Sonidegib (Erismodegib, NVP-LDE225)

目录号:S2151

Sonidegib (Erismodegib, NVP-LDE225) Chemical Structure

Molecular Weight(MW): 485.5

Sonidegib (Erismodegib, NVP-LDE225)是一种Smoothened(Smo)拮抗剂,抑制Hedgehog (Hh)信号通路,无细胞试验中IC50分别为1.3 nM (小鼠)和2.5 nM(人)。Phase 3。

规格 价格 库存 购买数量  
RMB 1727.35 现货
RMB 1219.02 现货
RMB 2235.15 现货
RMB 3844.77 现货
RMB 5731.59 现货
有超大折扣

今日订购,明日送达,全国免运费!

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用该产品的3个实验数据:

  • RU-SKI 43 blocks Shh signaling. (a) RU-SKI 43 blocks Gli activation. NIH 3T3 cells were cotransfected with vectors encoding 8× Gli-binding site (GliBS)-Firefly luciferase (unless indicated otherwise), Renilla luciferase reporter (pRL-TK) and Shh. Confluent cells were treated with DMSO, 10 μM LDE225, 10 μM RU-SKI 43 or 10 μM C-2. The firefly luciferase (FL)/Renilla luciferase (RL) ratio in cell lysates was calculated and normalized to that measured in DMSO-treated samples; error bars represent mean ± s.d. (n = 2–3). 

    Nat Chem Biol 2013 9, 247-9. Sonidegib (Erismodegib, NVP-LDE225) purchased from Selleck.

    Western blot analysis on total cell lysates from renal cancer cell lines treated with NVP-LDE225 at different concentrations. Densitometric measurements were normalised to b-actin and reported under western blot images.

    Br J Cancer 2014 111(6), 1168-79. Sonidegib (Erismodegib, NVP-LDE225) purchased from Selleck.

  • NVP-LDE225, everolimus, sunitinib, and their combination interfere with actin and with intracellular organisation of focal adhesion points. Cytoskeleton organisation of 786-O SuR treated with NVP-LDE225 ( 2.5 uM ), everolimus (1 uM ), sunitinib (1 uM ), and their combination for 24 h was analysed by confocal microscopy. Actin-based structures were revealed by rhodaminated phalloidin staining (red fluorescence). Localisation of focal adhesion points was obtained by immunofluorescent staining of p-paxillin (green fluorescence). Merged row images show overlapping of p-paxillin and actin signals. Moreover, all captures were shown in transmitted light. Scale bars, 10 um.

    Br J Cancer 2014 111(6), 1168-79. Sonidegib (Erismodegib, NVP-LDE225) purchased from Selleck.

产品安全说明书

Hedgehog/Smoothened抑制剂选择性比较

生物活性

产品描述 Sonidegib (Erismodegib, NVP-LDE225)是一种Smoothened(Smo)拮抗剂,抑制Hedgehog (Hh)信号通路,无细胞试验中IC50分别为1.3 nM (小鼠)和2.5 nM(人)。Phase 3。
特性 LDE225 是具有高效性和选择性的使平滑的拮抗剂
靶点
Smo (mouse) [1]
(Cell-free assay)
Smo (human) [1]
(Cell-free assay)
1.3 nM 2.5 nM
体外研究

Sonidegib (Erismodegib, NVP-LDE225)可在0.6-0.8μM剂量上抑制1nM-25nM Hh激动剂Ag1.5 处理的TM3荧光报告细胞系。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A2780ip2 Mlj3R5l1d3irY3n0fUBie3OjeR?= NYfydZpvhjFyIN88US=> MULJR|UxRTF{IN88US=> NGjXfYozOjV3M{O1OS=>
A2780cp20 NXTzZZNRS3m2b4jpZ4l1gSCjc4PhfS=> NIHBVVB,OTBizszN NGTsO2FKSzVyPUeuOUDPxE1? MX[yNlU2OzN3NR?=
SKOV3ip1 NH2xV5REgXSxeHnjbZR6KGG|c3H5 NUfNT2Z5hjFyIN88US=> NUDYZ2tGUUN3ME2yOEDPxE1? MnroNlI2PTN|NUW=
SKOV3TRip2 MUPDfZRwgGmlaYT5JIF{e2G7 M3W4eJ4yOCEQvF2= M13aOGlEPTB;MUKg{txO NVjPc2JiOjJ3NUOzOVU>
HeyA8 M{PWcWN6fG:6aXPpeJkh[XO|YYm= NXPMdXV2hjFyIN88US=> NXLTW2dpUUN3ME2xPEDPxE1? NYrDZ5ZiOjJ3NUOzOVU>
HeyA8MDR NUO4W|RIS3m2b4jpZ4l1gSCjc4PhfS=> MVP+NVAh|ryP M3Hy[WlEPTB;ODFOwG0> NFXCXmgzOjV3M{O1OS=>
OS5 M1H4[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIjE[Wp,PSEQvF2= Mk\pdoVlfWOnczD0bIUheHKxbHnm[ZJifGmxbh?= Mk\jNlMzPDN3OUW=
OS18 NU\tbIJkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGf1TXl,PSEQvF2= NGHHXHdz\WS3Y3XzJJRp\SCycn;sbYZmemG2aX;u NUO3[YwzOjN{NEO1PVU>
Glioblastoma initiating cells M1\jeGN6fG:6aXPpeJkh[XO|YYm= NV20TY5lhjFyIN88US=> MYTJcohq[mm2czDD[YxtKF[rYXLpcIl1gQ>? MoOwNlM1QDJ4N{G=
Glioblastoma initiating cells MkTpSpVv[3Srb36gZZN{[Xl? M1K1VJ4yOCEQvF2= MmHHbY5pcWKrdIOgcoV2em:|cHjldoUh\m:{bXH0bY9v M1HZPVI{PDh{Nkex
Glioblastoma initiating cells NEXTSmpEgXSxeHnjbZR6KGG|c3H5 NHXhdpJ,OTBizszN M1f3Rolv\HWlZYOgZZBweHSxc3nz M2nhN|I{PDh{Nkex
Glioblastoma initiating cells NVW3[phRTnWwY4Tpc44h[XO|YYm= MX;+NVAh|ryP MV7kc5dvemWpdXzheIV{KHSqZTDTTGghe2mpbnHsbY5oKHCjdHj3ZZk> M2W2V|I{PDh{Nkex
Glioblastoma initiating cells MlHISpVv[3Srb36gZZN{[Xl? NE\LTnV,OTBizszN NEXGPHpKdmirYnn0d{B1cGViRYjwdoV{e2mxbjDv[kBI\W6nczDJcpZwdH[nZDDpckBO[WmwdHHpcolv\yCSbIXybZBwfGWwY4m= MWCyN|Q5OjZ5MR?=
Glioblastoma initiating cells MofoSpVv[3Srb36gZZN{[Xl? MX;+NVAh|ryP MVHJcohq[mm2czDNc5RqdGm2eTygTY53[XOrb36sJIFv\CCPaXfyZZRqd25? MkXlNlM1QDJ4N{G=
LOX IMVI MXrGeY5kfGmxbjDhd5NigQ>? MojKNVAh|ryP M2nKd2ROW09? NV7pS|Q6cW6qaXLpeJMhUGWmZ3Xoc4cuT0yLIIDheIh4[Xl? MnnhNlM6OzV7MkW=
UACC 257 MmPVSpVv[3Srb36gZZN{[Xl? MWCxNEDPxE1? M4myNmROW09? NYX0XHZDcW6qaXLpeJMhUGWmZ3Xoc4cuT0yLIIDheIh4[Xl? MWiyN|k{PTl{NR?=
LOX IMVI MoHpSpVv[3Srb36gZZN{[Xl? NHK2OYQyOCEQvF2= M2OyZmROW09? MkHtbY5lfWOnczDHNUBk\WyuIHP5Z4xmKGG{cnXzeC=> NWXTc4tFOjN7M{W5NlU>
UACC 257 NXrNOmNKTnWwY4Tpc44h[XO|YYm= M1fIc|ExKM7:TR?= M1;sXWROW09? MlPGbY5lfWOnczDHNUBk\WyuIHP5Z4xmKGG{cnXzeC=> MmTuNlM6OzV7MkW=
LOX IMVI MV3DfZRwgGmlaYT5JIF{e2G7 NGTSeJYyOCEQvF2= NITzTmhFVVOR MWnk[YNz\WG|ZYOgeJVud3JiY3XscEB3cWGkaXzpeJk> MkXINlM6OzV7MkW=
UACC 257 NITHNJNEgXSxeHnjbZR6KGG|c3H5 NWHWSG9zOTBizszN NXLLW4k2TE2VTx?= M2S0UYRm[3KnYYPld{B1fW2xcjDj[YxtKH[rYXLpcIl1gQ>? NEHXcnIzOzl|NUmyOS=>
LOX IMVI NWj5PGFkSXCxcITvd4l{KGG|c3H5 MYmxNEDPxE1? MofuSG1UVw>? MU\pcoR2[2W|IHHwc5B1d3Orcx?= M1ryW|I{QTN3OUK1
UACC 257 NV7TS412SXCxcITvd4l{KGG|c3H5 NVXMWHdDOTBizszN MV\EUXNQ Mn;rbY5lfWOnczDhdI9xfG:|aYO= NGf5TnQzOzl|NUmyOS=>
ACHN MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYXK[ZJshjVizszN NFS5dppFVVOR MYfJR|UxRTJvM,MAje69VQ>? M1\oO|I2ODl|NEmx
769-P Ml;lS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NH:1OVB,PSEQvF2= MYTEUXNQ MXvJR|UxRTJvM,MAje69VQ>? MVmyOVA6OzR7MR?=
786-O MlK5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NH[4RXV,PSEQvF2= Mne0SG1UVw>? MnS5TWM2OD1{LURihKnPxE1? MmTQNlUxQTN2OUG=
786-O SuR NVe4[Jc2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NI[2UIt,PSEQvF2= MUXEUXNQ M{LmbmlEPTB;Mj2z5qCK|ryP Mn;aNlUxQTN2OUG=
SP53 MnHnSpVv[3Srb36gZZN{[Xl? NGnOcIg{OCEQvF2= NWXLSlI4TE2VTx?= MWrpcohq[mm2czDj[YxtKGGmaHXzbY9vKGGwZDDtbYdz[XSrb36= MXmyOlg5PTZyOB?=
SP53 NEf2UJhHfW6ldHnvckBie3OjeR?= NXf3ZlM3OzBizszN MWLEUXNQ MnPObY5pcWKrdIOgeIhmKF[OQUStcYVlcWG2ZXSgSmFMKHOrZ37hcIlv\yCyYYToe4F6 NX[1V5l5OjZ6OEW2NFg>
HS5 M3X5fmZ2dmO2aX;uJIF{e2G7 MX[zNEDPxE1? MnvkSG1UVw>? MVjpcohq[mm2czDj[YxtKGGmaHXzbY9vKGGwZDDtbYdz[XSrb36= MUiyOlg5PTZyOB?=
HS27a Mm\iSpVv[3Srb36gZZN{[Xl? M3HCbVMxKM7:TR?= M3j6bmROW09? NYrzXHN2cW6qaXLpeJMh[2WubDDh[Ihme2mxbjDhcoQhdWmpcnH0bY9v M3;se|I3QDh3NkC4
SP53 NHjOR4lEgXSxeHnjbZR6KGG|c3H5 NILhT4o{OCEQvF2= M{nJPGROW09? NVnnNHFrcW6mdXPld{BifXSxcHjh[5k> MW[yOlg5PTZyOB?=
Jeko M1TvbmN6fG:6aXPpeJkh[XO|YYm= M1q0UFMxKM7:TR?= MYXEUXNQ NGDMc|NqdmS3Y3XzJIF2fG:yaHHnfS=> MYGyOlg5PTZyOB?=

... Click to View More Cell Line Experimental Data

体内研究 Sonidegib (Erismodegib, NVP-LDE225)与小鼠,大鼠以及人源的血浆蛋白有很强的结合能力(>99%),同时与狗和猴子的血浆蛋白有适度的结合,结合能力分别是77 %和 85%。PAMPA 实验证明LDE225能够达到90.8%的渗透性。在梯度稀释的试验中,LDE225在临床物种上显示出很好的口服药效率,其生物药效率在69%到102%之间。LDE225呈弱碱性,pKa只有4.20,同时它的水溶性也相对较弱。LDE225被证明具有剂量依赖的抗肿瘤活性。给药剂量在5 mg/kg/天,一天一次时,LDE225明显抑制肿瘤生长,与33%的T/C值相一致。给药剂量在10 mg/kg/天,一天一次和 20 mg/kg/天,一天一次时,LDE225促使肿瘤退化的效果分别达到51%和83%。Gli1 mRNA抑制性与LDE225介导的肿瘤与血浆接触有关。在肿瘤移植的动物模型中,经过四天的给药处理,LDE225能够成功地穿过血脑屏障导致肿瘤生长受抑制[1]。LDE225能够使Rip1-Tag2小鼠中的肿瘤体积明显减少95.7%。LDE225减少LDE225给药处理小鼠的间质状标志基因的表达[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:

[1]

+ 展开
  • Cell lines: TM3Hh12 细胞
  • Concentrations: 0 μM -10 μM
  • Incubation Time: 30 分钟
  • Method:

    LDE225 用DMSO连续稀释后加入空的分析平板中。TM3Hh12 细胞 (TM3 细胞含有Hh的应答报告基因元件pTA-8xGli-Luc) 用含有5%的马血清,2.5%的胎牛血清(FBS)和15 mM HEPES, pH 7.3的F12 Ham’s/DMEM (1:1)培养基培养。收集细胞时用胰酶消化,然后用含有5%的马血清和15 mM HEPES, pH 7.3的F12 Ham’s/DMEM (1:1)培养基重悬,接着分铺到分析板中。然后加入LDE225在37 °C ,5% CO2的培养箱中大约孵育30分钟。接着加入1 nM 和25 nM 的Ag1.5到分析平板中,37 °C ,5% CO2的条件下培养。48小时后,向平板中加入Bright-Glo 或者 MTS试剂,测量492纳米下的荧光值或者吸收峰。通过MTS法检测Gli-驱动荧光素酶发光或吸光度信号,对浓度取Log(10)值做由非线性回归曲线,确定IC 50值。数据处理使用R统计软件包。


    (Only for Reference)
动物实验:

[1]

+ 展开
  • Animal Models: 采用无胸腺裸小鼠建立原位Ptch+/-p53-/-髓母细胞瘤同种异体移植模型
  • Formulation: 用0.5%纤维素钠配制
  • Dosages: 40 mg/kg/天
  • Administration: 口服,每天两次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 97 mg/mL (199.79 mM)
Ethanol 97 mg/mL warmed (199.79 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+corn oil
10mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 485.5
化学式

C26H26F3N3O3

CAS号 956697-53-3
稳定性 powder
in solvent
别名

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01787552 Completed Primary Myelofibrosis|Thrombocythemia Essential|Thrombocytosis|Myeloproliferative Disorders|Bone Marrow Diseases|Hematologic Diseases|Blood Coagulation Disorders|Blood Platelet Disorders|Hemorrhagic Disorders Novartis Pharmaceuticals|Novartis May 8 2013 Phase 1|Phase 2
NCT01708174 Completed Medulloblastoma Novartis Pharmaceuticals|Novartis May 6 2013 Phase 2
NCT01327053 Completed Basal Cell Carcinoma Novartis Pharmaceuticals|Novartis June 29 2011 Phase 2
NCT02254551 Terminated Multiple Myeloma SCRI Development Innovations LLC|Novartis January 2015 Phase 2
NCT02195973 Completed Recurrent Ovarian Cancer University of Alabama at Birmingham|Novartis Pharmaceuticals September 2014 Phase 1
NCT02182622 Unknown status Prostate Cancer Martin Gutierrez|Novartis|Hackensack Meridian Health July 2014 Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

Hedgehog/Smoothened Signaling Pathway Map

Hedgehog/Smoothened Inhibitors with Unique Features

相关Hedgehog/Smoothened产品

Tags: 购买Sonidegib (Erismodegib, NVP-LDE225) | Sonidegib (Erismodegib, NVP-LDE225)供应商 | 采购Sonidegib (Erismodegib, NVP-LDE225) | Sonidegib (Erismodegib, NVP-LDE225)价格 | Sonidegib (Erismodegib, NVP-LDE225)生产 | 订购Sonidegib (Erismodegib, NVP-LDE225) | Sonidegib (Erismodegib, NVP-LDE225)代理商
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID