Alectinib (CH5424802)

For research use only. Not for use in humans.

製品コードS2762 別名：AF-802, RG-7853

CAS No. 1256580-46-7

Alectinib (CH5424802, AF-802, RG-7853) is a potent ALK inhibitor with IC50 of 1.9 nM in cell-free assays, sensitive to L1196M mutation and higher selectivity for ALK than PF-02341066, NVP-TAE684 and PHA-E429.

サイズ

価格(税別)

5mg	JPY 30200
50mg	JPY 129800

最寄りの販売代理店を探す

東京
北海道
東北
北関東
南関東
東海
北信越
近畿
中国
四国
九州

お探しのディーラーが見当たらない場合は直接こちらのメールアドレスまでお問い合わせください：[email protected]

バルク問合せ

代表番号: 03-5615-9297|電子メール：[email protected]|よく尋ねられる質問

文献中Selleckの製品使用例(57)

製品安全説明書

ALK阻害剤の選択性比較

生物活性

製品説明

ターゲット

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

体外試験

The dissociation constant (KD) value of CH5424802 for ALK in an ATP-competitive manner is 2.4 nM. CH5424802 has substantial inhibitory potency against both native ALK and L1196M with K_i of 0.83 nM and 1.56 nM, respectively. CH5424802 prevents autophosphorylation of ALK in NCI-H2228 NSCLC cells expressing EML4-ALK. CH5424802 also suppresses the phosphorylation of STAT3 and AKT, but not of ERK1/2. CH5424802 completely inhibits the phosphorylation of STAT3 at Tyr705. CH5424802 is preferentially efficacious against NCI-H2228 cells expressing EML4-ALK, but not ALK fusion-negative NSCLC cell lines, including HCC827 cells (EGFR exon 19 deletion), A549 cells (KRAS mutant), or NCI-H522 cells (EGFR wild-type, KRAS wild-type, and ALK wild-type) in monolayer culture. CH5424802 elicits an apoptotic marker—caspase-3/7-like activation—in NCI-H2228 spheroid cells. CH5424802 blocks the growth of two lymphoma lines, KARPAS-299 and SR, with NPM-ALK fusion protein but does not influence the growth of an HDLM-2 lymphoma line without ALK fusion. ^[1] CH5424802 displays high target selectivity and the stronger anti-proliferative activity against KARPAS-299. CH5424802 inhibits KAPRAS-299 with an IC50 of 3 nM, and KDR with IC50 of 1.4 μM. The metabolic stability of CH5424802 is very high.^[2]

細胞データ

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
NCI-H2228	NFKwfYdMcW6jc3WgZZN{[Xl?	MV;+NUDPxE1?			MXHwdoV3\W62czDheZRweGixc4Doc5J6dGG2aX;uJI9nKEGOSx?=	NXPzRm5URGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O\|U5PjZpPkKxOVc2QDZ4PD;hQi=>
KARPAS-299	MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	Mo\MglExKM7:TR?=			NHfqUplKSzVyPUOgcm0>	Mk\IQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
SR	MYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M4LRTp4yOCEQvF2=			NIDZWW9KSzVyPU[uPUBvVQ>?	NUPsdJBpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O\|U5PjZpPkKxOVc2QDZ4PD;hQi=>
HDLM-2	M4XJZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NID5Ull,OTBizszN			MojwTWM2OD5zMDywNFAhdk1?	MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
NB-1	NFvhZWhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MoGxglExKM7:TR?=			NEjLZpRKSzVyPUSuOUBvVQ>?	MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
KELLY	MnvBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	M2TGVZ4yOCEQvF2=			NIGwe41KSzVyPU[yJI5O	M1fjOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
SK-N-FI	M2fw[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MmHtglExKM7:TR?=			NV\jXFFWUUN3ME6xNEwxODBibl2=	NF3FbVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O\|U5PjZ:L3G+
NCI-H2228	MXjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MUL+NVAh\|ryP			NH7iN2JKSzVyPUWzJI5O	MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
Calu-3	MlzES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NW\OPHVMhjFyIN88US=>			MnzYTWM2OD1-MUCsNFAxKG6P	MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
PC-1	MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NES2ZnJ,OTBizszN			NVPBT5A5UUN3ME6xNEwxODBibl2=	NVHtOFVCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O\|U5PjZpPkKxOVc2QDZ4PD;hQi=>
NCI-H23	M{nlfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	M4fUcJ4yOCEQvF2=			MX\JR\|UxRTN4MECgcm0>	MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
Calu-1	M1fEV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MU\+NVAh\|ryP			Ml7sTWM2OD5zMDywNFAhdk1?	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
NCI-H2009	MmS4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NVPZZXZzhjFyIN88US=>			MY\JR\|UxRjFyLECwNEBvVQ>?	NHmzN\|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O\|U5PjZ:L3G+
NCI-H1993	M4XBWmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MX3+NVAh\|ryP			M2T3SWlEPTB-MUCsNFAxKG6P	NF;0U\|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O\|U5PjZ:L3G+
MKN-45	NFfzeYpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	M{TWNZ4yOCEQvF2=			NHvnNHlKSzVyPkGwMFAxOCCwTR?=	MoHtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
SNU-5	NIi1ZZJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NYDYNXJDhjFyIN88US=>			NXLGVGNTUUN3ME2xPFAxKG6P	M{jtcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
KATO-III	M1fDUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NVS1N3hihjFyIN88US=>			NG\ldGxKSzVyPUe5NFAhdk1?	M3jaWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
SK-BR-3	M1XaXWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NHHSSIx,OTBizszN			MnnzTWM2OD5zMDywNFAhdk1?	Mn;oQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
BT-483	MkLqS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MWr+NVAh\|ryP			MYPJR\|UxRjFyLECwNEBvVQ>?	NG\vbmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O\|U5PjZ:L3G+
PC-3	MnHLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NES5WY1,OTBizszN			M4rieGlEPTB-MUCsNFAxKG6P	NETBcVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O\|U5PjZ:L3G+
22Rv1	NV;ZWpN3T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NWL4cY5ShjFyIN88US=>			MofYTWM2OD5zMDywNFAhdk1?	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
U-87 MG	MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M3;zdJ4yOCEQvF2=			M4DUZ2lEPTB-MUCsNFAxKG6P	NHPHVIY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O\|U5PjZ:L3G+
H3122	M3S0Umdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	Mn\6glExKM7:TR?=			MoCxTWM2OD1\|MzDuUS=>	MljiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyOU[0NFAoRjJ3MEm2OFAxRC:jPh?=
LC-2/ad	MmD0RZBweHSxc3nzJIF{e2G7	MWT+NUDPxE1?		MWfEUXNQ	MnvSbY5lfWOnczDhdI9xfG:\|aYO=	MnjtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV\|NEmzNFcoRjJ3M{S5N\|A4RC:jPh?=
LC-2/ad	MnfNSpVv[3Srb36gZZN{[Xl?	NXjHU29GhjFizszN		MY\EUXNQ	MYDpcohq[mm2czD0bIUhVUGSSzDzbYdv[WyrbnegdIF1cHejeR?=	M3GwelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{S5N\|A4Lz5{NUO0PVMxPzxxYU6=
Ba/F3	MWTGeY5kfGmxbjDhd5NigQ>?	NYG0R5pMhjFizszN		MmnnSG1UVw>?	NVe4O21Qe3WycILld5NmeyCyaH;zdIhwenmuYYTpc44hd2ZiRWLLJIFv\CCrbnPy[YF{\XNidHjlJIFjfW6mYX7j[UBw\iCESV2=	NEHaUm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO0PVMxPyd-MkWzOFk{ODd:L3G+
SNU-2535	MYXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M3LmRZ4yOCEQvF2=			Ml3hTWM2OD1\|Mz6xJI5O	NXfWVItnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4OFk3OzdpPkK2PFQ6PjN5PD;hQi=>
SNU-2535	NFzycHZMcW6jc3WgZZN{[Xl?	MnLyglEh\|ryP			M3nWWolvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVzLJIFv\CCrdIOg[I94dnO2cnXhcUBud2ynY4Xs[ZMhTVKNMT:yJIFv\CCDS2S=	NF3BNnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki0PVY{Pyd-Mk[4OFk3Ozd:L3G+
Ba/F3	NWHXNXRUTnWwY4Tpc44h[XO\|YYm=		NIjlVYo4OiCqcoO=		MX;Jcohq[mm2aX;uJI9nKEWPTEStRWxMKENzMUW2XUBufXSjboSgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO\|ZXSgbY4hdW:3c3WgRoEwTjNiY3XscJMh[XO\|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgO\|IhcHK\|IHL5JG1VWyCjc4PhfUwhUUN3MDC9JFAvODB{IN88UU4>	NFGwO5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
Ba/F3	NEO2ellHfW6ldHnvckBie3OjeR?=		MVS3NkBpenN?		M2iwfmlvcGmkaYTpc44hd2ZiRV3MOE1CVEtiU{GyNFZ[KG23dHHueEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCvb4Xz[UBD[S:IMzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCLQ{WwJF0hOC5yMEKg{txONg>?	MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
Ba/F3	MnjCSpVv[3Srb36gZZN{[Xl?		NIHEU3k4OiCqcoO=		NVLmRXlmUW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgSW1NPC2DTFugLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO\|ZXSgbY4hdW:3c3WgRoEwTjNiY3XscJMh[XO\|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgO\|IhcHK\|IHL5JG1VWyCjc4PhfUwhUUN3MDC9JFAvODB{IN88UU4>	MnPzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
KARPAS299	NWK1eXhMSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		M2DlVFk3KGi{cx?=		MnvvRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCNQWLQRXMzQTliY3XscJMh[W[2ZYKgPVYhcHK\|IHL5JINmdGxiY3;1cpRqdmdiYYPzZZktKEmFNUCgQUAxNjByMzFOwG0v	MoDpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MkW5NVcoRjJ{MkK1PVE4RC:jPh?=
Ba/F3	MlvWSpVv[3Srb36gZZN{[Xl?		NFzjZYM4OiCqcoO=		NH3XSHFKdmirYnn0bY9vKG:oIFXNUFQuSUyNIF[xNVc1VCCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSmFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiSVO1NEA:KDBwMECzJO69VS5?	NGrxVm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
Ba/F3	M1Xxe2Z2dmO2aX;uJIF{e2G7		NWHtRYpNPzJiaILz		NF7IdohKdmirYnn0bY9vKG:oIFXNUFQuSUyNIFexNlY6SSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSmFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiSVO1NEA:KDBwMEC5JO69VS5?	M2juc\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
NCI-H3122	MlrURY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NXjzdo1EPzJiaILz		M{XHemFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg{OTJ{IHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIFz1cYlv\XOlZX70JGNmdGxiVnnhZoltcXS7IFHzd4F6NCCHQ{WwJF0hOC5yMEmg{txONg>?	M1zlcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
KARPAS299	NYXaemlGSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		NEWzdXM4OiCqcoO=		MoPuRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCNQWLQRXMzQTliY3XscJMh[W[2ZYKgO\|IhcHK\|IHL5JHNTSi:FQ1utPEBie3OjeTygTWM2OCB;IECuNFE2KM7:TT6=	NF7Je\|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{GzNVA3Pid-MkexN\|ExPjZ:L3G+
NCI-H3122	M{LRdWFvfGmycn;sbYZmemG2aY\lJIF{e2G7		MYe3NkBpenN?		NVfvbmFnSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDNzMkKgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQj;DR2suQCCjc4PhfUwhUUN3MDC9JFAvODF5NDFOwG0v	MnPNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzM{GwOlYoRjJ5MUOxNFY3RC:jPh?=
SUP-M2	M1e2W2FvfGmycn;sbYZmemG2aY\lJIF{e2G7		MV:3NkBpenN?		NHfOTWNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPVVE1OOiClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDN0OFSz24JIF{e2G7LDDJR\|UxKD1iMD6wNVc6KM7:TT6=	M2D3NlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUOxNFY3Lz5{N{GzNVA3PjxxYU6=
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SMS-KCNR	MUnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		MV:3NkBpenN?		MnPYRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCVTWOtT2NPWiClZXzsd{BmgHC{ZYPzbY5oKEWPTEStRWxMKFJzMke1VUBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hVHWvaX7ld4NmdnRiQ3XscEBXcWGkaXzpeJkhSXO\|YYmsJGVEPTBiPTCwMlc3PSEQvF2u	MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
SK-N-SH	MXnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		NFnafFc4OiCqcoO=		NUfMbIFuSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1PNVOKIHPlcIx{KGW6cILld5NqdmdiRV3MOE1CVEtiRkGxO\|RNKG23dHHueEBi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCOdX3pcoV{[2WwdDDD[YxtKF[rYXLpcIl1gSCDc4PhfUwhTUN3MDC9JFAvQDd{IN88UU4>	M2ThSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
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アッセイ

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

体内試験

Oral administration of CH5424802 dose-dependently inhibits tumor growth with an ED50 of 0.46 mg/kg and tumor regression. Treatment of 20 mg/kg CH5424802 reveals rapid tumor regression by 168%, the tumor volume in any mouse is <30 mm³ after 11 days of treatment (at day 28), a potent antitumor effect is maintained, and tumor regrowth does not occur throughout the 4-week drug-free period. The half-life and the oral bioavailability of CH5424802 in mice are 8.6 hours and 70.8%, respectively. At a repeated dose of 6 mg/kg, the mean plasma levels reached 1.7, 1.5, and 0.3 nM at 2, 7, and 24 hours post-dose, respectively. Administration of CH5424802 leads to tumor growth prevention and tumor regression. Tumor growth inhibition at 20 mg/kg is 119% for KARPAS-299 and 104% for NB-1 on day 20. CH5424802 inhibits the phosphorylation of STAT3 in a dose-dependent manner (2–20 mg/kg). A partial decrease in AKT phosphorylation is also observed in CH5424802-treated xenograft tumors. ^[1]

お薦めの試験操作（参考用のみ）

キナーゼ試験：^[1]	- 合併 Kinase inhibitory assays in Vitro: The inhibitory ability against each kinase except for MEK1 and Raf-1 is evaluated by examining their ability to phosphorylate various substrate peptides in the presence of CH5424802 using time-resolved fluorescence resonance energy transfer (TR-FRET) assay or fluorescence polarization (FP) assay. The inhibitory activity against MEK1 is evaluated by quantitative analysis of the phosphorylation of a substrate peptide by a recombinant ERK2 protein in the presence of CH5424802. The inhibitory activity against Raf-1 is evaluated by examining the ability of the kinases to phosphorylate MEK1 in the presence of CH5424802.
細胞試験： ^[1]	- 合併細胞株： NSCLC, A549 and HCC827 cell lines 濃度： 0-1 μM 反応時間： 5 days 実験の流れ： Cells including NSCLC, A549 and HCC827 are seeded in 96-well plates overnight and incubated with various concentrations of CH5424802 for the indicated time. For spheroid cell growth inhibition assay, cells are seeded on spheroid plates, incubated overnight, and then treated with compound for the indicated times. The viable cells are measured by the Luminescent Cell Viability Assay. Caspase-3/7 assay is evaluated using the Caspase-Glo 3/7 Assay Kit. (参考用のみ)
動物試験：^[1]	- 合併動物モデル： SCID or nude mice bearing NCI-H2228 投薬量： 20 mg/kg 投与方法： Oral administration (参考用のみ)

参考

溶解度 (25°C)

体外	DMSO	0.5 mg/mL (1.03 mM) warming
	Water	Insoluble
	Ethanol	Insoluble

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報 Alectinib (CH5424802) SDFをダウンロードする

分子量	482.62
化学式	C₃₀H₃₄N₄O₂
CAS No.	1256580-46-7
Storage	3 years-20°C powder 2 years-80°C in solvent
別名	AF-802, RG-7853
Smiles	CCC1=CC2=C(C=C1N3CCC(CC3)N4CCOCC4)C(C5=C(C2=O)C6=C(N5)C=C(C=C6)C#N)(C)C

投与溶媒組成計算器(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量

mg/kg

動物平均体重

投与体積（動物毎）

動物数

匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO+ % + % Tween 80+ % ddH₂O

計算リセット

計算結果:

投与溶媒濃度： mg/ml；

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL，注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。）

投与溶媒調製方法：μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

便利ツール

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

質量

濃度

体積

分子量
=

×

×

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとSDS/COA（製品ページで利用可能な）。

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます：

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます：C1V1 = C2V2 ( 入力出力 )

C1

V1

C2

V2
×

=

×

常に貯蔵液を準備するとき、小びんラベルとSDS/COA（オンラインで利用できる）で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

連続希釈剤
初めの濃度：
稀釈倍数：

計算結果

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):

分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください：

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

臨床試験 (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

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須
*大学・企業名:
*名前:
*電子メール:
*電話番号:
*内容:

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FDA-approved ALK Inhibitor

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研究分野別

製品類型

Alectinib (CH5424802)

文献中Selleckの製品使用例(57)

製品安全説明書

ALK阻害剤の選択性比較

生物活性

お薦めの試験操作（参考用のみ）

参考

溶解度 (25°C)

化学情報 Alectinib (CH5424802) SDFをダウンロードする

投与溶媒組成計算器(クリア溶液)

便利ツール

モル濃度計算器

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

希釈計算器

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

連続希釈計算器方程式

連続希釈剤

計算結果

分子量计算器

総分子量：g/mol

モル濃度計算器

臨床試験 (data from https://clinicaltrials.gov, updated on 2022-01-17)

技術サポート

ALKシグナル伝達経路

ALK Inhibitors with Unique Features

相関ALK製品