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Selleck该产品发表文献12篇:

客户使用该产品的3个实验数据:

  • 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.

  • 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.

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 MkPpR5l1d3irY3n0fUBie3OjeR?= NUOxTXRVhjFyIN88US=> NUnoTIZnUUN3ME2xNkDPxE1? MV:yNlU2OzN3NR?=
A2780cp20 NUn2UGFRS3m2b4jpZ4l1gSCjc4PhfS=> NYLpbFZOhjFyIN88US=> MnLxTWM2OD15LkWg{txO NVHzXmhFOjJ3NUOzOVU>
SKOV3ip1 M{X6[WN6fG:6aXPpeJkh[XO|YYm= MnnLglExKM7:TR?= MW\JR|UxRTJ2IN88US=> NVHtd5dXOjJ3NUOzOVU>
SKOV3TRip2 Mk[3R5l1d3irY3n0fUBie3OjeR?= MofrglExKM7:TR?= MX\JR|UxRTF{IN88US=> MXuyNlU2OzN3NR?=
HeyA8 NGnicW5EgXSxeHnjbZR6KGG|c3H5 MV\+NVAh|ryP MYjJR|UxRTF6IN88US=> NEjueHgzOjV3M{O1OS=>
HeyA8MDR NWLabIJkS3m2b4jpZ4l1gSCjc4PhfS=> MW\+NVAh|ryP NXL2T29EUUN3ME24JO69VQ>? MlzYNlI2PTN|NUW=
OS5 MkT2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml:2glUh|ryP MlXjdoVlfWOnczD0bIUheHKxbHnm[ZJifGmxbh?= NWrRUpJ1OjN{NEO1PVU>
OS18 NV;ucGJOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NUfD[|NFhjVizszN NVXYOoZbemWmdXPld{B1cGVicILvcIln\XKjdHnvci=> MX2yN|I1OzV7NR?=
Glioblastoma initiating cells NX32NmhES3m2b4jpZ4l1gSCjc4PhfS=> MXX+NVAh|ryP NHG5TXRKdmirYnn0d{BE\WyuIG\pZYJqdGm2eR?= NGnVRoQzOzR6Mk[3NS=>
Glioblastoma initiating cells M4nzZWZ2dmO2aX;uJIF{e2G7 MoXsglExKM7:TR?= NE\o[IhqdmirYnn0d{Bv\XW{b4PwbIVz\SCob4LtZZRqd25? Mne2NlM1QDJ4N{G=
Glioblastoma initiating cells MnyzR5l1d3irY3n0fUBie3OjeR?= NX;6cJA2hjFyIN88US=> M4XvV4lv\HWlZYOgZZBweHSxc3nz MUCyN|Q5OjZ5MR?=
Glioblastoma initiating cells M{XhcmZ2dmO2aX;uJIF{e2G7 MYT+NVAh|ryP NHywTohld3ewcnXneYxifGW|IITo[UBUUEhic3nncoFtcW6pIIDheIh4[Xl? M3jCUFI{PDh{Nkex
Glioblastoma initiating cells NF;1WoxHfW6ldHnvckBie3OjeR?= NWLDO5BPhjFyIN88US=> Ml\uTY5pcWKrdIOgeIhmKEW6cILld5Nqd25ib3[gS4Vv\XNiSX72c4x3\WRiaX6gUYFqdnSjaX7pcochWGy3cnnwc5RmdmO7 M4rjWFI{PDh{Nkex
Glioblastoma initiating cells NFGySmVHfW6ldHnvckBie3OjeR?= MUL+NVAh|ryP M2fNNmlvcGmkaYTzJG1wfGmuaYT5MEBKdn[jc3nvckwh[W6mIF3p[5JifGmxbh?= NV3wUpZlOjN2OEK2O|E>
LOX IMVI NYDRd|U5TnWwY4Tpc44h[XO|YYm= M1;4dlExKM7:TR?= Mk\4SG1UVw>? MofVbY5pcWKrdIOgTIVl\2Wqb3etS2xKKHCjdHj3ZZk> NX\U[llDOjN7M{W5NlU>
UACC 257 NWn1dpJDTnWwY4Tpc44h[XO|YYm= M1jpbVExKM7:TR?= NUflfGV3TE2VTx?= NGO5VHVqdmirYnn0d{BJ\WSpZXjv[{1IVElicHH0bJdigQ>? MXqyN|k{PTl{NR?=
LOX IMVI M3TVSWZ2dmO2aX;uJIF{e2G7 MY[xNEDPxE1? M2XLOmROW09? MXLpcoR2[2W|IFexJINmdGxiY4njcIUh[XK{ZYP0 NYLMfotkOjN7M{W5NlU>
UACC 257 NWHIUpF3TnWwY4Tpc44h[XO|YYm= NYr2NWxlOTBizszN NVPqeGpSTE2VTx?= MmfxbY5lfWOnczDHNUBk\WyuIHP5Z4xmKGG{cnXzeC=> NIrDUnUzOzl|NUmyOS=>
LOX IMVI NETT[JVEgXSxeHnjbZR6KGG|c3H5 MV6xNEDPxE1? NEW1bXVFVVOR MVfk[YNz\WG|ZYOgeJVud3JiY3XscEB3cWGkaXzpeJk> M1vS[FI{QTN3OUK1
UACC 257 MVPDfZRwgGmlaYT5JIF{e2G7 M3y4NFExKM7:TR?= NIDuWFJFVVOR NH3MdnBl\WO{ZXHz[ZMhfHWvb4KgZ4VtdCC4aXHibYxqfHl? M2HyNVI{QTN3OUK1
LOX IMVI MYfBdI9xfG:|aYOgZZN{[Xl? MUWxNEDPxE1? MVXEUXNQ MXjpcoR2[2W|IHHwc5B1d3Orcx?= NXfmXGJpOjN7M{W5NlU>
UACC 257 MVnBdI9xfG:|aYOgZZN{[Xl? NVXIR|NYOTBizszN NVTz[pNQTE2VTx?= NFr0TGJqdmS3Y3XzJIFxd3C2b4Ppdy=> NIPqblMzOzl|NUmyOS=>
ACHN M3S1XGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NImzUVJ,PSEQvF2= NUL6R4M3TE2VTx?= MkTFTWM2OD1{LURihKnPxE1? NVXvO2lyOjVyOUO0PVE>
769-P NGflXJJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M130Np42KM7:TR?= Mk\ySG1UVw>? MXrJR|UxRTJvM,MAje69VQ>? NF7LTZYzPTB7M{S5NS=>
786-O MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmjRglUh|ryP MWnEUXNQ MUfJR|UxRTJvM,MAje69VQ>? NYTPfFI3OjVyOUO0PVE>
786-O SuR M36zbmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEH6[5l,PSEQvF2= M33uOmROW09? M4rxW2lEPTB;Mj2z5qCK|ryP NXXmPYhrOjVyOUO0PVE>
SP53 M4f3UGZ2dmO2aX;uJIF{e2G7 MU[zNEDPxE1? NIjISZZFVVOR NYLlZndOcW6qaXLpeJMh[2WubDDh[Ihme2mxbjDhcoQhdWmpcnH0bY9v MnLNNlY5QDV4MEi=
SP53 NILpS|ZHfW6ldHnvckBie3OjeR?= M4mzTlMxKM7:TR?= MmLoSG1UVw>? M{fBNIlvcGmkaYTzJJRp\SCYTFG0MY1m\GmjdHXkJGZCUyC|aXfuZYxqdmdicHH0bJdigQ>? NIjNRpczPjh6NU[wPC=>
HS5 NFO2[WRHfW6ldHnvckBie3OjeR?= MlPoN|Ah|ryP NEHMdVBFVVOR NIrae2NqdmirYnn0d{Bk\WyuIHHkbIV{cW:wIHHu[EBucWe{YYTpc44> MkHmNlY5QDV4MEi=
HS27a MkmySpVv[3Srb36gZZN{[Xl? Ml3oN|Ah|ryP M{TNV2ROW09? MojtbY5pcWKrdIOgZ4VtdCCjZHjld4lwdiCjbnSgcYloemG2aX;u NEHIOoczPjh6NU[wPC=>
SP53 M1PpeWN6fG:6aXPpeJkh[XO|YYm= M1XGOlMxKM7:TR?= M2nQUWROW09? MXPpcoR2[2W|IHH1eI9xcGGpeR?= MYSyOlg5PTZyOB?=
Jeko MXXDfZRwgGmlaYT5JIF{e2G7 NV3Jbm1uOzBizszN MmjOSG1UVw>? NXr6d21DcW6mdXPld{BifXSxcHjh[5k> M334e|I3QDh3NkC4

... 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
NCT02254551 Terminated Multiple Myeloma SCRI Development Innovations LLC|Novartis January 2015 Phase 2
NCT02254551 Terminated Multiple Myeloma SCRI Development Innovations LLC|Novartis January 2015 Phase 2
NCT02138929 Active not recruiting Esophageal Cancer M.D. Anderson Cancer Center|Novartis|National Cancer Institute (NCI) November 10 2014 Phase 1
NCT02138929 Active not recruiting Esophageal Cancer M.D. Anderson Cancer Center|Novartis|National Cancer Institute (NCI) November 10 2014 Phase 1
NCT02195973 Completed Recurrent Ovarian Cancer University of Alabama at Birmingham|Novartis Pharmaceuticals September 2014 Phase 1
NCT02195973 Completed Recurrent Ovarian Cancer University of Alabama at Birmingham|Novartis Pharmaceuticals September 2014 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID