6000 ext 672357       Canada, Ontario London Regional Cancer Program Recruiting London, Ontario, Canada, N6A 5W9 Contact: Stephen Welch    519 685-8640       Ottawa Hospital Research Institute Recruiting Ottawa, Ontario, Canada, K1H 8L6 Contact: John Hilton    613 737-7700 ext 70179       University Health Network Recruiting Toronto, Ontario, Canada, M5G 2M9 Contact: Lillian Siu    416 946-2911       Canada, Quebec The Jewish General Hospital Recruiting Montreal, Quebec, Canada, H3T 1E2 Contact: Cristiano Ferrario    514 398-8307 收起 <<
NCT02788201 Urothelial Carcinoma ... 展开 >> Bladder Cancer Urinary Bladder Neoplasms 收起 << Phase 2 Recruiting July 1, 2020 United States, Maryland ... 展开 >> National Institutes of Health Clinical Center Recruiting Bethesda, Maryland, United States, 20892 Contact: For more information at the NIH Clinical Center contact National Cancer Institute Referral Office    888-624-1937 收起 <<

Vismodegib/维莫德吉 参考文献

[1] Tian F, Schrödl K, Kiefl R, Huber RM, Bergner A. 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

[2]Wong H, Alicke B, 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.

[3]Wong H, Chen JZ, et al. Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide), an orally bioavailable systemic Hedgehog signalling pathway inhibitor. Xenobiotica. 2009 Nov;39(11):850-61.

[4]6:24928

[5]11(1):96-101

[6]Pyczek J, Buslei R, Schult D, Hölsken A, Buchfelder M, Heß I, Hahn H, Uhmann A. Hedgehog signaling activation induces stem cell proliferation and hormone release in the adult pituitary gland. Sci Rep. 2016 Apr 25;6:24928

[7]Zhang Y, Laterra J, Pomper MG. Hedgehog pathway inhibitor HhAntag691 is a potent inhibitor of ABCG2/BCRP and ABCB1/Pgp. Neoplasia. 2009 Jan;11(1):96-101

Vismodegib/维莫德吉 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.87mL

2.37mL

1.19mL

23.74mL

4.75mL

2.37mL

Vismodegib/维莫德吉 技术信息

CAS号879085-55-9
分子式C19H14Cl2N2O3S
分子量 421.3
SMILES Code O=C(NC1=CC=C(Cl)C(C2=NC=CC=C2)=C1)C3=CC=C(S(=O)(C)=O)C=C3Cl
MDL No. MFCD12407408
别名 GDC-0449
运输蓝冰
InChI Key BPQMGSKTAYIVFO-UHFFFAOYSA-N
Pubchem ID 24776445
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C
溶解方案

DMSO: 50 mg/mL(118.68 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 3 mg/mL(7.12 mM)，配合低频超声，并水浴加热至45℃助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: Vismodegib | GDC-0449 | Hedgehog | AmBeed-信号通路专用抑制剂 | Vismodegib/维莫德吉 纯度/质量文件 | Vismodegib/维莫德吉 生物活性 | Vismodegib/维莫德吉 动物研究 | Vismodegib/维莫德吉 临床数据 | Vismodegib/维莫德吉 参考文献 | Vismodegib/维莫德吉 实验方案 | Vismodegib/维莫德吉 技术信息

AmBeed 相关网站 AmBeed.cn AmBeed.com
AmBeed
关于我们
联系我们
资讯中心
网站地图
产品手册
  • 批次文件查询
    • 客户支持
    技术支持
    专业术语
    缩略词释义
    质量手册
    产品咨询
    计算器
    活动政策
    订购方法
    积分商城
    活动声明
    联系我们
    400-920-2911 sales@ambeed.cn tech@ambeed.cn
    AmBeed 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质用途提供服务。

    尊敬的 AmBeed 客户您好，
    请您选择所在区域，我们将转接对应客服为您服务！

    热门区域

    A

    B

    C

    F

    G

    H

    J

    L

    N

    Q

    S

    T

    X

    Y

    Z

    热 A B C F G H J L N Q S T X Y Z