Alectinib (CH5424802)

目录号:S2762 别名: AF-802, RG-7853,CH5424802 中文名称:阿来替尼,艾乐替尼

仅限科研使用

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。

Alectinib (CH5424802) Chemical Structure

CAS: 1256580-46-7

规格 价格 库存 购买数量
RMB 1421.96 现货
RMB 6315.15 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Alectinib (CH5424802)发表文献63篇:

产品安全说明书

ALK抑制剂选择性比较

相关ALK产品

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 MUfLbY5ie2ViYYPzZZk> NGjpOGV,OSEQvF2= NUTEfJF1eHKndnXueJMh[XW2b4Doc5NxcG:{eXzheIlwdiCxZjDBUGs> MkfSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
KARPAS-299 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYX+NVAh|ryP NFjIRohKSzVyPUOgcm0> MnjiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
SR NUnlT|V4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGO2foN,OTBizszN MlK4TWM2OD14Lkmgcm0> NF;5N4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
HDLM-2 MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGT2fFl,OTBizszN Ml7wTWM2OD5zMDywNFAhdk1? M1zRbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
NB-1 NYHUZpF1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYf+NVAh|ryP MoDDTWM2OD12LkWgcm0> NFP6cVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
KELLY MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVjzWIp[hjFyIN88US=> MonzTWM2OD14MjDuUS=> M3PBSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
SK-N-FI MmPXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWP+NVAh|ryP NXrmTW43UUN3ME6xNEwxODBibl2= MnTZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
NCI-H2228 NIC0c5pIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NX7JVG9WhjFyIN88US=> M2W4NmlEPTB;NUOgcm0> MnHVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
Calu-3 Ml3KS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX\zeZFihjFyIN88US=> MmPlTWM2OD1-MUCsNFAxKG6P MkW3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
PC-1 NVHZUJBUT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXr+NVAh|ryP M1\BemlEPTB-MUCsNFAxKG6P NULHRohORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
NCI-H23 NVrFXIpZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXX+NVAh|ryP MVHJR|UxRTN4MECgcm0> NHLLUJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
Calu-1 NX;p[FVUT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mnv4glExKM7:TR?= NHHQemxKSzVyPkGwMFAxOCCwTR?= NV;6PYpuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
NCI-H2009 M1HkZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4Lzep4yOCEQvF2= NWrQOIJiUUN3ME6xNEwxODBibl2= Mm\LQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
NCI-H1993 MofhS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2frdZ4yOCEQvF2= MljoTWM2OD5zMDywNFAhdk1? MoTnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
MKN-45 NVfFZolXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NXXBdYpKhjFyIN88US=> MULJR|UxRjFyLECwNEBvVQ>? MljvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
SNU-5 M2Wycmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXH+NVAh|ryP M1XJNWlEPTB;MUiwNEBvVQ>? NF[xXHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
KATO-III NGnFeGRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3LZVJ4yOCEQvF2= M1ToSWlEPTB;N{mwNEBvVQ>? M4jH[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
SK-BR-3 MlnjS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYX+NVAh|ryP NXHXNXZsUUN3ME6xNEwxODBibl2= NUC2NFl4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
BT-483 NI\OPHJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{nBS54yOCEQvF2= NX63N242UUN3ME6xNEwxODBibl2= NFPORpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
PC-3 M1LLcWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MX\+NVAh|ryP NXfyTndxUUN3ME6xNEwxODBibl2= M2jacVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
22Rv1 NF6yO3ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWfxTVJFhjFyIN88US=> NEe5ZppKSzVyPkGwMFAxOCCwTR?= MlfGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
U-87 MG MoPBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MV\+NVAh|ryP MXrJR|UxRjFyLECwNEBvVQ>? NX3veldqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
H3122 NYS0XFFrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEHZcJJ,OTBizszN M2\vT2lEPTB;M{Ogcm0> MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB7NkSwNEc,OjVyOU[0NFA9N2F-
LC-2/ad MVrBdI9xfG:|aYOgZZN{[Xl? MlT5glEh|ryP NWflT3pzTE2VTx?= MoXybY5lfWOnczDhdI9xfG:|aYO= M3jvOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{S5N|A4Lz5{NUO0PVMxPzxxYU6=
LC-2/ad MWLGeY5kfGmxbjDhd5NigQ>? MWr+NUDPxE1? NYnpb4xmTE2VTx?= M1HzUolvcGmkaYTzJJRp\SCPQWDLJJNq\26jbHnu[{Bx[XSqd3H5 NGfTenc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO0PVMxPyd-MkWzOFk{ODd:L3G+
Ba/F3 M1LrTmZ2dmO2aX;uJIF{e2G7 M1fqNJ4yKM7:TR?= M{\HVGROW09? NF;2Tm1{fXCycnXzd4V{KHCqb4PwbI9zgWyjdHnvckBw\iCHUlugZY5lKGmwY4LlZZNmeyC2aHWgZYJ2dmSjbnPlJI9nKEKLTR?= NVXjS|VnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOFk{ODdpPkK1N|Q6OzB5PD;hQi=>
SNU-2535 NGrTdplIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFX6ZY9,OTBizszN MYPJR|UxRTN|LkGgcm0> NGi5Nlk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki0PVY{Pyd-Mk[4OFk3Ozd:L3G+
SNU-2535 MWTLbY5ie2ViYYPzZZk> MXv+NUDPxE1? NH22[3hqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHMT{BidmRiaYTzJIRwf26|dILlZY0hdW:uZXP1cIV{KEWUS{GvNkBidmRiQVvU MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh2OU[zO{c,OjZ6NEm2N|c9N2F-
Ba/F3 NYnIN2V5TnWwY4Tpc44h[XO|YYm= M3;qXlczKGi{cx?= NIPZXJZKdmirYnn0bY9vKG:oIFXNUFQuSUyNIFOxNVU3YSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSmFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiSVO1NEA:KDBwMECyJO69VS5? MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
Ba/F3 M3XrVGZ2dmO2aX;uJIF{e2G7 NHPUN4Q4OiCqcoO= NUnmUHl5UW6qaXLpeIlwdiCxZjDFUWw1NUGOSzDTNVIxPllibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIH3veZNmKEKjL1[zJINmdGy|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSCPVGOgZZN{[XluIFnDOVAhRSByLkCwNkDPxE1w NWjHO3hORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OlgzQDlpPkK2OVY5Ojh7PD;hQi=>
Ba/F3 MVzGeY5kfGmxbjDhd5NigQ>? MmDwO|IhcHK| NGKyb4JKdmirYnn0bY9vKG:oIIfpcIQhfHmyZTDFUWw1NUGOSzCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBud3W|ZTDCZU9HOyClZXzsd{Bie3Onc4Pl[EBieyClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgUXRUKGG|c3H5MEBKSzVyIE2gNE4xODJizszNMi=> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
KARPAS299 NEDlNW9CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MUe5OkBpenN? MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEuDUmDBV|I6QSClZXzsd{Bi\nSncjC5OkBpenNiYomgZ4VtdCClb4XueIlv\yCjc4PhfUwhUUN3MDC9JFAvODB|IN88UU4> NGnQbog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKyOVkyPyd-MkKyNlU6OTd:L3G+
Ba/F3 M3\DSGZ2dmO2aX;uJIF{e2G7 MlK5O|IhcHK| NFvFW4VKdmirYnn0bY9vKG:oIFXNUFQuSUyNIF[xNVc1VCCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSmFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiSVO1NEA:KDBwMECzJO69VS5? NFHpTpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
Ba/F3 MYTGeY5kfGmxbjDhd5NigQ>? NF7kbno4OiCqcoO= NHjxWpVKdmirYnn0bY9vKG:oIFXNUFQuSUyNIFexNlY6SSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSmFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiSVO1NEA:KDBwMEC5JO69VS5? NU[0VW9URGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OlgzQDlpPkK2OVY5Ojh7PD;hQi=>
NCI-H3122 MoO3RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MVG3NkBpenN? NHi0cGFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOzF{MjDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDMeY1qdmW|Y3XueEBE\WyuIG\pZYJqdGm2eTDBd5NigSxiRVO1NEA:KDBwMEC5JO69VS5? NWDhe4JMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OlgzQDlpPkK2OVY5Ojh7PD;hQi=>
KARPAS299 MVnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NI[1VpQ4OiCqcoO= MlzkRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNQWLQRXMzQTliY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSi:FQ1utPEBie3OjeTygTWM2OCB;IECuNFE2KM7:TT6= M1;kOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUOxNFY3Lz5{N{GzNVA3PjxxYU6=
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Assay
Methods Test Index PMID
Western blot pALK / ALK / pAKT / AKT / pERK / ERK / pS6 / S6 PARP / cleaved PARP / Akt / caspase 3 / Cleaved caspase 3 pROS1 / ROS1 / pSTAT3 / STAT3 p-EGFR Tyr1068 / EGFR / p-HER3 Tyr1222 / HER3 / p-IGF-1R Tyr1135 / IGF-1R 25228534 28455243 25351743 26992917
Growth inhibition assay Cell viability 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]
  • 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]
  • 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。
动物实验:[1]
  • Animal Models: 携带NCI-H2228细胞的 SCID 或裸鼠
  • Dosages: 20 mg/kg
  • Administration: 口服处理

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 482.62
化学式

C30H34N4O2

CAS号 1256580-46-7
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
NCT04774718 Recruiting Drug: Alectinib ALK Fusion-positive Solid or CNS Tumors Hoffmann-La Roche September 14 2021 Phase 1|Phase 2
NCT04979988 Completed 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 Terminated 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

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

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