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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价格

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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59篇：

Nature, 2021, 600(7888):319-323

PubMed: 34819663 ( click the link to review the publication )

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 )

NPJ Precis Oncol, 2022, 6(1):5

PubMed: 35042943 ( click the link to review the publication )

Thorac Cancer, 2022, 10.1111/1759-7714.14372

PubMed: 35253386 ( click the link to review the publication )

mBio, 2021, 12(6):e0322821

PubMed: 34933455 ( 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 )

Mol Cancer Res, 2017, 15(1):106-114

PubMed: 27707887 ( 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

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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 )

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

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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	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=
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LAN1	MlLtRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		M37zeVczKGi{cx?=		NEPWWW9CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzBUlEh[2WubIOg[ZhxemW\|c3nu[{BGVUx2LVHMT{BHOTF5NFygcZV1[W62IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJGx2dWmwZYPj[Y51KEOnbHygWoli[mmuaYT5JGF{e2G7LDDFR\|UxKD1iMj6wNFQh\|ryPLh?=	MmexQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
SK-N-AS	MljNRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		MVy3NkBpenN?		NWPDTmRlSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1PNUGVIHPlcIx{KGW6cILld5Nqdmdid3ns[EB1gXCnIFXNUFQuSUyNIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJGx2dWmwZYPj[Y51KEOnbHygWoli[mmuaYT5JGF{e2G7LDDFR\|UxKD1iMj6xN\|kh\|ryPLh?=	NVizWHhURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OlgzQDlpPkK2OVY5Ojh7PD;hQi=>
SK-N-FI	MojZRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NFvU[VE4OiCqcoO=		NVPhTHdxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1PNU[LIHPlcIx{KGW6cILld5Nqdmdid3ns[EB1gXCnIFXNUFQuSUyNIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJGx2dWmwZYPj[Y51KEOnbHygWoli[mmuaYT5JGF{e2G7LDDFR\|UxKD1iMj60NFEh\|ryPLh?=	NYHoN2lQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OlgzQDlpPkK2OVY5Ojh7PD;hQi=>
NIH/3T3	MnfxRY51cXS3bX;yJIF{e2G7	NULKTVlwPTBibXevb4c>	NVvWTlBkOTBiZHH5dy=>		MVjBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6\|dDDtc5V{\SCQSVivN3Q{KGOnbHzzJIV5eHKnc4PpcochTU2OND3BUGshVDFzOU\NJI12fGGwdDD4[Y5w\3KjZoTl[EBqdiCwdXTlJI1wfXOnIHHzd4V{e2WmIHHzJJR2dW:{IIP0ZZNqeyCjdDC1NEBu\y:tZzygdI8heWRiYXTtbY5qe3SncnXkJIZweiBzMDDkZZl{	NEjqVIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{GzNVA3Pid-MkexN\|ExPjZ:L3G+
NIH/3T3	NWT5SHROSW62aYT1cY9zKGG\|c3H5	NEn5eWM2OCCvZz;r[y=>	M{LIeFExKGSjeYO=		NEHnXIFCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBud3W\|ZTDOTWgwO1R\|IHPlcIx{KGW6cILld5NqdmdiRV3MOE1CVEtiTEGxPVZOKG23dHHueEB5\W6xZ4Lh[pRm\CCrbjDueYRmKG2xdYPlJIF{e2W\|c3XkJIF{KHCjcoTpZYwhfHWvb4KgdoVoemW\|c3nvckBifCB3MDDt[{9s\yxicH:gdYQh[WSvaX7pd5RmemWmIH\vdkAyOCCmYYnz	NIPUfo09[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 2022-01-17)

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

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59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 2022-01-17)

技术支持

ALK Signaling Pathway Map

ALK Inhibitors with Unique Features

相关ALK产品