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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
5mg	RMB 1421.96	现货
50mg	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

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	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=
NCI-H3122	NVOwU3U1SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MkHmO\|IhcHK\|		M{n1S2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg{OTJ{IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJxQ1PLMVgh[XO\|YYmsJGlEPTBiPTCwMlAyPzRizszNMi=>	MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF\|MUC2Okc,OjdzM{GwOlY9N2F-
SUP-M2	NV\nc5VZSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		M{\nSlczKGi{cx?=		NWK3SFU{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTWXAuVTJiY3XscJMh[W[2ZYKgO\|IhcHK\|IHL5JHNTSi:FQ1utPEBie3OjeTygTWM2OCB;IECuNFE4QSEQvF2u	NELMS\|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{GzNVA3Pid-MkexN\|ExPjZ:L3G+
NCI-H3122	M3\qbWZ2dmO2aX;uJIF{e2G7		NWrReZRmPzJiaILz		NVXQbmZ5UW6qaXLpeIlwdiCxZjDBUGsh\XiycnXzd4VlKGmwIHj1cYFvKE6FST3IN\|EzOiClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDTVmIwS0ONLUigZZN{[XluIFnDOVAhRSByLkCxPUDPxE1w	MkXHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzM{GwOlYoRjJ5MUOxNFY3RC:jPh?=
NCI-H3122	MXLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		MknWO\|IhcHK\|		MkHsRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDBUGsu\GWyZX7k[Y51KGi3bXHuJG5EUS2KM{GyNkBk\WyuczDh[pRmeiB5MjDodpMtKEmFNUCgQUAxNjBzOTFOwG0v	NIfob5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkS3Olc1QSd-Mk[0O\|Y4PDl:L3G+
SU-DHL1	MmnzRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		Mkm3O\|IhcHK\|		NE\hU2dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPVMWRJVDFiY3XscJMh[W[2ZYKgO\|IhcHK\|IHL5JHNTSi:FQ1utPEBie3OjeTygTWM2OCB;IECuNFIxPSEQvF2u	MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF\|MUC2Okc,OjdzM{GwOlY9N2F-
NIH/3T3	NWX1PJRmSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		M{ixNlczKGi{cx?=		MnfjRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDtc5V{\SCQSVivN3Q{KGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKEWPTEStRWxMKGGodHXyJFczKGi{czDifUBUWkJxQ1PLMVgh[XO\|YYmsJGlEPTBiPTCwMlA{OjNizszNMi=>	MkDCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzM{GwOlYoRjJ5MUOxNFY3RC:jPh?=
Ba/F3	NUS2THpOTnWwY4Tpc44h[XO\|YYm=		NH7XNos4OiCqcoO=		MlrjTY5pcWKrdHnvckBw\iCHTVy0MWFNUyBzMUWxWIlveyCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSmFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiSVO1NEA:KDBwMEeyJO69VS5?	MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
Ba/F3	MYLGeY5kfGmxbjDhd5NigQ>?		NXPm[JFVPzJiaILz		M2DubGlvcGmkaYTpc44hd2ZiRV3MOE1CVEtiTEGxPVZOKG23dHHueEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCvb4Xz[UBD[S:IMzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCLQ{WwJF0hOC5yOTFOwG0v	Ml7GQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
NIH/3T3	NVXGUFFESW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MXG3NkBpenN?		Mk\4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDtc5V{\SCQSVivN3Q{KGOnbHzzJIV5eHKnc4PpcochTU2OND3BUGshVDFzOU[gcZV1[W62IHHmeIVzKDd{IHjyd{BjgSCVUlKvR2NMNThiYYPzZZktKEmFNUCgQUAxNjF\|MjFOwG0v	NFjiRlY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{GzNVA3Pid-MkexN\|ExPjZ:L3G+
Ba/F3	NW[3N5o{TnWwY4Tpc44h[XO\|YYm=		NVvQR\|NRPzJiaILz		NUPNemJxUW6qaXLpeIlwdiCxZjDFUWw1NUGOSzDMNVE2OlJibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIH3veZNmKEKjL1[zJINmdGy\|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSCPVGOgZZN{[XluIFnDOVAhRSByLkG2PUDPxE1w	M2PRb\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
Ba/F3	NUP0TldUTnWwY4Tpc44h[XO\|YYm=		NIrCXVE4OiCqcoO=		NV:ycVk2UW6qaXLpeIlwdiCxZjDFUWw1NUGOSzDHNVIxOlJibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIH3veZNmKEKjL1[zJINmdGy\|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSCPVGOgZZN{[XluIFnDOVAhRSByLkKwO{DPxE1w	MmPoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
DFCI114	MW\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		M4HPUlczKGi{cx?=		NHPpcG5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFTGR2kyOTRiY3XscJMh\XiycnXzd4lv\yCHTVy0MWFNUyCJMUK2PWEhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKEy3bXnu[ZNk\W62IFPlcIwhXmmjYnnsbZR6KEG\|c3H5MEBGSzVyIE2gNE4zODdizszNMi=>	NXzkVWpPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OlgzQDlpPkK2OVY5Ojh7PD;hQi=>
CHLA20	Moj1RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		M1yyNFczKGi{cx?=		MlTERY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCFSFzBNlAh[2WubIOg[ZhxemW\|c3nu[{BGVUx2LVHMT{BTOTJ5NWGgcZV1[W62IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJGx2dWmwZYPj[Y51KEOnbHygWoli[mmuaYT5JGF{e2G7LDDFR\|UxKD1iMD60N{DPxE1w	MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
Kelly	MVjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		M1LzVVczKGi{cx?=		MUnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEunbHz5JINmdGy\|IHX4dJJme3OrbnegSW1NPC2DTFugSlEyPzSOIH31eIFvfCCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDMeY1qdmW\|Y3XueEBE\WyuIG\pZYJqdGm2eTDBd5NigSxiRVO1NEA:KDBwNEO0JO69VS5?	NEf4PY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
DFCI76	M3nrSmFvfGmycn;sbYZmemG2aY\lJIF{e2G7		NYfWNIRxPzJiaILz		M1TIUWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRF\DTVc3KGOnbHzzJIV5eHKnc4PpcochTU2OND3BUGshVDFzNULSJI12fGGwdDDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BNfW2rbnXzZ4VvfCCFZXzsJHZq[WKrbHn0fUBCe3OjeTygSWM2OCB;IECuOVEyKM7:TT6=	MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
LAN5	MYfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		NH7idFY4OiCqcoO=		M3HIN2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTFHOOUBk\WyuczDlfJBz\XO\|aX7nJGVOVDRvQVzLJHIyOjd3UTDteZRidnRiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gUJVucW6nc3PlcpQhS2WubDDWbYFjcWyrdImgRZN{[XluIFXDOVAhRSByLk[xO{DPxE1w	MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
SMS-KCNR	NH22NHBCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NIHZbnA4OiCqcoO=		MXXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOPUz3LR25TKGOnbHzzJIV5eHKnc4PpcochTU2OND3BUGshWjF{N{XRJI12fGGwdDDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BNfW2rbnXzZ4VvfCCFZXzsJHZq[WKrbHn0fUBCe3OjeTygSWM2OCB;IECuO\|Y2KM7:TT6=	NFLwOY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
SK-N-SH	NWDPPGd{SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		NGDBN3Y4OiCqcoO=		M2fYNmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utUk1UUCClZXzsd{BmgHC{ZYPzbY5oKEWPTEStRWxMKEZzMUe0UEBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hVHWvaX7ld4NmdnRiQ3XscEBXcWGkaXzpeJkhSXO\|YYmsJGVEPTBiPTCwMlg4OiEQvF2u	NFPqbpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
SH-SY5Y	MmLuRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NVfIRWszPzJiaILz		NFTiTWtCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPIMXN[PVliY3XscJMh\XiycnXzd4lv\yCHTVy0MWFNUyCIMUG3OGwhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKEy3bXnu[ZNk\W62IFPlcIwhXmmjYnnsbZR6KEG\|c3H5MEBGSzVyIE2gNU4yPSEQvF2u	M2q2[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
SK-N-BE(2)	NYLqclgzSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		NEXlNlU4OiCqcoO=		MlvaRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCVSz3OMWJGMDJrIHPlcIx{KGW6cILld5Nqdmdid3ns[EB1gXCnIFXNUFQuSUyNIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJGx2dWmwZYPj[Y51KEOnbHygWoli[mmuaYT5JGF{e2G7LDDFR\|UxKD1iMT61OVQh\|ryPLh?=	MoXPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
LAN1	MljxRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NEDMW2c4OiCqcoO=		M1y2XWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTFHONUBk\WyuczDlfJBz\XO\|aX7nJGVOVDRvQVzLJGYyOTd2TDDteZRidnRiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gUJVucW6nc3PlcpQhS2WubDDWbYFjcWyrdImgRZN{[XluIFXDOVAhRSB{LkCwOEDPxE1w	NHflO\|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
SK-N-AS	NUTqV2ljSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		NWLrW\|VpPzJiaILz		NFTjPGFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMW4uSVNiY3XscJMh\XiycnXzd4lv\yC5aXzkJJR6eGViRV3MOE1CVEtiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gUJVucW6nc3PlcpQhS2WubDDWbYFjcWyrdImgRZN{[XluIFXDOVAhRSB{LkGzPUDPxE1w	NI\5Wmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
SK-N-FI	MlK0RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		M2\FV\|czKGi{cx?=		MnjoRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCVSz3OMWZKKGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKEWPTEStRWxMKGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIFz1cYlv\XOlZX70JGNmdGxiVnnhZoltcXS7IFHzd4F6NCCHQ{WwJF0hOi52MEGg{txONg>?	MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
NIH/3T3	NGrLTYFCdnSrdIXtc5Ih[XO\|YYm=	M17TPFUxKG2pL3vn	NYLHSI1rOTBiZHH5dy=>		NEm0R49CdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBud3W\|ZTDOTWgwO1R\|IHPlcIx{KGW6cILld5NqdmdiRV3MOE1CVEtiTEGxPVZOKG23dHHueEB5\W6xZ4Lh[pRm\CCrbjDueYRmKG2xdYPlJIF{e2W\|c3XkJIF{KHS3bX;yJJN1[XOrczDheEA2OCCvZz;r[{wheG9icXSgZYRucW6rc4TldoVlKG[xcjCxNEBl[Xm\|	NHW2Rnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{GzNVA3Pid-MkexN\|ExPjZ:L3G+
NIH/3T3	NXjkVXEzSW62aYT1cY9zKGG\|c3H5	MWC1NEBu\y:tZx?=	MVqxNEBl[Xm\|		M3\vfGFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIF7JTE8{XDNiY3XscJMh\XiycnXzd4lv\yCHTVy0MWFNUyCOMUG5Om0hdXW2YX70JJhmdm:pcnHmeIVlKGmwIH71[IUhdW:3c3WgZZN{\XO\|ZXSgZZMheGG{dHnhcEB1fW2xcjDy[Ydz\XO\|aX;uJIF1KDVyIH3nM4toNCCybzDx[EBi\G2rbnnzeIVz\WRiZn;yJFExKGSjeYO=	NGO1bXI9[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 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]

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

参考文献	[1] Sakamoto H, et al. Cancer Cell. 2011, 19(5), 679-690. [2] Kinoshita K, et al. Bioorg Med Chem. 2012, 20(3), 1271-1280.

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
储存条件	2年	-80°C	溶于溶剂

Download Alectinib (CH5424802) SDF

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 μL 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

%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，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。

体内配方配制方法：取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
=	×	×

稀释计算器分子量计算器

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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