Sonidegib (NVP-LDE225)

For research use only. Not for use in humans.

目录号:S2151 别名: Erismodegib

Sonidegib (NVP-LDE225) Chemical Structure

CAS No. 956697-53-3

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  
10mM (1mL in DMSO) 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
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客户使用Selleck生产的Sonidegib (NVP-LDE225)发表文献34篇:

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 MVXDfZRwgGmlaYT5JIF{e2G7 MUP+NVAh|ryP MlrhTWM2OD1zMjFOwG0> NULTTHJPOjJ3NUOzOVU>
A2780cp20 NXLOO2tMS3m2b4jpZ4l1gSCjc4PhfS=> M2nVU54yOCEQvF2= M{nKZWlEPTB;Nz61JO69VQ>? NXLPU|g1OjJ3NUOzOVU>
SKOV3ip1 MkHQR5l1d3irY3n0fUBie3OjeR?= NIHvfG1,OTBizszN NVXaV|lVUUN3ME2yOEDPxE1? MVKyNlU2OzN3NR?=
SKOV3TRip2 NX:4bZB3S3m2b4jpZ4l1gSCjc4PhfS=> MkH4glExKM7:TR?= M2fzdmlEPTB;MUKg{txO M1e5clIzPTV|M{W1
HeyA8 MUDDfZRwgGmlaYT5JIF{e2G7 M4jI[Z4yOCEQvF2= M13MbWlEPTB;MUig{txO MX[yNlU2OzN3NR?=
HeyA8MDR NUm1c3IzS3m2b4jpZ4l1gSCjc4PhfS=> NEWycW1,OTBizszN NFzReJFKSzVyPUig{txO NHO4boQzOjV3M{O1OS=>
OS5 MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1LDNZ42KM7:TR?= NEnaNZdz\WS3Y3XzJJRp\SCycn;sbYZmemG2aX;u NFL1TnIzOzJ2M{W5OS=>
OS18 NWDGXlRUT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXLZXoVHhjVizszN NFXwXHVz\WS3Y3XzJJRp\SCycn;sbYZmemG2aX;u MnXXNlMzPDN3OUW=
Glioblastoma initiating cells Mn3wR5l1d3irY3n0fUBie3OjeR?= Mn7JglExKM7:TR?= MkDKTY5pcWKrdIOgR4VtdCCYaXHibYxqfHl? MnuxNlM1QDJ4N{G=
Glioblastoma initiating cells M1X5cWZ2dmO2aX;uJIF{e2G7 NHGy[Gt,OTBizszN MVHpcohq[mm2czDu[ZVzd3OyaHXy[UBnd3KvYYTpc44> MWSyN|Q5OjZ5MR?=
Glioblastoma initiating cells MnjqR5l1d3irY3n0fUBie3OjeR?= NUWyTGo{hjFyIN88US=> M2C5dYlv\HWlZYOgZZBweHSxc3nz MV2yN|Q5OjZ5MR?=
Glioblastoma initiating cells NHHRSWFHfW6ldHnvckBie3OjeR?= MV3+NVAh|ryP NVy5fFhO\G:5boLl[5Vt[XSnczD0bIUhW0iKIIPp[45idGmwZzDwZZRpf2G7 NUS1XG11OjN2OEK2O|E>
Glioblastoma initiating cells MmHOSpVv[3Srb36gZZN{[Xl? NV3zSGZzhjFyIN88US=> NWLQdG01UW6qaXLpeJMhfGinIFX4dJJme3Orb36gc4YhT2WwZYOgTY53d2y4ZXSgbY4hVWGrboThbY5qdmdiUHz1dolxd3SnbnP5 NVf3e|RROjN2OEK2O|E>
Glioblastoma initiating cells M1PLSmZ2dmO2aX;uJIF{e2G7 MlnxglExKM7:TR?= M{PTbWlvcGmkaYTzJG1wfGmuaYT5MEBKdn[jc3nvckwh[W6mIF3p[5JifGmxbh?= NGPl[m4zOzR6Mk[3NS=>
LOX IMVI M3LMNWZ2dmO2aX;uJIF{e2G7 NFj3UVgyOCEQvF2= NWC4[WszTE2VTx?= NGHBRWFqdmirYnn0d{BJ\WSpZXjv[{1IVElicHH0bJdigQ>? NX;kbXZqOjN7M{W5NlU>
UACC 257 NWnHXoFVTnWwY4Tpc44h[XO|YYm= NIjPXm0yOCEQvF2= MVXEUXNQ NInkRWRqdmirYnn0d{BJ\WSpZXjv[{1IVElicHH0bJdigQ>? NEfsO5EzOzl|NUmyOS=>
LOX IMVI M3ra[2Z2dmO2aX;uJIF{e2G7 MnfvNVAh|ryP MlHzSG1UVw>? NHmzc5lqdmS3Y3XzJGcyKGOnbHygZ5lkdGViYYLy[ZN1 MX:yN|k{PTl{NR?=
UACC 257 NF3WT4lHfW6ldHnvckBie3OjeR?= NE\OdFUyOCEQvF2= MoDISG1UVw>? MmXwbY5lfWOnczDHNUBk\WyuIHP5Z4xmKGG{cnXzeC=> MXSyN|k{PTl{NR?=
LOX IMVI M1\C[mN6fG:6aXPpeJkh[XO|YYm= M4Ttd|ExKM7:TR?= MnO3SG1UVw>? MXHk[YNz\WG|ZYOgeJVud3JiY3XscEB3cWGkaXzpeJk> NH\YXpMzOzl|NUmyOS=>
UACC 257 MofSR5l1d3irY3n0fUBie3OjeR?= MVOxNEDPxE1? NWfhWWhETE2VTx?= M{LoU4Rm[3KnYYPld{B1fW2xcjDj[YxtKH[rYXLpcIl1gQ>? NVTT[ml5OjN7M{W5NlU>
LOX IMVI NUfOWHpHSXCxcITvd4l{KGG|c3H5 M1\1VFExKM7:TR?= NWK1RpRrTE2VTx?= MX;pcoR2[2W|IHHwc5B1d3Orcx?= M3XhXFI{QTN3OUK1
UACC 257 M4TNVWFxd3C2b4Ppd{Bie3OjeR?= NFuyZVYyOCEQvF2= MUjEUXNQ MorFbY5lfWOnczDhdI9xfG:|aYO= MWKyN|k{PTl{NR?=
ACHN M33VVmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFXmWWZ,PSEQvF2= MUTEUXNQ M3vCSWlEPTB;Mj2z5qCK|ryP NYjoO5VTOjVyOUO0PVE>
769-P MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3fVRp42KM7:TR?= MoizSG1UVw>? MWPJR|UxRTJvM,MAje69VQ>? Mn\pNlUxQTN2OUG=
786-O M1LQdWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUjMWJA1hjVizszN MUDEUXNQ Mk\YTWM2OD1{LURihKnPxE1? MYKyOVA6OzR7MR?=
786-O SuR M2HMOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2DBdZ42KM7:TR?= MU\EUXNQ NHHVbZRKSzVyPUKtN-KBkc7:TR?= MomxNlUxQTN2OUG=
SP53 MkHvSpVv[3Srb36gZZN{[Xl? NYnrR|dCOzBizszN MkDXSG1UVw>? NGD0[|BqdmirYnn0d{Bk\WyuIHHkbIV{cW:wIHHu[EBucWe{YYTpc44> MorNNlY5QDV4MEi=
SP53 MoD1SpVv[3Srb36gZZN{[Xl? NF;FdmU{OCEQvF2= NVv1[WJmTE2VTx?= MYHpcohq[mm2czD0bIUhXkyDND3t[YRq[XSnZDDGRWshe2mpbnHsbY5oKHCjdHj3ZZk> Mmi0NlY5QDV4MEi=
HS5 MmPzSpVv[3Srb36gZZN{[Xl? MYWzNEDPxE1? MXTEUXNQ M2nZUIlvcGmkaYTzJINmdGxiYXTo[ZNqd25iYX7kJI1q\3KjdHnvci=> NF7wcHMzPjh6NU[wPC=>
HS27a MoTsSpVv[3Srb36gZZN{[Xl? MWqzNEDPxE1? MlHiSG1UVw>? NFTEe2RqdmirYnn0d{Bk\WyuIHHkbIV{cW:wIHHu[EBucWe{YYTpc44> MUeyOlg5PTZyOB?=
SP53 Mnf0R5l1d3irY3n0fUBie3OjeR?= MV6zNEDPxE1? NXXaTJNETE2VTx?= MYTpcoR2[2W|IHH1eI9xcGGpeR?= MUOyOlg5PTZyOB?=
Jeko MlfsR5l1d3irY3n0fUBie3OjeR?= NGjsVG4{OCEQvF2= M37BO2ROW09? MofTbY5lfWOnczDheZRweGijZ4m= M1nq[VI3QDh3NkC4

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Bcl2 / c-myc / Cyclin D1 / pERK / ERK / pJNK / JNK / Caspase 3 / Cleaved caspase 3 ; 

PubMed: 22821765     


Immunoblot experiment of protein lysate from OPM1 cells treated with NVP-LDE225 (5μM) for 12, 24, and 36 hours and fractionated by electrophoresis and stained with different Abs as shown in figure (left). Cells were treated with different concentrations o䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෕Ð鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸

Gli-1 / Gli-2 / p-Akt / Akt; 

PubMed: 25093491     


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

pp70S6K / P70s6k; 

PubMed: 25093491     


Percentage of survival of 786-O, 786-O SuR, and 769-P renal cancer cell lines treated with NVP-LDE225 and everolimus or their combination, as measured by the MTT assay. Data represent the mean (±s.d.) of three independent experiments, each performed in tr䲧疝Ỵ疞㧀疜膉痘 瘿뙠ෆᾰƌෆĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ෆĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ�෋䐺痖暼瘿�෋ᾰƌ �෋Ð㺣痖�෋€𢡄�෋€䀷痗�෋౴�෋㵶痗�෋뺖᎒泌Itemセ᎒Count﫨呂�෋猴፲�

p-p130CAS / p130CAS / p-FAK / FAK / p-Paxillin / Paxillin; 

PubMed: 25093491     


Western blot analysis of total cell lysates from 786-O, 786-O SuR, and 769-P human renal cancer cell lines treated with NVP-LDE225 (2.5 μm), everolimus (1 μm), and their combination. Densitometric measurements were normalised to β-actin and reported under䲧疝Ỵ疞㧀疜膉痘 

22821765 25093491
Immunofluorescence
GLI1; 

PubMed: 22821765     


U266 were cultured in the presence of control medium or NVP-LDE225 (5μM) for 24 hours. Immunocytochemical analysis was assessed using anti-Gli1 Ab, and 4,6-diamidino-2-phenylindole was used to stain nuclei. The cells were analyzed using an epifluorescence䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෕Ð鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ뙠ෆ䐺痖暼瘿뙠ෆᾰƌ 뙠ෆÐ㺣痖뙠ෆ€𢡄뙤ෆ€

22821765
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]

- 合并
  • 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]

- 合并
  • 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
  • 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
储存条件 粉状
溶于溶剂
别名 Erismodegib

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

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 (mg) = 浓度 (mM) x 体积 (mL) 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02358161 Completed Drug: gemcitabine and nab paclitaxel Pancreatic Cancer Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)|Novartis|Celgene Corporation September 2015 Phase 1|Phase 2
NCT02254551 Terminated Drug: LDE225|Drug: Bortezomib Multiple Myeloma SCRI Development Innovations LLC|Novartis January 2015 Phase 2
NCT02138929 Completed Drug: Everolimus|Drug: LDE 225 Esophageal Cancer M.D. Anderson Cancer Center|Novartis|National Cancer Institute (NCI) November 10 2014 Phase 1
NCT02195973 Completed Drug: LDE225 Recurrent Ovarian Cancer University of Alabama at Birmingham|Novartis Pharmaceuticals September 2014 Phase 1
NCT02027376 Completed Drug: LDE225|Drug: Docetaxel Advanced Breast Cancer Spanish Breast Cancer Research Group|Novartis May 2014 Phase 1
NCT02111187 Completed Drug: LDE225 Prostate Cancer Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins April 2014 Phase 1

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操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID