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59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 NW\BO2dFU2mwYYPlJIF{e2G7 NYf3UYdChjFizszN NEnjcYNxemW4ZX70d{BifXSxcHjvd5Bpd3K7bHH0bY9vKG:oIFHMTy=> MlzNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
KARPAS-299 NWjFbJQ5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUf+NVAh|ryP NGPKcINKSzVyPUOgcm0> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
SR MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1rid54yOCEQvF2= NGnxeHNKSzVyPU[uPUBvVQ>? NIO3e289[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
HDLM-2 NUDFb|RuT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MofPglExKM7:TR?= MUfJR|UxRjFyLECwNEBvVQ>? MlTEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
NB-1 MnG3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWP+NVAh|ryP NIjFb|JKSzVyPUSuOUBvVQ>? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
KELLY M{f3XGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYT+NVAh|ryP MWTJR|UxRTZ{IH7N NFv1T4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
SK-N-FI NXLyclRJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVqwNIp5hjFyIN88US=> MmDhTWM2OD5zMDywNFAhdk1? MnLQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
NCI-H2228 NH;Me5FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUP+NVAh|ryP NVvwWoc3UUN3ME21N{BvVQ>? M3zmT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
Calu-3 MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXHVbnhshjFyIN88US=> NWLRW2pIUUN3ME2+NVAtODByIH7N NETl[Yg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
PC-1 Mnn0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYLWTVREhjFyIN88US=> MlqwTWM2OD5zMDywNFAhdk1? NXLsWVExRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
NCI-H23 MkW5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmHFglExKM7:TR?= NYXZ[nhwUUN3ME2zOlAxKG6P M3nJ[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
Calu-1 MUfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIrwSW9,OTBizszN NGPFV2VKSzVyPkGwMFAxOCCwTR?= MkSzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
NCI-H2009 NV3YdoRMT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NETWdVB,OTBizszN MoHhTWM2OD5zMDywNFAhdk1? NHzBTIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
NCI-H1993 MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYT+NVAh|ryP MYfJR|UxRjFyLECwNEBvVQ>? NVvkfoZlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
MKN-45 M2DOZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Ml3PglExKM7:TR?= MoXYTWM2OD5zMDywNFAhdk1? NIHIdWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
SNU-5 MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MY\+NVAh|ryP NVrIUZFtUUN3ME2xPFAxKG6P M3zsfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
KATO-III M{m3T2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2T5Sp4yOCEQvF2= MVjJR|UxRTd7MECgcm0> NGHMZWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
SK-BR-3 MlS4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1zvRp4yOCEQvF2= NHXNV3RKSzVyPkGwMFAxOCCwTR?= NXW2dllJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
BT-483 MkfES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWjNNG5GhjFyIN88US=> NXz2fVkxUUN3ME6xNEwxODBibl2= NUTtdGZbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
PC-3 NHWzcJBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFHJToN,OTBizszN M3TZTGlEPTB-MUCsNFAxKG6P NU\4b3JORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
22Rv1 NWm4RYVFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYX+NVAh|ryP M2PnbGlEPTB-MUCsNFAxKG6P MmjuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
U-87 MG NVniU5hXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1vpcZ4yOCEQvF2= NGnteJBKSzVyPkGwMFAxOCCwTR?= NYrGTW9uRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
H3122 M3P4Xmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NV\EZ2djhjFyIN88US=> MYXJR|UxRTN|IH7N NHPWSnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC5OlQxOCd-MkWwPVY1ODB:L3G+
LC-2/ad NEHPdW5CeG:ydH;zbZMh[XO|YYm= NVTPcZZNhjFizszN MoLzSG1UVw>? NWn1SY9RcW6mdXPld{BieG:ydH;zbZM> MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN2OUOwO{c,OjV|NEmzNFc9N2F-
LC-2/ad M3rUc2Z2dmO2aX;uJIF{e2G7 MlzEglEh|ryP MnH0SG1UVw>? NFnVSItqdmirYnn0d{B1cGViTVHQT{B{cWewYXzpcocheGG2aIfhfS=> M{DNXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{S5N|A4Lz5{NUO0PVMxPzxxYU6=
Ba/F3 MkDJSpVv[3Srb36gZZN{[Xl? NVrMeJhrhjFizszN MnvOSG1UVw>? NFLVTXF{fXCycnXzd4V{KHCqb4PwbI9zgWyjdHnvckBw\iCHUlugZY5lKGmwY4LlZZNmeyC2aHWgZYJ2dmSjbnPlJI9nKEKLTR?= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN2OUOwO{c,OjV|NEmzNFc9N2F-
SNU-2535 NEHzRYlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXzhV2pQhjFyIN88US=> NFr1OZRKSzVyPUOzMlEhdk1? M3X1dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OES5OlM4Lz5{Nki0PVY{PzxxYU6=
SNU-2535 M{fDbmtqdmG|ZTDhd5NigQ>? NYq5WIZQhjFizszN M2DSUolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVzLJIFv\CCrdIOg[I94dnO2cnXhcUBud2ynY4Xs[ZMhTVKNMT:yJIFv\CCDS2S= M3zNRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OES5OlM4Lz5{Nki0PVY{PzxxYU6=
Ba/F3 MW\GeY5kfGmxbjDhd5NigQ>? MWe3NkBpenN? NW\P[Yo2UW6qaXLpeIlwdiCxZjDFUWw1NUGOSzDDNVE2PllibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIH3veZNmKEKjL1[zJINmdGy|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSCPVGOgZZN{[XluIFnDOVAhRSByLkCwNkDPxE1w Ml7XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
Ba/F3 MV;GeY5kfGmxbjDhd5NigQ>? M{KyRlczKGi{cx?= MVrJcohq[mm2aX;uJI9nKEWPTEStRWxMKFNzMkC2XUBufXSjboSgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hdW:3c3WgRoEwTjNiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JG1VWyCjc4PhfUwhUUN3MDC9JFAvODB{IN88UU4> NIfq[VM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
Ba/F3 NVLiVmdiTnWwY4Tpc44h[XO|YYm= MVO3NkBpenN? M4HIe2lvcGmkaYTpc44hd2Zid3ns[EB1gXCnIFXNUFQuSUyNIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJI1wfXOnIFLhM2Y{KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGlEPTBiPTCwMlAxOiEQvF2u MnW3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
KARPAS299 M{j4VGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NXXsVYdbQTZiaILz MYfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEuDUmDBV|I6QSClZXzsd{Bi\nSncjC5OkBpenNiYomgZ4VtdCClb4XueIlv\yCjc4PhfUwhUUN3MDC9JFAvODB|IN88UU4> NEm5doE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKyOVkyPyd-MkKyNlU6OTd:L3G+
Ba/F3 NIXHenZHfW6ldHnvckBie3OjeR?= MmPKO|IhcHK| MWDJcohq[mm2aX;uJI9nKEWPTEStRWxMKEZzMUe0UEBufXSjboSgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hdW:3c3WgRoEwTjNiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JG1VWyCjc4PhfUwhUUN3MDC9JFAvODB|IN88UU4> MoLQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
Ba/F3 NGP6dZpHfW6ldHnvckBie3OjeR?= NXPOWFNPPzJiaILz NF2xUYJKdmirYnn0bY9vKG:oIFXNUFQuSUyNIFexNlY6SSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSmFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiSVO1NEA:KDBwMEC5JO69VS5? MnP0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
NCI-H3122 MWPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M4LIPFczKGi{cx?= NVHlWGlkSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDNzMkKgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gUJVucW6nc3PlcpQhS2WubDDWbYFjcWyrdImgRZN{[XluIFXDOVAhRSByLkCwPUDPxE1w M4\jSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
KARPAS299 MWfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NE\hVVY4OiCqcoO= MoWxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNQWLQRXMzQTliY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSi:FQ1utPEBie3OjeTygTWM2OCB;IECuNFE2KM7:TT6= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF|MUC2Okc,OjdzM{GwOlY9N2F-
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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 Recruiting Drug: Lortlatinib 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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操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID