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55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 NIG0cppMcW6jc3WgZZN{[Xl? Ml\NglEh|ryP NHnSOZJxemW4ZX70d{BifXSxcHjvd5Bpd3K7bHH0bY9vKG:oIFHMTy=> NUL5cXBGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
KARPAS-299 NU\nWJA6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWjPSZc5hjFyIN88US=> MV\JR|UxRTNibl2= Mlz1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
SR NXPobYVwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWX+NVAh|ryP MXfJR|UxRTZwOTDuUS=> MmTHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
HDLM-2 NXrzZ5doT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYrGeI1VhjFyIN88US=> NULUTIRmUUN3ME6xNEwxODBibl2= NYPvcYZERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
NB-1 NIHRVGRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NV7SOIJOhjFyIN88US=> MV3JR|UxRTRwNTDuUS=> MkHwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
KELLY NWPqboNIT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3zLUZ4yOCEQvF2= MofHTWM2OD14MjDuUS=> MneyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
SK-N-FI M4jhUGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmrhglExKM7:TR?= M4HodGlEPTB-MUCsNFAxKG6P NFfLWlE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
NCI-H2228 NVj5dJduT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2fud54yOCEQvF2= MnjmTWM2OD13MzDuUS=> NXrFfZlIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
Calu-3 MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVfCS4huhjFyIN88US=> MXrJR|UxRT5zMDywNFAhdk1? NWnMRnhbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
PC-1 NInlPZFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2KxZp4yOCEQvF2= NIW3cIhKSzVyPkGwMFAxOCCwTR?= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
NCI-H23 M13xfGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{nNZ54yOCEQvF2= NU\pNFY1UUN3ME2zOlAxKG6P Mo\sQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
Calu-1 MnLvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFTwWnF,OTBizszN NHLpcpVKSzVyPkGwMFAxOCCwTR?= MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
NCI-H2009 MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NF7peGN,OTBizszN MWTJR|UxRjFyLECwNEBvVQ>? NGn3fHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
NCI-H1993 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVf+NVAh|ryP MWXJR|UxRjFyLECwNEBvVQ>? NHq4Umk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
MKN-45 MkTnS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnXDglExKM7:TR?= NGXsUWtKSzVyPkGwMFAxOCCwTR?= M2[0WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
SNU-5 MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnS0glExKM7:TR?= M{HWU2lEPTB;MUiwNEBvVQ>? MoXsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
KATO-III MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFvWVYl,OTBizszN NWmxcFRpUUN3ME23PVAxKG6P NYjDUmoyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
SK-BR-3 MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1XjbZ4yOCEQvF2= M{\j[mlEPTB-MUCsNFAxKG6P MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
BT-483 NEjqU5RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYP+NVAh|ryP MUfJR|UxRjFyLECwNEBvVQ>? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
PC-3 NInsZW5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHT4TZl,OTBizszN Mlr4TWM2OD5zMDywNFAhdk1? MkLjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
22Rv1 M3;WXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUHaUYFphjFyIN88US=> NInO[ppKSzVyPkGwMFAxOCCwTR?= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
U-87 MG M1HZOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlfJglExKM7:TR?= NIX2NIZKSzVyPkGwMFAxOCCwTR?= NVr2Om83RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
H3122 MnT2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlHMglExKM7:TR?= NGrEVpVKSzVyPUOzJI5O Ml7VQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyOU[0NFAoRjJ3MEm2OFAxRC:jPh?=
LC-2/ad NX\SRolySXCxcITvd4l{KGG|c3H5 NFi3SGZ,OSEQvF2= MVHEUXNQ M3j0fIlv\HWlZYOgZZBweHSxc3nz M3y3cVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{S5N|A4Lz5{NUO0PVMxPzxxYU6=
LC-2/ad NFvTVItHfW6ldHnvckBie3OjeR?= NFO4T4V,OSEQvF2= MUjEUXNQ M1\OeolvcGmkaYTzJJRp\SCPQWDLJJNq\26jbHnu[{Bx[XSqd3H5 M4[ySFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{S5N|A4Lz5{NUO0PVMxPzxxYU6=
Ba/F3 NUi0VmgyTnWwY4Tpc44h[XO|YYm= NF\IboV,OSEQvF2= MljXSG1UVw>? NYPmWFdCe3WycILld5NmeyCyaH;zdIhwenmuYYTpc44hd2ZiRWLLJIFv\CCrbnPy[YF{\XNidHjlJIFjfW6mYX7j[UBw\iCESV2= NYG2b2s5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOFk{ODdpPkK1N|Q6OzB5PD;hQi=>
SNU-2535 M2nMZmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{mzOZ4yOCEQvF2= NXS1d|FoUUN3ME2zN{4yKG6P MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh2OU[zO{c,OjZ6NEm2N|c9N2F-
SNU-2535 M4CxUWtqdmG|ZTDhd5NigQ>? MVj+NUDPxE1? NEmy[HRqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHMT{BidmRiaYTzJIRwf26|dILlZY0hdW:uZXP1cIV{KEWUS{GvNkBidmRiQVvU MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh2OU[zO{c,OjZ6NEm2N|c9N2F-
Ba/F3 M1jEU2Z2dmO2aX;uJIF{e2G7 NEDyeos4OiCqcoO= NIDvSGVKdmirYnn0bY9vKG:oIFXNUFQuSUyNIFOxNVU3YSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSmFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiSVO1NEA:KDBwMECyJO69VS5? NXPrOGF2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OlgzQDlpPkK2OVY5Ojh7PD;hQi=>
Ba/F3 NHXNR4pHfW6ldHnvckBie3OjeR?= MnO2O|IhcHK| NFf0O4JKdmirYnn0bY9vKG:oIFXNUFQuSUyNIGOxNlA3YSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSmFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiSVO1NEA:KDBwMECyJO69VS5? M2nH[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
Ba/F3 MXTGeY5kfGmxbjDhd5NigQ>? NYryeWFQPzJiaILz MonMTY5pcWKrdHnvckBw\iC5aXzkJJR6eGViRV3MOE1CVEtiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gcY92e2ViQnGvSlMh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDD2bYFjcWyrdImgZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygTWM2OCB;IECuNFAzKM7:TT6= Ml\JQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
KARPAS299 NIjEcWNCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= Mo\RPVYhcHK| M3Hx[WFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1HSVGFUOjl7IHPlcIx{KGGodHXyJFk3KGi{czDifUBk\WyuIHPveY51cW6pIHHzd4F6NCCLQ{WwJF0hOC5yMEOg{txONg>? NILuOpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKyOVkyPyd-MkKyNlU6OTd:L3G+
Ba/F3 NXPYfZpGTnWwY4Tpc44h[XO|YYm= NYnTfWZ1PzJiaILz NFjhU2ZKdmirYnn0bY9vKG:oIFXNUFQuSUyNIF[xNVc1VCCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSmFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiSVO1NEA:KDBwMECzJO69VS5? NFLSZmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
Ba/F3 M2nEW2Z2dmO2aX;uJIF{e2G7 MYS3NkBpenN? MWnJcohq[mm2aX;uJI9nKEWPTEStRWxMKEdzMk[5RUBufXSjboSgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hdW:3c3WgRoEwTjNiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JG1VWyCjc4PhfUwhUUN3MDC9JFAvODB7IN88UU4> MlTZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
NCI-H3122 MYTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MWS3NkBpenN? MlPDRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFMyOjJiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9iTIXtbY5me2OnboSgR4VtdCCYaXHibYxqfHliQYPzZZktKEWFNUCgQUAxNjByOTFOwG0v MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
KARPAS299 NV30OmVUSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NITXU3c4OiCqcoO= NFLVb3dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvBVnBCWzJ7OTDj[YxteyCjZoTldkA4OiCqcoOgZpkhW1KEL1PDT{05KGG|c3H5MEBKSzVyIE2gNE4xOTVizszNMi=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF|MUC2Okc,OjdzM{GwOlY9N2F-
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SMS-KCNR M{\HVWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M4[5UFczKGi{cx?= NXfzSW1MSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTUXMuU0OQUjDj[YxteyCneIDy[ZN{cW6pIFXNUFQuSUyNIGKxNlc2WSCvdYThcpQh[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9iTIXtbY5me2OnboSgR4VtdCCYaXHibYxqfHliQYPzZZktKEWFNUCgQUAxNjd4NTFOwG0v NYXyeoRQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OlgzQDlpPkK2OVY5Ojh7PD;hQi=>
SK-N-SH NIjzdmJCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M4TLN|czKGi{cx?= M2PxfGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utUk1UUCClZXzsd{BmgHC{ZYPzbY5oKEWPTEStRWxMKEZzMUe0UEBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hVHWvaX7ld4NmdnRiQ3XscEBXcWGkaXzpeJkhSXO|YYmsJGVEPTBiPTCwMlg4OiEQvF2u NYfU[4pYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OlgzQDlpPkK2OVY5Ojh7PD;hQi=>
SH-SY5Y Mm\3RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M1fQPVczKGi{cx?= MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOKLWPZOXkh[2WubIOg[ZhxemW|c3nu[{BGVUx2LVHMT{BHOTF5NFygcZV1[W62IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJGx2dWmwZYPj[Y51KEOnbHygWoli[mmuaYT5JGF{e2G7LDDFR|UxKD1iMT6xOUDPxE1w NX7yS25rRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OlgzQDlpPkK2OVY5Ojh7PD;hQi=>
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... 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、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
NCT04774718 Recruiting Drug: Alectinib ALK Fusion-positive Solid or CNS Tumors Hoffmann-La Roche December 31 2021 Phase 1|Phase 2
NCT04979988 Not yet recruiting Drug: Lorlatinib ALK-positive Non-small-cell Lung Cancer Pfizer August 2 2021 --
NCT04764188 Recruiting Drug: Alectinib NSCLC Hoffmann-La Roche May 10 2021 --
NCT04644315 Recruiting Drug: Alectinib Neoplasms|Colorectal Neoplasms|Melanoma|Pancreatic Neoplasms|Sarcoma|Ovarian Neoplasms|Brain Neoplasms|Thyroid Neoplasms|Neuroendocrine Tumors|Cholangiocarcinoma|Salivary Gland Neoplasms|Head and Neck Neoplasms|Thyroid Cancer Papillary|Lymphoma Large-Cell Anaplastic|Neoplasms by Site|Respiratory Tract Neoplasms|Thoracic Neoplasms|Respiratory Tract Diseases|Carcinoma Bronchogenic|Bronchial Neoplasms|Intestinal Neoplasms|Gastrointestinal Neoplasms|Digestive System Neoplasms|Digestive System Diseases|Gastrointestinal Diseases|Colonic Diseases|Intestinal Diseases|Central Nervous System Hoffmann-La Roche May 24 2021 Phase 2
NCT04111705 Recruiting Drug: Lorlatinib Non Small Cell Lung Cancer Metastatic Intergroupe Francophone de Cancerologie Thoracique August 5 2020 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID