计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 1 篇同行评审文献引用。
概述
Vismodegib (GDC-0449)是一种有效的，新型的，特异性的hedgehog抑制剂，IC50为3 nM。GDC-0449也抑制P-gp作用，IC50为3.0μM。A potent hedgehog (Hh) signaling pathway inhibitor.
Information
Vismodegib (GDC-0449) is a potent, novel and specifichedgehoginhibitor withIC50of 3 nM and also inhibits P-gp withIC50of 3.0 μM in a cell-free assay.
In vitro
GDC-0449 targets the Hedgehog signaling pathway, blocking the activities of the Hedgehog-ligand cell surface receptors PTCH and/or SMO and suppressing Hedgehog signaling. GDC-0449 prevents multiple ATP-binding cassette (ABC) transporters. GDC-0449 also blocks ABCG2, Pgp, and MRP1-important ABC transporters associated with MDR. GDC-0449 is a potent inhibitor of ABC transporters, ABCG2/BCRP and ABCB1/Pgp, and is a mild inhibitor of ABCC1/MRP1. In ABCG2-overexpressing HEK293 cells, GDC-0449 increases retention of the fluorescent ABCG2 substrate BODIPY-prazosin and resensitizes these cells to mitoxantrone. In Madin-Darby canine kidney II cells engineered to overexpress Pgp or MRP1, GDC-0449 increases the retention of calcein-AM and resensitizes them to colchicine. GDC-0449 also resensitizes 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 IC50 values of GDC-0449 for prevention of ABCG2 and Pgp are about 1.4 μM and 3.0 μM, respectively. GDC-0449 alters intracellular Ca2+ homeostasis and inhibits cell growth in cisplatin-resistant lung cancer cells.
In vivo
GDC-0449 has been used to treat medulloblastoma in animal models. GDC-0449 prevents the growth of primary pancreatic xenografts without non-specifically inhibiting pancreatic cell proliferation. Oral dosing of GDC-0449 causes 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 colorectal cancer models, D5123, and 1040830. Analysis of Hh pathway activity and PK/PD modeling reveals that GDC-0449 inhibits Gli1 with a similar IC50 in both the medulloblastoma and D5123 models (0.165 μM and 0.267 μM, respectively). Pathway modulation is linked to efficacy using an integrated PK/PD model revealing a steep relationship where > 50% of the activity of GDC-0449 is associated with >80% repression of the Hh pathway.
Cell Data
cell lines：H2AX cells
Concentrations：20 μM
Incubation Time：2 hours
Powder Purity:≥99%
规格
别名
维斯莫德吉 (GDC-0449)
英文别名
2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Vismodegib (GDC-0449)
生化机理
Vismodegib（GDC-0449）是一种强效、新型和特异性刺猬抑制剂，IC50 为 3 nM，在无细胞试验中还能抑制 P-gp，IC50 为 3.0 μM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
平滑肌同源物抑制剂
名称和识别符
EC号
806-752-3
分子类型
小分子
Isomeric SMILES
CS(=O)(=O)C1=CC(=C(C=C1)C(=O)NC2=CC(=C(C=C2)Cl)C3=CC=CC=N3)Cl
PubChem CID
分子量
421.31
技术文档
高级数据
产品属性
| ALogP | 3.8 |
|---|
关联靶点（人）
SMO
Tclin
平滑同源物(Smoothened homolog)
(16 活性数据)
SHH
Tchem
音猬蛋白(Sonic hedgehog protein)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 57 mg/mL (197.65 mM); Ethanol: 57 mg/mL (197.65 mM); Water: Insoluble;
熔点
168-180°C
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 A2303674 |
分析证书 | V408303 |
技术文档和文章
此产品的引用文献
溶液计算器
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