Alectinib (CH5424802)

For research use only. Not for use in humans.

目录号:S2762 别名: AF-802, RG-7853 中文名称:阿来替尼

Alectinib (CH5424802) Chemical Structure

CAS No. 1256580-46-7

Alectinib (CH5424802, AF-802, RG-7853) 是一种有效的ALK抑制剂,在无细胞试验中IC50为1.9 nM,对L1196M突变型敏感,对ALK比PF-02341066, NVP-TAE684和PHA-E429选择性高。

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客户使用Selleck生产的Alectinib (CH5424802)发表文献53篇:

产品安全说明书

ALK抑制剂选择性比较

生物活性

产品描述 Alectinib (CH5424802, AF-802, RG-7853) 是一种有效的ALK抑制剂,在无细胞试验中IC50为1.9 nM,对L1196M突变型敏感,对ALK比PF-02341066, NVP-TAE684和PHA-E429选择性高。
靶点
ALK (F1174L) [1]
(Cell-free assay)
ALK [1]
(Cell-free assay)
ALK (R1275Q) [1]
(Cell-free assay)
1 nM 1.9 nM 3.5 nM
体外研究

CH5424802作用于ALK 为ATP竞争性的,解离常数(KD)为2.4 nM。CH5424802对ALK 和L1196M 具有强大的抑制效果,Ki分别为0.83 和1.56 nM。 CH5424802 作用于表达EML4-ALK的NCI-H2228 NSCLC细胞,抑制ALK自磷酸化。 CH5424802 也抑制STAT3 和AKT,而不是 ERK1/2的磷酸化。CH5424802 完全抑制STAT3在Tyr705位点的磷酸化。CH5424802优先有效作用于表达EML4-ALK的 NCI-H2228细胞,而不作用于融合ALK的阴性 NSCLC细胞系,包括单层培养的HCC827细胞(EGFR外显子19缺失), A549细胞(KRAS突变), 或NCI-H522细胞(EGFR 野生型, KRAS 野生型, 和ALK野生型)。CH5424802作用于 NCI-H2228球体细胞,引起凋亡标记—caspase-3/7样激活。CH5424802抑制含NPM-ALK融合蛋白的两种淋巴瘤细胞, KARPAS-299和SR生长,为不影响不含ALK融合的 HDLM-2淋巴瘤细胞生长。[1] CH5424802 作用于KARPAS-299具有高度靶向选择性和更强的抗增殖活性。CH5424802抑制KAPRAS-299,IC50为3 nM, 抑制KDR, IC50为1.4 μM。CH5424802代谢稳定性很高。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H2228 NXXjNok5U2mwYYPlJIF{e2G7 NFLDeop,OSEQvF2= MUHwdoV3\W62czDheZRweGixc4Doc5J6dGG2aX;uJI9nKEGOSx?= NU\tfXd7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
KARPAS-299 NVPs[FZIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkG1glExKM7:TR?= MX;JR|UxRTNibl2= M3j2clxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
SR MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1;5VJ4yOCEQvF2= MlXYTWM2OD14Lkmgcm0> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
HDLM-2 NUfPcJhUT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFeye2Z,OTBizszN MW\JR|UxRjFyLECwNEBvVQ>? NVSy[XFxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
NB-1 MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFPGVmJ,OTBizszN NYjHOlFQUUN3ME20MlUhdk1? M4\HT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
KELLY MUfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHnaW3p,OTBizszN NXPlblNNUUN3ME22NkBvVQ>? NIOyTmM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
SK-N-FI MkfLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUT+NVAh|ryP NWGyZ484UUN3ME6xNEwxODBibl2= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
NCI-H2228 MlHDS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWH+NVAh|ryP NXTYenlSUUN3ME21N{BvVQ>? NEjqSmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
Calu-3 NGf2enhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{LOTp4yOCEQvF2= NYDUZ|Y2UUN3ME2+NVAtODByIH7N Mni2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
PC-1 M4T4TWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUT+NVAh|ryP NVKxNo5oUUN3ME6xNEwxODBibl2= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
NCI-H23 MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUn+NVAh|ryP M4nrZmlEPTB;M{[wNEBvVQ>? MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
Calu-1 M2LnT2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWrwOZlrhjFyIN88US=> NF;BZ5FKSzVyPkGwMFAxOCCwTR?= M{nYblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
NCI-H2009 NFjuVGZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3rMTJ4yOCEQvF2= MmLvTWM2OD5zMDywNFAhdk1? NVnLdmh5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
NCI-H1993 NXrwTlVFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUT+NVAh|ryP M4DCXWlEPTB-MUCsNFAxKG6P M1nx[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
MKN-45 M4S2Zmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYm1SIQ2hjFyIN88US=> MnjxTWM2OD5zMDywNFAhdk1? MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
SNU-5 NFfBdnlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFPXRnR,OTBizszN M3\MNGlEPTB;MUiwNEBvVQ>? NV3QRW1GRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
KATO-III MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXz+NVAh|ryP M4HKNmlEPTB;N{mwNEBvVQ>? NVz3TnJORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
SK-BR-3 NYnlSFRNT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWCxVI1OhjFyIN88US=> M{PPNWlEPTB-MUCsNFAxKG6P M{juO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
BT-483 NYjWXXRpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2PLSZ4yOCEQvF2= MmTRTWM2OD5zMDywNFAhdk1? NVTCSmp5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
PC-3 MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVP+NVAh|ryP MY\JR|UxRjFyLECwNEBvVQ>? NFrCOnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
22Rv1 NGLi[4hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWn+NVAh|ryP M2XUTWlEPTB-MUCsNFAxKG6P NVHuTFZyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
U-87 MG NWPSOnNST3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXL+NVAh|ryP M1j6NmlEPTB-MUCsNFAxKG6P MoLHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
H3122 NUfaO49WT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mm\iglExKM7:TR?= M4HwVGlEPTB;M{Ogcm0> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB7NkSwNEc,OjVyOU[0NFA9N2F-
LC-2/ad MnTqRZBweHSxc3nzJIF{e2G7 NWG4RoxGhjFizszN NES2b5FFVVOR M{[3O4lv\HWlZYOgZZBweHSxc3nz M2rUZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{S5N|A4Lz5{NUO0PVMxPzxxYU6=
LC-2/ad M1L0RWZ2dmO2aX;uJIF{e2G7 MWr+NUDPxE1? NFvNRXJFVVOR NWLtV2RzcW6qaXLpeJMhfGinIF3BVGshe2mpbnHsbY5oKHCjdHj3ZZk> NWXGRmh2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOFk{ODdpPkK1N|Q6OzB5PD;hQi=>
Ba/F3 MWTGeY5kfGmxbjDhd5NigQ>? NV\ZTIxZhjFizszN M4nxR2ROW09? NXLOe4lXe3WycILld5NmeyCyaH;zdIhwenmuYYTpc44hd2ZiRWLLJIFv\CCrbnPy[YF{\XNidHjlJIFjfW6mYX7j[UBw\iCESV2= NFuxOFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO0PVMxPyd-MkWzOFk{ODd:L3G+
SNU-2535 MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGrV[YJ,OTBizszN M3PrWWlEPTB;M{OuNUBvVQ>? NHP1UIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki0PVY{Pyd-Mk[4OFk3Ozd:L3G+
SNU-2535 Mn;VT4lv[XOnIHHzd4F6 MVv+NUDPxE1? NWHhWZhucW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBUGsh[W6mIHn0d{Bld3ewc4Ty[YFuKG2xbHXjeYxmeyCHUluxM|Ih[W6mIFHLWC=> NHztfZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki0PVY{Pyd-Mk[4OFk3Ozd:L3G+
Ba/F3 NFzkZ3lHfW6ldHnvckBie3OjeR?= NV73RYZCPzJiaILz NU\2XWFlUW6qaXLpeIlwdiCxZjDFUWw1NUGOSzDDNVE2PllibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIH3veZNmKEKjL1[zJINmdGy|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSCPVGOgZZN{[XluIFnDOVAhRSByLkCwNkDPxE1w Mn6yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
Ba/F3 NHfhUlVHfW6ldHnvckBie3OjeR?= NELjOJE4OiCqcoO= MmfxTY5pcWKrdHnvckBw\iCHTVy0MWFNUyCVMUKwOnkhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKG2xdYPlJGJiN0Z|IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFczKGi{czDifUBOXFNiYYPzZZktKEmFNUCgQUAxNjByMjFOwG0v MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
Ba/F3 NYHGdHlOTnWwY4Tpc44h[XO|YYm= MWW3NkBpenN? MlPuTY5pcWKrdHnvckBw\iC5aXzkJJR6eGViRV3MOE1CVEtiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gcY92e2ViQnGvSlMh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDD2bYFjcWyrdImgZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygTWM2OCB;IECuNFAzKM7:TT6= M4LCeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
KARPAS299 M1TGXGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NVvjRVBkQTZiaILz NGLuO2dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvBVnBCWzJ7OTDj[YxteyCjZoTldkA6PiCqcoOgZpkh[2WubDDjc5VvfGmwZzDhd5NigSxiSVO1NEA:KDBwMECzJO69VS5? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ{NUmxO{c,OjJ{MkW5NVc9N2F-
Ba/F3 M1SwO2Z2dmO2aX;uJIF{e2G7 NVPYeZFtPzJiaILz MmfQTY5pcWKrdHnvckBw\iCHTVy0MWFNUyCIMUG3OGwhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKG2xdYPlJGJiN0Z|IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFczKGi{czDifUBOXFNiYYPzZZktKEmFNUCgQUAxNjByMzFOwG0v M2rKflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
Ba/F3 Mn\ZSpVv[3Srb36gZZN{[Xl? NF3sNJA4OiCqcoO= NEHV[llKdmirYnn0bY9vKG:oIFXNUFQuSUyNIFexNlY6SSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSmFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiSVO1NEA:KDBwMEC5JO69VS5? M1HDSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
NCI-H3122 NYnCfpZsSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MkfvO|IhcHK| NITSSZdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOzF{MjDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDMeY1qdmW|Y3XueEBE\WyuIG\pZYJqdGm2eTDBd5NigSxiRVO1NEA:KDBwMEC5JO69VS5? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
KARPAS299 M4TWcWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M3fSfFczKGi{cx?= M{nrW2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1HSVGFUOjl7IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJxQ1PLMVgh[XO|YYmsJGlEPTBiPTCwMlAyPSEQvF2u MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF|MUC2Okc,OjdzM{GwOlY9N2F-
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SUP-M2 NGH4enRCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NV\jc49WPzJiaILz NY\YVpZjSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTWXAuVTJiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSi:FQ1utPEBie3OjeTygTWM2OCB;IECuNFE4QSEQvF2u MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF|MUC2Okc,OjdzM{GwOlY9N2F-
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SMS-KCNR NWji[|h7SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NGn0SoY4OiCqcoO= NWnZUWJqSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTUXMuU0OQUjDj[YxteyCneIDy[ZN{cW6pIFXNUFQuSUyNIGKxNlc2WSCvdYThcpQh[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9iTIXtbY5me2OnboSgR4VtdCCYaXHibYxqfHliQYPzZZktKEWFNUCgQUAxNjd4NTFOwG0v NXXROlM4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OlgzQDlpPkK2OVY5Ojh7PD;hQi=>
SK-N-SH MXvBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M2HicFczKGi{cx?= Mm[4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3OMXNJKGOnbHzzJIV5eHKnc4PpcochTU2OND3BUGshTjFzN{TMJI12fGGwdDDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BNfW2rbnXzZ4VvfCCFZXzsJHZq[WKrbHn0fUBCe3OjeTygSWM2OCB;IECuPFczKM7:TT6= NXrsRXFyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OlgzQDlpPkK2OVY5Ojh7PD;hQi=>
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LAN1 M{P2d2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 M37Rd|czKGi{cx?= NVu5Ro13SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMRW4yKGOnbHzzJIV5eHKnc4PpcochTU2OND3BUGshTjFzN{TMJI12fGGwdDDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BNfW2rbnXzZ4VvfCCFZXzsJHZq[WKrbHn0fUBCe3OjeTygSWM2OCB;IEKuNFA1KM7:TT6= NEC2W|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
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NIH/3T3 M4fBTmFvfGm2dX3vdkBie3OjeR?= MWC1NEBu\y:tZx?= MoL1NVAh\GG7cx?= MWPBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCQSVivN3Q{KGOnbHzzJIV5eHKnc4PpcochTU2OND3BUGshVDFzOU\NJI12fGGwdDD4[Y5w\3KjZoTl[EBqdiCwdXTlJI1wfXOnIHHzd4V{e2WmIHHzJJBienSrYXygeJVud3JicnXndoV{e2mxbjDheEA2OCCvZz;r[{wheG9icXSgZYRucW6rc4TldoVlKG[xcjCxNEBl[Xm| M1rabVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUOxNFY3Lz5{N{GzNVA3PjxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pALK / ALK / pAKT / AKT / pERK / ERK / pS6 / S6 ; 

PubMed: 25228534     


Parental H3122 and CHR-A1 cells were treated with alectinib at the indicated concentrations for 6 hrs. Cell extracts were immunoblotted to detect the indicated proteins.

PARP / cleaved PARP / Akt / caspase 3 / Cleaved caspase 3; 

PubMed: 28455243     


Alectinib inhibits PI3K/Akt/mTOR signaling and induces apoptosis in NB cells. NB-19, Kelly, IMR-32, SH-SY5Y, SK-N-AS and LA-N-6 cells were treated with 10 μM alectinib for various time points as indicated. The anti-β-Actin antibody was used as a loading c䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ

pROS1 / ROS1 / pSTAT3 / STAT3; 

PubMed: 25351743     


Inhibition of phospho-ROS1 by various ALK inhibitors in Ba/F3 models. CD74-ROS1 expressing Ba/F3 cells were exposed to increasing concentrations of crizotinib, ceritinib, AP26113, or ASP3026 for 3 h. Cell lysates were immunoblotted to detect the indicated䲧疝Ỵ疞㧀

p-EGFR Tyr1068 / EGFR / p-HER3 Tyr1222 / HER3 / p-IGF-1R Tyr1135 / IGF-1R; 

PubMed: 26992917     


Cells were treated with indicated drugs for 1 hour; immunoblotting for RTKs in both resistant cell lines showed upregulation of phosphor-EGFR and phosphor-HER3 when compared with parental cells.

25228534 28455243 25351743 26992917
Growth inhibition assay
Cell viability ; 

PubMed: 25228534     


(A) Cells were seeded in 96-well black plates and treated with increasing concentrations of alectinib for 72 hrs. Cell survival was analyzed using the CellTiter-Glo assay. While H3122 cells showed high sensitivity to alectinib (red line), H3122 CHR-A1 cel䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ෋à 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෋à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

25228534
体内研究 CH5424802口服处理,抑制肿瘤生长,这种作用存在剂量依赖性,ED50为0.46 mg/kg。CH5424802按20 mg/kg剂量处理,引起肿瘤快速衰退,衰退达168%,处理11天后(在第28天)每个鼠中的肿瘤体积<30 mm3, 维持有效的抗肿瘤效果,且在4周的无药处理期间,不会出现肿瘤再生长。CH5424802 处理小鼠的半衰期和口服生物有效性分别为8.6 小时和 70.8%。按6 mg/kg重复剂量处理,在2,7,和24小时后,平均血浆水平达到1.7,1.5,和0.3 nM。CH5424802处理抑制肿瘤生长。CH5424802按20 mg/kg剂量处理 KARPAS-299 和 NB-1,在第20天,肿瘤生长抑制达 119% 和104%。CH5424802 抑制STAT3磷酸化,这种作用存在剂量依赖性(2-20 mg/kg)。CH5424802处理的移植瘤中,观察到AKT磷酸化部分降低。[1]

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)

激酶实验:[1]
- 合并

体外激酶抑制检测:

在CH5424802存在时,通过时间分辨荧光共振能量转移(TR-FRET)分析或荧光偏振(FP)法测量磷酸化各种底物肽的能力,而测评抑制各种激酶(除了MEK1和 Raf-1)的能力。在CH5424802存在时,通过定量分析重组ERK2 蛋白对底物的磷酸化而测评对MEK1的抑制活性。在 CH5424802存在时,通过测定激酶磷酸化MEK1的能力而测评对Raf-1的抑制活性。
细胞实验:[1]
- 合并
  • Cell lines: NSCLC, A549 和 HCC827 细胞
  • Concentrations: 0-1 μM
  • Incubation Time: 5天
  • Method: NSCLC, A549 和HCC827细胞接种在96孔板中过夜,与不同浓度CH5424802按指定时间温育。球体细胞生长抑制实验中,细胞接种在球板上,温育过夜,然后在指定时间用化合物处理。通过发光细胞活性检测存活细胞。使用Caspase-Glo 3/7 检测试剂盒进行Caspase-3/7检测。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 携带NCI-H2228细胞的 SCID 或裸鼠
  • Dosages: 20 mg/kg
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 0.5 mg/mL warmed (1.03 mM)
Water Insoluble
Ethanol 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 482.62
化学式

C30H34N4O2

CAS号 1256580-46-7
储存条件 粉状
溶于溶剂
别名 AF-802, RG-7853

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
NCT04774718 Not yet recruiting Drug: Alectinib ALK Fusion-positive Solid or CNS Tumors Hoffmann-La Roche December 31 2021 Phase 1|Phase 2
NCT04764188 Not yet recruiting Drug: Alectinib NSCLC Hoffmann-La Roche May 17 2021 --
NCT04644315 Recruiting Drug: Alectinib Solid Tumors Hoffmann-La Roche May 3 2021 Phase 2
NCT04708639 Enrolling by invitation Drug: Alectinib Lung Cancer|ALK Gene Mutation|Resistance Disease|Mutation Aarhus University Hospital|Roche Pharma AG June 19 2019 --
NCT03445000 Terminated Drug: Alectinib Non-small Cell Lung Cancer|Non-small Cell Lung Cancer Metastatic|Non-small Cell Lung Cancer Recurrent European Thoracic Oncology Platform|Hoffmann-La Roche November 6 2018 Phase 2

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操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID