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。

规格

价格

库存

购买数量

5mg	RMB 1421.96	现货
10mg	RMB 2229.22	现货
50mg	RMB 6315.15	现货
100mg	RMB 10401.3	现货
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客户使用Selleck生产的Alectinib (CH5424802)发表文献55篇：

Cell, 2020, 182(5):1232-1251.e22

PubMed: 32822576 ( click the link to review the publication )

Cancer Discov, 2015, 10.1158/2159-8290.CD-15-0913

PubMed: 26566875 ( click the link to review the publication )

Cancer Lett, 2021, 522:119-128

PubMed: 34534615 ( click the link to review the publication )

Mol Cancer Ther, 2021, molcanther.0965.2020

PubMed: 34158345 ( click the link to review the publication )

Mol Cancer Ther, 2021, molcanther.0221.2021

PubMed: 34158340 ( click the link to review the publication )

Cancer Sci, 2021, 112(5):1853-1864

PubMed: 33410241 ( click the link to review the publication )

Sci Rep, 2021, 11(1):9011

PubMed: 33907223 ( click the link to review the publication )

EMBO Mol Med, 2020, e11099

PubMed: 32558295 ( click the link to review the publication )

Cell Death Dis, 2020, 11(2):111

PubMed: 32041944 ( click the link to review the publication )

Cancer Discov, 2020, 1 pii: CD-19-1030

PubMed: 32238360 ( click the link to review the publication )

Lung Cancer, 2020, 144:20-29

PubMed: 32353632 ( click the link to review the publication )

Bosn J Basic Med Sci, 2020, 10.17305/bjbms.2020.5066

PubMed: 33091333 ( click the link to review the publication )

Anticancer Res, 2020, 40(3):1395-1403

PubMed: 32132036 ( click the link to review the publication )

J Neurooncol, 2020, 146(1):9-23

PubMed: 31776900 ( click the link to review the publication )

Mol Pharmacol, 2020, 97(2):123-131

PubMed: 31734646 ( click the link to review the publication )

Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-1104

PubMed: 31585938 ( click the link to review the publication )

Oncogene, 2019, 101038/s41388-019-1136-4

PubMed: 31804622 ( click the link to review the publication )

Front Oncol, 2019, 9:579

PubMed: 31334113 ( click the link to review the publication )

Sci Rep, 2019,

PubMed: 31882684 ( click the link to review the publication )

Drug Metab Dispos, 2019, 47(7):699-709

PubMed: 31068367 ( click the link to review the publication )

Invest New Drugs, 2019, 10.1007/s10637-019-00802-7

PubMed: 31177400 ( click the link to review the publication )

Cancer Res Treat, 2019, 51(3):1231-1240

PubMed: 30653748 ( click the link to review the publication )

Transl Oncol, 2019, 12(1):116-121

PubMed: 30290287 ( click the link to review the publication )

Anticancer Res, 2019, 39(7):3579-3584

PubMed: 31262882 ( click the link to review the publication )
Cancer Immunol Res, 2019,

PubMed: 31540894 ( click the link to review the publication )

Oncotarget, 2019, 10(48):4937-4950

PubMed: 31452835 ( click the link to review the publication )

J Thorac Oncol, 2018, 13(7):926-937

PubMed: 29596910 ( click the link to review the publication )

Clin Cancer Res, 2018, 24(12):2732-2739

PubMed: 29559559 ( click the link to review the publication )

Cancer Res, 2018, 78(24):6866-6880

PubMed: 30322862 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(11-:2271-2284

PubMed: 30135214 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(1):222-231

PubMed: 29054983 ( click the link to review the publication )

Anticancer Drugs, 2018, 29(10):935-943

PubMed: 30074936 ( click the link to review the publication )

Sci Adv, 2018, 4(9):eaar3938

PubMed: 30258985 ( click the link to review the publication )

Oncotarget, 2018, 9(43-:27242-27255

PubMed: 29930762 ( click the link to review the publication )

Sci Transl Med, 2017, 14;9(394):eaah6144

PubMed: 28615362 ( click the link to review the publication )

Arch Toxicol, 2017, 91(8):2921-2938

PubMed: 28032146 ( click the link to review the publication )

Oncologist, 2017, 22(2):158-164

PubMed: 28167572 ( click the link to review the publication )

Cancer Sci, 2017,

PubMed: 27783866 ( click the link to review the publication )

Oncotarget, 2017, 8(43):73766-73773

PubMed: 29088743 ( click the link to review the publication )

Oncotarget, 2017, 8(35):58771-58780

PubMed: 28938595 ( click the link to review the publication )

Oncogene, 2016, 35(29):3854-3865

PubMed: 26657151 ( click the link to review the publication )

Sci Signal, 2016, 9(450):rs12

PubMed: 27811184 ( click the link to review the publication )

Mol Oncol, 2016, 10(4):601-9

PubMed: 26639656 ( click the link to review the publication )

Oncotarget, 2016, 7(17):23715-29

PubMed: 27009859 ( click the link to review the publication )

Oncotarget, 2016, 7(45):72886-72897

PubMed: 27662658 ( click the link to review the publication )

Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-15-0016

PubMed: 26019170 ( click the link to review the publication )

Mol Oncol, 2015, 10.1016/j.molonc.2015.11.007

PubMed: 26639656 ( click the link to review the publication )

Cancer Sci, 2015, 106(3):244-52

PubMed: 25581823 ( click the link to review the publication )
Mol Cancer Res, 2015, 13(4):775-83

PubMed: 25421750 ( click the link to review the publication )

Int J Oncol, 2015, 46(3):1025-30

PubMed: 25502629 ( click the link to review the publication )

Cancer Med, 2015, 10.1002/cam4.413

PubMed: 25727400 ( click the link to review the publication )

Oncotarget, 2015, 6(8):5720-34

PubMed: 25749034 ( click the link to review the publication )

Int J Oncol, 2014, 45(4):1430-6

PubMed: 25096400 ( click the link to review the publication )

Oncotarget, 2014, 5(13):4920-8

PubMed: 24952482 ( click the link to review the publication )

Br J Pharmacol, 2012, 166(3):858-76

PubMed: 22250956 ( click the link to review the publication )

产品安全说明书

ALK抑制剂选择性比较

生物活性

产品描述

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，K_i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-
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LAN1	NEW2VIxCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		M2XLWlczKGi{cx?=		NHjsclhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzBUlEh[2WubIOg[ZhxemW\|c3nu[{BGVUx2LVHMT{BHOTF5NFygcZV1[W62IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJGx2dWmwZYPj[Y51KEOnbHygWoli[mmuaYT5JGF{e2G7LDDFR\|UxKD1iMj6wNFQh\|ryPLh?=	MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
SK-N-AS	MmX6RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		MoHmO\|IhcHK\|		M3vWTWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utUk1CWyClZXzsd{BmgHC{ZYPzbY5oKHerbHSgeJlx\SCHTVy0MWFNUyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDMeY1qdmW\|Y3XueEBE\WyuIG\pZYJqdGm2eTDBd5NigSxiRVO1NEA:KDJwMUO5JO69VS5?	NHjtTGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
SK-N-FI	MnnORY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NUDT[I92PzJiaILz		NXrwW4pWSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1PNU[LIHPlcIx{KGW6cILld5Nqdmdid3ns[EB1gXCnIFXNUFQuSUyNIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJGx2dWmwZYPj[Y51KEOnbHygWoli[mmuaYT5JGF{e2G7LDDFR\|UxKD1iMj60NFEh\|ryPLh?=	MljOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
NIH/3T3	M1HzUWFvfGm2dX3vdkBie3OjeR?=	MWi1NEBu\y:tZx?=	MmnoNVAh\GG7cx?=		NYrObHNtSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhdW:3c3WgUmlJNzOWMzDj[YxteyCneIDy[ZN{cW6pIFXNUFQuSUyNIFyxNVk3VSCvdYThcpQhgGWwb3fyZYZ1\WRiaX6gcpVl\SCvb4Xz[UBie3Onc4Pl[EBieyC2dX3vdkB{fGG\|aYOgZZQhPTBibXevb4ctKHCxIIHkJIFldWmwaYP0[ZJm\CCob4KgNVAh\GG7cx?=	NF25bmY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{GzNVA3Pid-MkexN\|ExPjZ:L3G+
NIH/3T3	M1jLT2FvfGm2dX3vdkBie3OjeR?=	NWPvOYRtPTBibXevb4c>	MXWxNEBl[Xm\|		MV3BcpRqfHWvb4KgZYN1cX[rdImgZYdicW6\|dDDtc5V{\SCQSVivN3Q{KGOnbHzzJIV5eHKnc4PpcochTU2OND3BUGshVDFzOU\NJI12fGGwdDD4[Y5w\3KjZoTl[EBqdiCwdXTlJI1wfXOnIHHzd4V{e2WmIHHzJJBienSrYXygeJVud3JicnXndoV{e2mxbjDheEA2OCCvZz;r[{wheG9icXSgZYRucW6rc4TldoVlKG[xcjCxNEBl[Xm\|	NFz0PYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{GzNVA3Pid-MkexN\|ExPjZ:L3G+

... 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 Clin Cancer Res 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 Cancer Lett 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 Clin Cancer Res 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 Neoplasia 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 Clin Cancer Res (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]

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)

参考文献

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 Download Alectinib (CH5424802) SDF

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
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

每只动物给药体积

动物数量

只

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，注：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：取 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。

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。

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

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
初始浓度:
稀释倍数:

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

通过输入化合物的化学式来计算其分子量：

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 (data from https://clinicaltrials.gov, updated on 2021-09-06)

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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

ALK Signaling Pathway Map

ALK Inhibitors with Unique Features

非特异性的ALK抑制剂

GSK1838705A : IGF-1R, IC50=2.0 nM; IR, IC50=1.6 nM, ALK, IC50=0.5 nM.
活性最高的ALK抑制剂

Ceritinib (LDK378) : ALK, IC50=0.2 nM.
FDA批准的ALK抑制剂

Crizotinib (PF-02341066) : Approved by FDA for non-small cell lung carcinoma (NSCLC).
最新的ALK抑制剂

ASP3026 ^New : Novel and selective inhibitor for ALK with IC50 of 3.5 nM.

研究领域

产品类型

定制您的化合物库

Alectinib (CH5424802)

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

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)

参考文献

溶解度 (25°C)

化学数据 Download Alectinib (CH5424802) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-09-06)

技术支持

ALK Signaling Pathway Map

ALK Inhibitors with Unique Features

相关ALK产品