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Sonidegib

別名: NVP-LDE225, Erismodegib 中文名稱:索尼德吉

Sonidegib是一種Smoothened(Smo)拮抗劑,抑制Hedgehog (Hh)信號通路,無細胞試驗中IC50分別為1.3 nM (小鼠)和2.5 nM(人)。Phase 3。

Sonidegib Chemical Structure

Sonidegib Chemical Structure

CAS: 956697-53-3

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 794.43 現(xiàn)貨
5mg 647.01 現(xiàn)貨
25mg 1941.03 現(xiàn)貨
100mg 4832.1 現(xiàn)貨
1g 24488.1 現(xiàn)貨
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Sonidegib相關(guān)產(chǎn)品

相關(guān)信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
UACC 257 Function assay 10 μM inhibits Hedgehog-GLI pathway 23935925
LOX IMVI Function assay 10 μM inhibits Hedgehog-GLI pathway 23935925
Glioblastoma initiating cells Function assay ~10 μM Inhibits Motility, Invasion, and Migration 23482671
Glioblastoma initiating cells Function assay ~10 μM Inhibits the Expression of Genes Involved in Maintaining Pluripotency 23482671
Glioblastoma initiating cells Function assay ~10 μM downregulates the SHH signaling pathway 23482671
Glioblastoma initiating cells Cytoxicity assay ~10 μM induces apoptosis 23482671
Glioblastoma initiating cells Function assay ~10 μM inhibits neurosphere formation 23482671
Glioblastoma initiating cells Cytoxicity assay ~10 μM Inhibits Cell Viability 23482671
OS18 Growth inhibitory assay ~5 μM reduces the proliferation 23243595
OS5 Growth inhibitory assay ~5 μM reduces the proliferation 23243595
HeyA8MDR Cytoxicity assay ~10 μM IC50=8 μM 22553355
HeyA8 Cytoxicity assay ~10 μM IC50=18 μM 22553355
SKOV3TRip2 Cytoxicity assay ~10 μM IC50=12 μM 22553355
SKOV3ip1 Cytoxicity assay ~10 μM IC50=24 μM 22553355
A2780cp20 Cytoxicity assay ~10 μM IC50=7.5 μM 22553355
A2780ip2 Cytoxicity assay ~10 μM IC50=12 μM 22553355
LOX IMVI Function assay 10 μM induces G1 cell cycle arrest 23935925
UACC 257 Function assay 10 μM induces G1 cell cycle arrest 23935925
LOX IMVI Cytoxicity assay 10 μM decreases tumor cell viability 23935925
UACC 257 Cytoxicity assay 10 μM decreases tumor cell viability 23935925
LOX IMVI Apoptosis assay 10 μM induces apoptosis 23935925
UACC 257 Apoptosis assay 10 μM induces apoptosis 23935925
ACHN Growth inhibitory assay ~5 μM IC50=2-3?μM 25093491
769-P Growth inhibitory assay ~5 μM IC50=2-3?μM 25093491
786-O Growth inhibitory assay ~5 μM IC50=2-3?μM 25093491
786-O SuR Growth inhibitory assay ~5 μM IC50=2-3?μM 25093491
SP53 Function assay 30 μM inhibits cell adhesion and migration 26885608
SP53 Function assay 30 μM inhibits the VLA4-mediated FAK signaling pathway 26885608
HS5 Function assay 30 μM inhibits cell adhesion and migration 26885608
HS27a Function assay 30 μM inhibits cell adhesion and migration 26885608
SP53 Cytoxicity assay 30 μM induces autophagy 26885608
Jeko Cytoxicity assay 30 μM induces autophagy 26885608
U2OS Function assay 2 hrs Displacement of [3H]cyclopamine from wild type Smo expressed in U2OS cells after 2 hrs by scintillation counting, Ki = 0.006 μM. 23063522
NIH/3T3 Function assay 24 hrs Inhibition of hedgehog signaling pathway in mouse NIH/3T3 cells measured after 24 hrs by Gli-dual luciferase reporter gene assay, IC50 = 0.006 μM. 27810591
TM3 Function assay 48 hrs Inhibition of Hh signaling pathway in mouse TM3 cells assessed as downregulation of Gli1 gene expression after 48 hrs by luciferase reporter gene assay, EC50 = 0.0012 μM. 26976215
NIH3T3 Function assay 48 hrs Inhibition of SHH signaling pathway in mouse NIH3T3 cells measured after 48 hrs by Gli-luciferase reporter assay, IC50 = 0.0055 μM. 24176396
NIH3T3 Function assay 48 hrs Inhibition of Sonic-induced hedgehog signalling in mouse NIH3T3 cells after 48 hrs by Gli-luciferase reporter assay, IC50 = 0.0055 μM. 26820554
NIH/3T3 Function assay Inhibition of hedgehog signaling pathway in mouse NIH/3T3 cells expressing wild type Smo assessed as reduction in Gli mRNA expression by RT-PCR method, IC50 = 0.0044 μM. 27810591
NIH/3T3 Function assay Inhibition of hedgehog signaling pathway in mouse NIH/3T3 cells harboring Smo D477H mutant assessed as reduction in Gli mRNA expression by RT-PCR method, IC50 = 0.0227 μM. 27810591
NIH/3T3 Function assay Inhibition of hedgehog signaling pathway expressed in mouse NIH/3T3 cells assessed as inhibition of hedgehog-induced Gli-2 accumulation at tip of primary cilia by DAPI staining based confocal microscopic analysis 27810591
NIH/3T3 Function assay Inhibition of hedgehog signaling pathway in mouse NIH/3T3 cells assessed as inhibition of hedgehog-induced Smo-EGFP ciliary translocation by DAPI staining based confocal microscopic analysis 27810591
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
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生物活性

產(chǎn)品描述 Sonidegib是一種Smoothened(Smo)拮抗劑,抑制Hedgehog (Hh)信號通路,無細胞試驗中IC50分別為1.3 nM (小鼠)和2.5 nM(人)。Phase 3。
特性 LDE225 是具有高效性和選擇性的使平滑的拮抗劑
靶點
Smo (mouse) [1]
(Cell-free assay)
Smo (human) [1]
(Cell-free assay)
1.3 nM 2.5 nM
體外研究(In Vitro)
體外研究活性 Sonidegib (Erismodegib, NVP-LDE225)可在0.6-0.8μM劑量上抑制1nM-25nM Hh激動劑Ag1.5 處理的TM3熒光報告細胞系。[1]
細胞實驗 細胞系 TM3Hh12 細胞
濃度 0 μM -10 μM
孵育時間 30 分鐘
方法

LDE225 用DMSO連續(xù)稀釋后加入空的分析平板中。TM3Hh12 細胞 (TM3 細胞含有Hh的應(yīng)答報告基因元件pTA-8xGli-Luc) 用含有5%的馬血清,2.5%的胎牛血清(FBS)和15 mM HEPES, pH 7.3的F12 Ham’s/DMEM (1:1)培養(yǎng)基培養(yǎng)。收集細胞時用胰酶消化,然后用含有5%的馬血清和15 mM HEPES, pH 7.3的F12 Ham’s/DMEM (1:1)培養(yǎng)基重懸,接著分鋪到分析板中。然后加入LDE225在37 °C ,5% CO2的培養(yǎng)箱中大約孵育30分鐘。接著加入1 nM 和25 nM 的Ag1.5到分析平板中,37 °C ,5% CO2的條件下培養(yǎng)。48小時后,向平板中加入Bright-Glo 或者 MTS試劑,測量492納米下的熒光值或者吸收峰。通過MTS法檢測Gli-驅(qū)動熒光素酶發(fā)光或吸光度信號,對濃度取Log(10)值做由非線性回歸曲線,確定IC 50值。數(shù)據(jù)處理使用R統(tǒng)計軟件包。

實驗圖片 檢測方法 檢測指標(biāo) 實驗圖片 PMID
Western blot

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