Crenigacestat (LY3039478)

For research use only. Not for use in humans.

目录号:S7169

Crenigacestat (LY3039478) Chemical Structure

CAS No. 1421438-81-4

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

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
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客户使用Selleck生产的Crenigacestat (LY3039478)发表文献12篇:

客户使用该产品的1个实验数据:

  • Effect of LY3039478 on Hes protein in SGC7901/DDP cells. A, Protein expression of Hes-1 by Western blot. B, Expression level of Hes-1 by Western blot experiment. (*p < 0.05 control with LY3039478 0 μmol/L group; **p < 0.01 control with LY3039478 0 μmol/L group).

    Eur Rev Med Pharmacol Sci, 2018, 22(13):4121-4127. Crenigacestat (LY3039478) purchased from Selleck.

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 NYDDZ5pTTnWwY4Tpc44h[XO|YYm= M33ld|I1KGi{cx?= M{PTe2lvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iU2e0PFAh[2WubIOgZZN{\XO|ZXSgZZMhdnWlbHXhdkBi[2O3bYXsZZRqd25ib3[gUo91[2hiMTDpcpRz[WOnbHz1cIFzKGSxbXHpckApVjGLQ1SpJIFnfGW{IEK0JIhzeyCkeTDFUGlUSSxiSVO1NEA:KDBwMECwNUDPxE1w MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[3PEc,OjR7MEC2O|g9N2F-
HEL 92.1.7 MnXmSpVv[3Srb36gZZN{[Xl? NID2Z3UzPCCqcoO= MWDJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBu\WSrYYTl[EBkdGWjdnHn[UBw\iCQb4TjbEAyKGmwIHj1cYFvKEiHTDC5Nk4yNjdiY3XscJMh[XO|ZYPz[YQh[XNiboXjcIVieiCjY3P1cZVt[XSrb36gc4YhVm:2Y3igNUBqdnS{YXPlcIx2dGG{IHTvcYFqdiBqTkHJR2QqKGGodHXyJFI1KGi{czDifUBGVEmVQTygTWM2OCB;IECuNFAxOjNizszNMi=> NGjUOpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFY4QCd-MkS5NFA3Pzh:L3G+
U-87-MG MXXGeY5kfGmxbjDhd5NigQ>? MoX6NlQhcHK| NID6emZKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCvZXTpZZRm\CClbHXheoFo\SCxZjDOc5RkcCBzIHnuJIh2dWGwIGWtPFcuVUdiY3XscJMh[XO|ZYPz[YQh[XNiboXjcIVieiCjY3P1cZVt[XSrb36gc4YhVm:2Y3igNUBqdnS{YXPlcIx2dGG{IHTvcYFqdiBqTkHJR2QqKGGodHXyJFI1KGi{czDifUBGVEmVQTygTWM2OCB;IECuNFAxOjhizszNMi=> NFfRVVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFY4QCd-MkS5NFA3Pzh:L3G+
BxPC3 MYPGeY5kfGmxbjDhd5NigQ>? NG\jepUzPCCqcoO= NUn4XXlJUW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2VibXXkbYF1\WRiY3zlZZZi\2Vib3[gUo91[2hiMTDpckBpfW2jbjDCfHBEOyClZXzsd{Bie3Onc4Pl[EBieyCwdXPs[YFzKGGlY4XteYxifGmxbjDv[kBPd3SlaDCxJIlvfHKjY3XscJVt[XJiZH;tZYlvKCiQMVnDSEkh[W[2ZYKgNlQhcHK|IHL5JGVNUVODLDDJR|UxKD1iMD6wNFA{QSEQvF2u NY\3dFI4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3PzhpPkK0PVAxPjd6PD;hQi=>
HEK293deltaE12 NGXaUopHfW6ldHnvckBie3OjeR?= NYDLSXBrUW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2VibXXkbYF1\WRiY3zlZZZi\2Vib3[geJJidnOoZXP0[YQhdW:3c3WgUo91[2hiMTCoNVcxOy1{MUizLUBp[XKkb4LpcochVi22ZYLtbY5idCB{MzDhcYlvd2GlaXSgd4lodmGuIIDldJRq\GVic3XxeYVv[2ViaX6gbJVu[W5iSFXLNlk{\GWudHHFNVIh[2WubIOgZZN{\XO|ZXSgZZMhdnWlbHXhdkBi[2O3bYXsZZRqd25ib3[gUo91[2hiMTDpcpRz[WOnbHz1cIFzKGSxbXHpckApVjGLQ1SpJIFnfGW{LDDJR|UxKD1iMD6wNFA1OSEQvF2u NGXUbJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFY4QCd-MkS5NFA3Pzh:L3G+
A375 MVLGeY5kfGmxbjDhd5NigQ>? NG\nZVkzPCCqcoO= Mon6TY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhdWWmaXH0[YQh[2ynYY\h[4Uhd2ZiTn;0Z4ghOSCrbjDoeY1idiCDM{e1JINmdGy|IHHzd4V{e2WmIHHzJI52[2ynYYKgZYNkfW23bHH0bY9vKG:oIF7veINpKDFiaX70doFk\WyudXzhdkBld22jaX6gLG4yUUOGKTDh[pRmeiB{NDDodpMh[nliRVzJV2EtKEmFNUCgQUAxNjByMES4JO69VS5? NGm1dIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFY4QCd-MkS5NFA3Pzh:L3G+
MDA-MB-231 MonOSpVv[3Srb36gZZN{[Xl? MkfzNlQhcHK| M4jxOmlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjc4Pld5Nm\CCjczDueYNt\WG{IHHjZ5VufWyjdHnvckBw\iCQb4TjbEAyKGmwdILhZ4VtdHWuYYKg[I9u[WmwIDjONWlETCliYX\0[ZIhOjRiaILzJIJ6KEWOSWPBMEBKSzVyIE2gNE4xODB3IN88UU4> NInUW5U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFY4QCd-MkS5NFA3Pzh:L3G+
MOLT-3 MVrGeY5kfGmxbjDhd5NigQ>? NEjLOpozPCCqcoO= M4TXO2lvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iTV;MWE0{KGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVAhRSByLkCwNFYyKM7:TT6= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[3PEc,OjR7MEC2O|g9N2F-
MIAPaCa2 NWL0NJp7TnWwY4Tpc44h[XO|YYm= NY\PPWF{OjRiaILz NVvIe|h[UW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2VibXXkbYF1\WRiY3zlZZZi\2Vib3[gUo91[2hiMTDpckBpfW2jbjDNTWFR[UOjMjDj[YxteyCjc4Pld5Nm\CCjczDueYNt\WG{IHHjZ5VufWyjdHnvckBw\iCQb4TjbEAyKGmwdILhZ4VtdHWuYYKg[I9u[WmwIDjONWlETCliYX\0[ZIhOjRiaILzJIJ6KEWOSWPBMEBKSzVyIE2gNE4xODB5MTFOwG0v MmLwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC2O|goRjJ2OUCwOlc5RC:jPh?=
HCT 116 NFm0V2VHfW6ldHnvckBie3OjeR?= M{HqVFI1KGi{cx?= MlzYTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhdWWmaXH0[YQh[2ynYY\h[4Uhd2ZiTn;0Z4ghOSCrbjDoeY1idiCKQ2SgNVE3KGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVAhRSByLkCwNFczKM7:TT6= Mm\MQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC2O|goRjJ2OUCwOlc5RC:jPh?=
MOLT-4 M{GzRWZ2dmO2aX;uJIF{e2G7 NWK0XHV1OjRiaILz MnnqTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhdWWmaXH0[YQh[2ynYY\h[4Uhd2ZiTn;0Z4ghOSCrbjDoeY1idiCPT1zUMVQh[2WubIOgZZN{\XO|ZXSgZZMhdnWlbHXhdkBi[2O3bYXsZZRqd25ib3[gUo91[2hiMTDpcpRz[WOnbHz1cIFzKGSxbXHpckApVjGLQ1SpJIFnfGW{IEK0JIhzeyCkeTDFUGlUSSxiSVO1NEA:KDBwMECwO|Qh|ryPLh?= Mn3UQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC2O|goRjJ2OUCwOlc5RC:jPh?=
K562 MYPGeY5kfGmxbjDhd5NigQ>? NUDJ[IhFOjRiaILz MWXJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBu\WSrYYTl[EBkdGWjdnHn[UBw\iCQb4TjbEAyKGmwIHj1cYFvKEt3NkKgZ4VtdHNiYYPz[ZN{\WRiYYOgcpVkdGWjcjDhZ4N2dXWuYYTpc44hd2ZiTn;0Z4ghOSCrboTyZYNmdGy3bHHyJIRwdWGrbjCoUlFKS0RrIHHmeIVzKDJ2IHjyd{BjgSCHTFnTRUwhUUN3MDC9JFAvODByN{Sg{txONg>? M{jZ[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwOlc5Lz5{NEmwNFY4QDxxYU6=
CCRF-CEM MVrGeY5kfGmxbjDhd5NigQ>? NEXvU3QzPCCqcoO= MYnJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBu\WSrYYTl[EBkdGWjdnHn[UBw\iCQb4TjbEAyKGmwIHj1cYFvKEOFUl[tR2VOKGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVAhRSByLkCwNFc3KM7:TT6= MkPqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC2O|goRjJ2OUCwOlc5RC:jPh?=
DLD1 M1LLNGZ2dmO2aX;uJIF{e2G7 MY[yOEBpenN? MkDETY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhdWWmaXH0[YQh[2ynYY\h[4Uhd2ZiTn;0Z4ghOSCrbjDoeY1idiCGTFSxJINmdGy|IHHzd4V{e2WmIHHzJI52[2ynYYKgZYNkfW23bHH0bY9vKG:oIF7veINpKDFiaX70doFk\WyudXzhdkBld22jaX6gLG4yUUOGKTDh[pRmeiB{NDDodpMh[nliRVzJV2EtKEmFNUCgQUAxNjByMEm4JO69VS5? MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[3PEc,OjR7MEC2O|g9N2F-
A2780 NF\Y[5VHfW6ldHnvckBie3OjeR?= NEXiS5EzPCCqcoO= MkXsTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhdWWmaXH0[YQh[2ynYY\h[4Uhd2ZiTn;0Z4ghOSCrbjDoeY1idiCDMke4NEBk\WyuczDhd5Nme3OnZDDhd{BvfWOuZXHyJIFk[3WvdXzheIlwdiCxZjDOc5RkcCBzIHnueJJi[2WubIXsZZIh\G:vYXnuJEhPOUmFRDmgZYZ1\XJiMkSgbJJ{KGK7IFXMTXNCNCCLQ{WwJF0hOC5yMEGwN{DPxE1w MmDsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC2O|goRjJ2OUCwOlc5RC:jPh?=
SUP-T1 NYOxWI1yTnWwY4Tpc44h[XO|YYm= Mn7VNlQhcHK| M1XWfWlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iU2XQMXQyKGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVAhRSByLkCwNVI1KM7:TT6= MonlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC2O|goRjJ2OUCwOlc5RC:jPh?=
Jurkat MX\GeY5kfGmxbjDhd5NigQ>? NVfmUYxpOjRiaILz M3nmdWlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iSoXyb4F1KGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVAhRSByLkCwOVk2KM7:TT6= NVizVoZtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3PzhpPkK0PVAxPjd6PD;hQi=>

... Click to View More Cell Line Experimental Data

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]

- 合并
  • 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。


    (Only for Reference)
动物实验:

[3]

- 合并
  • Animal Models: Mice
  • Dosages: 8 mg/kg
  • Administration: oral gavage
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 92 mg/mL (198.08 mM)
Ethanol 71 mg/mL (152.87 mM)
Water Insoluble

* 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 粉状
溶于溶剂
别名

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、SDS / 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、SDS / 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
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID