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。

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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 NV;NV|N6S3m2b4jpZ4l1gSCjc4PhfS=> NH;acpp,OTBizszN M36zW2lEPTB;MUKg{txO M3v2U|IzPTV|M{W1
A2780cp20 M3\Md2N6fG:6aXPpeJkh[XO|YYm= NIjNfJB,OTBizszN NF;OTnpKSzVyPUeuOUDPxE1? NGnP[WIzOjV3M{O1OS=>
SKOV3ip1 NWDGXlRXS3m2b4jpZ4l1gSCjc4PhfS=> NX7xXYhChjFyIN88US=> MUnJR|UxRTJ2IN88US=> M1jIbVIzPTV|M{W1
SKOV3TRip2 M4O5XWN6fG:6aXPpeJkh[XO|YYm= M{PLWp4yOCEQvF2= MmnSTWM2OD1zMjFOwG0> NGTlUpAzOjV3M{O1OS=>
HeyA8 NELmenBEgXSxeHnjbZR6KGG|c3H5 M1zq[J4yOCEQvF2= Moi4TWM2OD1zODFOwG0> MX6yNlU2OzN3NR?=
HeyA8MDR NEW4b4hEgXSxeHnjbZR6KGG|c3H5 NVPNRVc5hjFyIN88US=> M1mwb2lEPTB;ODFOwG0> MVeyNlU2OzN3NR?=
OS5 MVHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXP+OUDPxE1? MljGdoVlfWOnczD0bIUheHKxbHnm[ZJifGmxbh?= MYmyN|I1OzV7NR?=
OS18 M1m2N2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXL+OUDPxE1? NIjwSFdz\WS3Y3XzJJRp\SCycn;sbYZmemG2aX;u MYGyN|I1OzV7NR?=
Glioblastoma initiating cells NX7YfWN2S3m2b4jpZ4l1gSCjc4PhfS=> M{DIcZ4yOCEQvF2= NF[zNo9KdmirYnn0d{BE\WyuIG\pZYJqdGm2eR?= NHzpVGEzOzR6Mk[3NS=>
Glioblastoma initiating cells MorsSpVv[3Srb36gZZN{[Xl? Ml7aglExKM7:TR?= NF[0NohqdmirYnn0d{Bv\XW{b4PwbIVz\SCob4LtZZRqd25? NVLiZo8xOjN2OEK2O|E>
Glioblastoma initiating cells NXP1NItGS3m2b4jpZ4l1gSCjc4PhfS=> M2rj[54yOCEQvF2= M4rT[olv\HWlZYOgZZBweHSxc3nz MUKyN|Q5OjZ5MR?=
Glioblastoma initiating cells NIXZR2pHfW6ldHnvckBie3OjeR?= MWP+NVAh|ryP MVTkc5dvemWpdXzheIV{KHSqZTDTTGghe2mpbnHsbY5oKHCjdHj3ZZk> MWGyN|Q5OjZ5MR?=
Glioblastoma initiating cells MnflSpVv[3Srb36gZZN{[Xl? MnXxglExKM7:TR?= MlXkTY5pcWKrdIOgeIhmKEW6cILld5Nqd25ib3[gS4Vv\XNiSX72c4x3\WRiaX6gUYFqdnSjaX7pcochWGy3cnnwc5RmdmO7 MnflNlM1QDJ4N{G=
Glioblastoma initiating cells NUjYUndPTnWwY4Tpc44h[XO|YYm= MWL+NVAh|ryP NIfqPHVKdmirYnn0d{BOd3SrbHn0fUwhUW64YYPpc44tKGGwZDDNbYdz[XSrb36= NXvJfWc6OjN2OEK2O|E>
LOX IMVI MXzGeY5kfGmxbjDhd5NigQ>? M2fqO|ExKM7:TR?= NXrNcWJtTE2VTx?= M2fiWIlvcGmkaYTzJGhm\GenaH;nMWdNUSCyYYToe4F6 NEDsNZUzOzl|NUmyOS=>
UACC 257 MmPESpVv[3Srb36gZZN{[Xl? M13Pe|ExKM7:TR?= MUfEUXNQ MmXJbY5pcWKrdIOgTIVl\2Wqb3etS2xKKHCjdHj3ZZk> NEKxN3YzOzl|NUmyOS=>
LOX IMVI MVPGeY5kfGmxbjDhd5NigQ>? M3W2fFExKM7:TR?= MXrEUXNQ MWLpcoR2[2W|IFexJINmdGxiY4njcIUh[XK{ZYP0 NV7vbZhjOjN7M{W5NlU>
UACC 257 MmflSpVv[3Srb36gZZN{[Xl? MYexNEDPxE1? M{f5WmROW09? MWPpcoR2[2W|IFexJINmdGxiY4njcIUh[XK{ZYP0 NWTY[JNxOjN7M{W5NlU>
LOX IMVI MkL1R5l1d3irY3n0fUBie3OjeR?= NFnTXlIyOCEQvF2= M2TuSWROW09? MUjk[YNz\WG|ZYOgeJVud3JiY3XscEB3cWGkaXzpeJk> NYr1cWEyOjN7M{W5NlU>
UACC 257 M322PWN6fG:6aXPpeJkh[XO|YYm= M4X1NFExKM7:TR?= NHOwcW9FVVOR NXHMR4x4\GWlcnXhd4V{KHS3bX;yJINmdGxidnnhZoltcXS7 MlHPNlM6OzV7MkW=
LOX IMVI NGTWclFCeG:ydH;zbZMh[XO|YYm= NEnl[nAyOCEQvF2= Mni3SG1UVw>? M2nINYlv\HWlZYOgZZBweHSxc3nz MnfBNlM6OzV7MkW=
UACC 257 Ml7ERZBweHSxc3nzJIF{e2G7 M4XZfVExKM7:TR?= MUfEUXNQ Mkn3bY5lfWOnczDhdI9xfG:|aYO= NFLKRYwzOzl|NUmyOS=>
ACHN M3juT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmC1glUh|ryP Mn;4SG1UVw>? M2nIbmlEPTB;Mj2z5qCK|ryP NXf4cJRDOjVyOUO0PVE>
769-P NHfLUI5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkHqglUh|ryP M3rIOmROW09? NXu4XGp{UUN3ME2yMVPjiIoQvF2= NXjPcGJ2OjVyOUO0PVE>
786-O NYH3d|YzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUH4[XpMhjVizszN NWHRSm5kTE2VTx?= M4TuN2lEPTB;Mj2z5qCK|ryP MnzhNlUxQTN2OUG=
786-O SuR NUXNcYJ5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVP+OUDPxE1? NFHtXmdFVVOR MnXGTWM2OD1{LURihKnPxE1? MmHQNlUxQTN2OUG=
SP53 NV7VcYNpTnWwY4Tpc44h[XO|YYm= MontN|Ah|ryP MXLEUXNQ NHrwNZBqdmirYnn0d{Bk\WyuIHHkbIV{cW:wIHHu[EBucWe{YYTpc44> NH\3R3gzPjh6NU[wPC=>
SP53 M{mxZmZ2dmO2aX;uJIF{e2G7 M3\HPVMxKM7:TR?= MV3EUXNQ M2TNXolvcGmkaYTzJJRp\SCYTFG0MY1m\GmjdHXkJGZCUyC|aXfuZYxqdmdicHH0bJdigQ>? Mkf5NlY5QDV4MEi=
HS5 NFfnNVZHfW6ldHnvckBie3OjeR?= M4HOc|MxKM7:TR?= NFnSWVNFVVOR NV;Fb2RpcW6qaXLpeJMh[2WubDDh[Ihme2mxbjDhcoQhdWmpcnH0bY9v MWOyOlg5PTZyOB?=
HS27a NEXJTldHfW6ldHnvckBie3OjeR?= MYezNEDPxE1? M1\mXWROW09? NHfpOI9qdmirYnn0d{Bk\WyuIHHkbIV{cW:wIHHu[EBucWe{YYTpc44> MknlNlY5QDV4MEi=
SP53 NEj4e4lEgXSxeHnjbZR6KGG|c3H5 MXKzNEDPxE1? MYjEUXNQ MXrpcoR2[2W|IHH1eI9xcGGpeR?= NH6zcYUzPjh6NU[wPC=>
Jeko M{jkVGN6fG:6aXPpeJkh[XO|YYm= NHTGOXM{OCEQvF2= M4DxemROW09? M3\IT4lv\HWlZYOgZZV1d3CqYXf5 NV;mT4FSOjZ6OEW2NFg>

... 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:
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
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 Active, not recruiting 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
NCT02254551 Terminated Multiple Myeloma SCRI Development Innovations, LLC|Novartis January 2015 Phase 2
NCT02138929 Recruiting Esophageal Cancer M.D. Anderson Cancer Center|Novartis|National Cancer Institute (NCI) November 2014 Phase 1
NCT02195973 Active, not recruiting Recurrent Ovarian Cancer University of Alabama at Birmingham|Novartis Pharmaceuticals September 2014 Phase 1
NCT02151864 Recruiting Hepatocellular Carcinoma|Cirrhosis Jason K. Sicklick, M.D.|Novartis Pharmaceuticals|University of California, San Diego July 2014 Phase 1
NCT02182622 Unknown status Prostate Cancer Martin Gutierrez|Novartis|Hackensack University Medical Center July 2014 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID