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

货号：A603143 同义名： GDC-0449 Ambeed 开学季，买赠积分，赢豪礼

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 化学结构 CAS号：879085-55-9
Vismodegib 化学结构
CAS号：879085-55-9
Vismodegib 3D分子结构
CAS号：879085-55-9
Vismodegib 化学结构 CAS号：879085-55-9
Vismodegib 3D分子结构 CAS号：879085-55-9
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Vismodegib 纯度/质量文件 产品仅供科研

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Vismodegib 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 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
23132-87 Growth Inhibition Assay IC50=4.40147 μM SANGER
8505C Growth Inhibition Assay IC50=25.6331 μM SANGER
A101D Growth Inhibition Assay IC50=44.8023 μM SANGER
A172 Growth Inhibition Assay IC50=37.4921 μM SANGER

Vismodegib 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 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 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 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 技术信息

CAS号879085-55-9
分子式C19H14Cl2N2O3S
分子量 421.297
别名 GDC-0449
运输蓝冰
存储条件

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度

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
动物实验配方

5% DMSO+40% PEG 300+5% Tween 80+50% water 12.5 mg/mL

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

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