Crenigacestat (LY3039478)

目录号:S7169

仅限科研使用

Crenigacestat (LY3039478) 是一种有效的Notchgamma-secretase 的抑制剂,其对Notch的IC50值为0.41 nM。

Crenigacestat (LY3039478) Chemical Structure

CAS: 1421438-81-4

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 2121.21 现货
RMB 1417.68 现货
RMB 4677.69 现货
大包装 有超大折扣

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客户使用Selleck生产的Crenigacestat (LY3039478)发表文献16篇:

产品安全说明书

Notch抑制剂选择性比较

生物活性

产品描述 Crenigacestat (LY3039478) 是一种有效的Notchgamma-secretase 的抑制剂,其对Notch的IC50值为0.41 nM。
靶点
Notch [1]
~1 nM
体外研究

LY3039478是一种Notch-1胞内区域剪切的有效抑制剂,在大多数所检测的肿瘤细胞中IC50中约为1 nM。LY3039478也有效地抑制突变型Notch受体活性[2]。LY3039478可显著地抑制两种肾透明细胞癌细胞的生长。其处理可减少Myc和cyclin A1的表达,引起透明细胞癌细胞在G0/G1期的细胞阻滞[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SW480 NXq4VIZiTnWwY4Tpc44h[XO|YYm= Ml7RNlQhcHK| NITEXJRKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCvZXTpZZRm\CClbHXheoFo\SCxZjDOc5RkcCBzIHnuJIh2dWGwIGPXOFgxKGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVAhRSByLkCwNFEh|ryPLh?= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[3PEc,OjR7MEC2O|g9N2F-
HEL 92.1.7 NXz0UpRITnWwY4Tpc44h[XO|YYm= NIfhe3ozPCCqcoO= MUjJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBu\WSrYYTl[EBkdGWjdnHn[UBw\iCQb4TjbEAyKGmwIHj1cYFvKEiHTDC5Nk4yNjdiY3XscJMh[XO|ZYPz[YQh[XNiboXjcIVieiCjY3P1cZVt[XSrb36gc4YhVm:2Y3igNUBqdnS{YXPlcIx2dGG{IHTvcYFqdiBqTkHJR2QqKGGodHXyJFI1KGi{czDifUBGVEmVQTygTWM2OCB;IECuNFAxOjNizszNMi=> MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[3PEc,OjR7MEC2O|g9N2F-
U-87-MG M{LKSGZ2dmO2aX;uJIF{e2G7 Mo\tNlQhcHK| NWLFT2VpUW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2VibXXkbYF1\WRiY3zlZZZi\2Vib3[gUo91[2hiMTDpckBpfW2jbjDVMVg4NU2JIHPlcIx{KGG|c3Xzd4VlKGG|IH71Z4xm[XJiYXPjeY12dGG2aX;uJI9nKE6xdHPoJFEhcW62cnHj[YxtfWyjcjDkc41icW5iKF6xTWNFMSCjZoTldkAzPCCqcoOgZpkhTUyLU1GsJGlEPTBiPTCwMlAxODJ6IN88UU4> MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[3PEc,OjR7MEC2O|g9N2F-
BxPC3 MWLGeY5kfGmxbjDhd5NigQ>? M{\B[|I1KGi{cx?= NGSzbmVKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCvZXTpZZRm\CClbHXheoFo\SCxZjDOc5RkcCBzIHnuJIh2dWGwIFL4VGM{KGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVAhRSByLkCwNFM6KM7:TT6= NWL5RokyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3PzhpPkK0PVAxPjd6PD;hQi=>
HEK293deltaE12 NV7jTZAxTnWwY4Tpc44h[XO|YYm= NILxS5VKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCvZXTpZZRm\CClbHXheoFo\SCxZjD0doFve2[nY4Tl[EBud3W|ZTDOc5RkcCBzIDixO|A{NTJzOEOpJIhiemKxcnnu[{BPNXSncn3pcoFtKDJ|IHHtbY5w[WOrZDDzbYdv[WxicHXweIll\SC|ZYH1[Y5k\SCrbjDoeY1idiCKRVuyPVNl\Wy2YVWxNkBk\WyuczDhd5Nme3OnZDDhd{BvfWOuZXHyJIFk[3WvdXzheIlwdiCxZjDOc5RkcCBzIHnueJJi[2WubIXsZZIh\G:vYXnuJEhPOUmFRDmgZYZ1\XJuIFnDOVAhRSByLkCwNFQyKM7:TT6= NU\VTJI{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3PzhpPkK0PVAxPjd6PD;hQi=>
A375 NXH2PVVrTnWwY4Tpc44h[XO|YYm= M2TDUlI1KGi{cx?= NYX2[YZ3UW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2VibXXkbYF1\WRiY3zlZZZi\2Vib3[gUo91[2hiMTDpckBpfW2jbjDBN|c2KGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVAhRSByLkCwNFQ5KM7:TT6= M4r0blxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwOlc5Lz5{NEmwNFY4QDxxYU6=
MDA-MB-231 NWS4[ohoTnWwY4Tpc44h[XO|YYm= MUGyOEBpenN? MkXITY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhdWWmaXH0[YQh[2ynYY\h[4Uhd2ZiTn;0Z4ghOSCrbjDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGG|c3Xzd4VlKGG|IH71Z4xm[XJiYXPjeY12dGG2aX;uJI9nKE6xdHPoJFEhcW62cnHj[YxtfWyjcjDkc41icW5iKF6xTWNFMSCjZoTldkAzPCCqcoOgZpkhTUyLU1GsJGlEPTBiPTCwMlAxODVizszNMi=> NWLMbXZ4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3PzhpPkK0PVAxPjd6PD;hQi=>
MOLT-3 NY\Lco1QTnWwY4Tpc44h[XO|YYm= NIjXfmgzPCCqcoO= MVLJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBu\WSrYYTl[EBkdGWjdnHn[UBw\iCQb4TjbEAyKGmwIHj1cYFvKE2RTGStN{Bk\WyuczDhd5Nme3OnZDDhd{BvfWOuZXHyJIFk[3WvdXzheIlwdiCxZjDOc5RkcCBzIHnueJJi[2WubIXsZZIh\G:vYXnuJEhPOUmFRDmgZYZ1\XJiMkSgbJJ{KGK7IFXMTXNCNCCLQ{WwJF0hOC5yMEC2NUDPxE1w MlLFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC2O|goRjJ2OUCwOlc5RC:jPh?=
MIAPaCa2 MV;GeY5kfGmxbjDhd5NigQ>? M{\4e|I1KGi{cx?= MYPJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBu\WSrYYTl[EBkdGWjdnHn[UBw\iCQb4TjbEAyKGmwIHj1cYFvKE2LQWDhR4EzKGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVAhRSByLkCwNFcyKM7:TT6= M4jWZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwOlc5Lz5{NEmwNFY4QDxxYU6=
HCT 116 NHn4[3ZHfW6ldHnvckBie3OjeR?= NETpPXQzPCCqcoO= Mn[4TY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhdWWmaXH0[YQh[2ynYY\h[4Uhd2ZiTn;0Z4ghOSCrbjDoeY1idiCKQ2SgNVE3KGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVAhRSByLkCwNFczKM7:TT6= NIPHUIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFY4QCd-MkS5NFA3Pzh:L3G+
MOLT-4 NISyOJJHfW6ldHnvckBie3OjeR?= MVuyOEBpenN? NIW2UYpKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCvZXTpZZRm\CClbHXheoFo\SCxZjDOc5RkcCBzIHnuJIh2dWGwIF3PUHQuPCClZXzsd{Bie3Onc4Pl[EBieyCwdXPs[YFzKGGlY4XteYxifGmxbjDv[kBPd3SlaDCxJIlvfHKjY3XscJVt[XJiZH;tZYlvKCiQMVnDSEkh[W[2ZYKgNlQhcHK|IHL5JGVNUVODLDDJR|UxKD1iMD6wNFA4PCEQvF2u Mk\0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC2O|goRjJ2OUCwOlc5RC:jPh?=
K562 M{HDR2Z2dmO2aX;uJIF{e2G7 MlTzNlQhcHK| NF7ubGRKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCvZXTpZZRm\CClbHXheoFo\SCxZjDOc5RkcCBzIHnuJIh2dWGwIFu1OlIh[2WubIOgZZN{\XO|ZXSgZZMhdnWlbHXhdkBi[2O3bYXsZZRqd25ib3[gUo91[2hiMTDpcpRz[WOnbHz1cIFzKGSxbXHpckApVjGLQ1SpJIFnfGW{IEK0JIhzeyCkeTDFUGlUSSxiSVO1NEA:KDBwMECwO|Qh|ryPLh?= NGPyPFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFY4QCd-MkS5NFA3Pzh:L3G+
CCRF-CEM M1KyVGZ2dmO2aX;uJIF{e2G7 NF\DbIozPCCqcoO= MkHZTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhdWWmaXH0[YQh[2ynYY\h[4Uhd2ZiTn;0Z4ghOSCrbjDoeY1idiCFQ2LGMWNGVSClZXzsd{Bie3Onc4Pl[EBieyCwdXPs[YFzKGGlY4XteYxifGmxbjDv[kBPd3SlaDCxJIlvfHKjY3XscJVt[XJiZH;tZYlvKCiQMVnDSEkh[W[2ZYKgNlQhcHK|IHL5JGVNUVODLDDJR|UxKD1iMD6wNFA4PiEQvF2u NWLsXJBxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3PzhpPkK0PVAxPjd6PD;hQi=>
DLD1 NVPsWoJTTnWwY4Tpc44h[XO|YYm= MXWyOEBpenN? M1fTXmlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iRFzENUBk\WyuczDhd5Nme3OnZDDhd{BvfWOuZXHyJIFk[3WvdXzheIlwdiCxZjDOc5RkcCBzIHnueJJi[2WubIXsZZIh\G:vYXnuJEhPOUmFRDmgZYZ1\XJiMkSgbJJ{KGK7IFXMTXNCNCCLQ{WwJF0hOC5yMEC5PEDPxE1w M2TJT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwOlc5Lz5{NEmwNFY4QDxxYU6=
A2780 MXHGeY5kfGmxbjDhd5NigQ>? MVqyOEBpenN? MmTsTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhdWWmaXH0[YQh[2ynYY\h[4Uhd2ZiTn;0Z4ghOSCrbjDoeY1idiCDMke4NEBk\WyuczDhd5Nme3OnZDDhd{BvfWOuZXHyJIFk[3WvdXzheIlwdiCxZjDOc5RkcCBzIHnueJJi[2WubIXsZZIh\G:vYXnuJEhPOUmFRDmgZYZ1\XJiMkSgbJJ{KGK7IFXMTXNCNCCLQ{WwJF0hOC5yMEGwN{DPxE1w NF\PbIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFY4QCd-MkS5NFA3Pzh:L3G+
SUP-T1 M37QOWZ2dmO2aX;uJIF{e2G7 NHr2RlUzPCCqcoO= NEDqZXJKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCvZXTpZZRm\CClbHXheoFo\SCxZjDOc5RkcCBzIHnuJIh2dWGwIGPVVE1VOSClZXzsd{Bie3Onc4Pl[EBieyCwdXPs[YFzKGGlY4XteYxifGmxbjDv[kBPd3SlaDCxJIlvfHKjY3XscJVt[XJiZH;tZYlvKCiQMVnDSEkh[W[2ZYKgNlQhcHK|IHL5JGVNUVODLDDJR|UxKD1iMD6wNFEzPCEQvF2u M3rwSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwOlc5Lz5{NEmwNFY4QDxxYU6=
Jurkat MWHGeY5kfGmxbjDhd5NigQ>? Ml7jNlQhcHK| M4CzeWlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iSoXyb4F1KGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVAhRSByLkCwOVk2KM7:TT6= NXHIOXdpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3PzhpPkK0PVAxPjd6PD;hQi=>
体内研究 在大鼠中,其口服生物利用度为65%,CL=98 mL/min/kg, VDss=4.9 L/kg。在狗中,口服生物利用度为67%,CL=3.8 mL/min/kg, VDss=1.4 L/kg[1]。在异种移植瘤模型中,LY3039478可在肿瘤微环境中抑制N1ICD的剪切以及Notch靶基因的表达。在依赖于Notch信号的移植瘤模型中,Notch剪切的抑制诱导了凋亡的产生[2]。在免疫缺陷NSG携瘤小鼠(移植769-P CCRCC细胞)中,LY3039478可显著地提高其生存率、延迟肿瘤生长[3]

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:

[4]

  • Cell lines: K07074细胞
  • Concentrations: 100 nM
  • Incubation Time: 24, 48, 72, 96 h
  • Method:

    将K07074细胞以105 cells/孔铺于24孔板中。接种24小时后,向培养基中加入K0704或DMSO。处理完后,测定细胞活性。

动物实验:

[3]

  • Animal Models: Mice
  • Dosages: 8 mg/kg
  • Administration: oral gavage

溶解度(25°C)

体外

* 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 464.44
化学式

C22H23F3N4O4

CAS号 1421438-81-4
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02906618 Completed Drug: LY3039478|Drug: 3C 15N 2H-LY3039478 IV Healthy Eli Lilly and Company October 4 2016 Phase 1
NCT02917733 Completed Drug: LY3039478 Healthy Eli Lilly and Company September 2016 Phase 1
NCT02836600 Active not recruiting Drug: LY3039478 Advanced Solid Tumor Eli Lilly and Company September 9 2016 Phase 1
NCT02518113 Completed Drug: LY3039478|Drug: Dexamethasone|Drug: Placebo T-cell Acute Lymphoblastic Leukemia|T-cell Lymphoblastic Lymphoma Eli Lilly and Company October 1 2015 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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