Name: Alectinib (CH5424802)
Brand: Selleck Chemicals
SKU: S2762
Rating: 5 (57 reviews)

Alectinib (CH5424802) Chemical Structure

CAS No. 1256580-46-7

Selleck's Alectinib (CH5424802) has been cited by 57 publications

Purity & Quality Control

Choose Selective ALK Inhibitors

Related Compound Libraries

Other ALK Products

Download Inhibitor Catalog

ALK Signaling Pathway Map

Biological Activity

Description

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.

Targets

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

In vitro

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]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

NCI-H2228	NX3SO\|VjU2mwYYPlJIF{e2G7	MUj+NUDPxE1?			MljMdJJmfmWwdIOgZZV1d3Cqb4PwbI9zgWyjdHnvckBw\iCDTFu=	NVL3OWw6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O\|U5PjZpPkKxOVc2QDZ4PD;hQi=>
KARPAS-299	MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MoLKglExKM7:TR?=			Mnj2TWM2OD1\|IH7N	M2TRc\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
SR	M2ftPGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NGrEOIt,OTBizszN			NEnPUldKSzVyPU[uPUBvVQ>?	NYPFUI1RRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O\|U5PjZpPkKxOVc2QDZ4PD;hQi=>
HDLM-2	NXLNVpZtT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NFP1UJZ,OTBizszN			NVTtNHdUUUN3ME6xNEwxODBibl2=	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
NB-1	MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M{DWfp4yOCEQvF2=			M{GxTGlEPTB;ND61JI5O	MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
KELLY	MVnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M135W54yOCEQvF2=			NF\1[JNKSzVyPU[yJI5O	NFHnTnc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O\|U5PjZ:L3G+
SK-N-FI	MmPkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NV3pbohthjFyIN88US=>			MnywTWM2OD5zMDywNFAhdk1?	Mn;HQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
NCI-H2228	MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NFTtXFh,OTBizszN			NUjl[oxJUUN3ME21N{BvVQ>?	MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
Calu-3	NYTrNWxwT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M1noVJ4yOCEQvF2=			MmPrTWM2OD1-MUCsNFAxKG6P	NUDNd5ZnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O\|U5PjZpPkKxOVc2QDZ4PD;hQi=>
PC-1	MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MUP+NVAh\|ryP			MmS4TWM2OD5zMDywNFAhdk1?	NWXRPXZIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O\|U5PjZpPkKxOVc2QDZ4PD;hQi=>
NCI-H23	MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NE[1Rpd,OTBizszN			NEHLZWdKSzVyPUO2NFAhdk1?	MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
Calu-1	NXi2XnYzT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MWf+NVAh\|ryP			NHSwd49KSzVyPkGwMFAxOCCwTR?=	NGLOS5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O\|U5PjZ:L3G+
NCI-H2009	MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MWr+NVAh\|ryP			M{LFc2lEPTB-MUCsNFAxKG6P	NEi2OXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O\|U5PjZ:L3G+
NCI-H1993	NFLOcZRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	M{iz[J4yOCEQvF2=			NYfMN3h1UUN3ME6xNEwxODBibl2=	MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
MKN-45	MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NHTGbFh,OTBizszN			MnexTWM2OD5zMDywNFAhdk1?	MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
SNU-5	M13LfWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	MmPoglExKM7:TR?=			MUTJR\|UxRTF6MECgcm0>	M1fBd\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
KATO-III	NV32V3p2T3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NH7OXZd,OTBizszN			NGDOd5RKSzVyPUe5NFAhdk1?	MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
SK-BR-3	NY\UW3VoT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MXz+NVAh\|ryP			Mo\yTWM2OD5zMDywNFAhdk1?	NFXmVFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O\|U5PjZ:L3G+
BT-483	MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MUn+NVAh\|ryP			NXrzbm5FUUN3ME6xNEwxODBibl2=	M1\Zd\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
PC-3	NEXhR3dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NUi2NmtWhjFyIN88US=>			M{j2TWlEPTB-MUCsNFAxKG6P	NEewUJg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O\|U5PjZ:L3G+
22Rv1	NGDOV3hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MlnaglExKM7:TR?=			NGLaUFhKSzVyPkGwMFAxOCCwTR?=	Mn:yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
U-87 MG	MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MmXHglExKM7:TR?=			MYnJR\|UxRjFyLECwNEBvVQ>?	MmfOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
H3122	NInMc5VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MnvsglExKM7:TR?=			M{nCZ2lEPTB;M{Ogcm0>	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB7NkSwNEc,OjVyOU[0NFA9N2F-
LC-2/ad	MmXJRZBweHSxc3nzJIF{e2G7	M33tNZ4yKM7:TR?=		NGjKSo5FVVOR	Mnr0bY5lfWOnczDhdI9xfG:\|aYO=	MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN2OUOwO{c,OjV\|NEmzNFc9N2F-
LC-2/ad	MVnGeY5kfGmxbjDhd5NigQ>?	MlPlglEh\|ryP		MnXTSG1UVw>?	MVXpcohq[mm2czD0bIUhVUGSSzDzbYdv[WyrbnegdIF1cHejeR?=	NEi4VIk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO0PVMxPyd-MkWzOFk{ODd:L3G+
Ba/F3	MnrzSpVv[3Srb36gZZN{[Xl?	MUD+NUDPxE1?		MYfEUXNQ	MVfzeZBxemW\|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBGWktiYX7kJIlv[3KnYYPld{B1cGViYXL1coRidmOnIH;mJGJKVQ>?	MoHkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV\|NEmzNFcoRjJ3M{S5N\|A4RC:jPh?=
SNU-2535	MVrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	MXn+NVAh\|ryP			NVrNV3dQUUN3ME2zN{4yKG6P	NWPOWmdLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4OFk3OzdpPkK2PFQ6PjN5PD;hQi=>
SNU-2535	MXXLbY5ie2ViYYPzZZk>	M161fZ4yKM7:TR?=			NHfUNGVqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHMT{BidmRiaYTzJIRwf26\|dILlZY0hdW:uZXP1cIV{KEWUS{GvNkBidmRiQVvU	NXLidXhmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4OFk3OzdpPkK2PFQ6PjN5PD;hQi=>
Ba/F3	MmOySpVv[3Srb36gZZN{[Xl?		MWS3NkBpenN?		NHPldZpKdmirYnn0bY9vKG:oIFXNUFQuSUyNIFOxNVU3YSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSmFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiSVO1NEA:KDBwMECyJO69VS5?	Ml;OQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
Ba/F3	NVzSSlRtTnWwY4Tpc44h[XO\|YYm=		MWG3NkBpenN?		NYW1cIh2UW6qaXLpeIlwdiCxZjDFUWw1NUGOSzDTNVIxPllibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIH3veZNmKEKjL1[zJINmdGy\|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSCPVGOgZZN{[XluIFnDOVAhRSByLkCwNkDPxE1w	NXLYeVc2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OlgzQDlpPkK2OVY5Ojh7PD;hQi=>
Ba/F3	MmjHSpVv[3Srb36gZZN{[Xl?		NUHhZmhQPzJiaILz		NUewPJpIUW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgSW1NPC2DTFugLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO\|ZXSgbY4hdW:3c3WgRoEwTjNiY3XscJMh[XO\|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgO\|IhcHK\|IHL5JG1VWyCjc4PhfUwhUUN3MDC9JFAvODB{IN88UU4>	M2TE[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
KARPAS299	MlvsRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NFLkNXM6PiCqcoO=		Mnr4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCNQWLQRXMzQTliY3XscJMh[W[2ZYKgPVYhcHK\|IHL5JINmdGxiY3;1cpRqdmdiYYPzZZktKEmFNUCgQUAxNjByMzFOwG0v	Mk\uQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MkW5NVcoRjJ{MkK1PVE4RC:jPh?=
Ba/F3	NFr5elNHfW6ldHnvckBie3OjeR?=		MY[3NkBpenN?		MXzJcohq[mm2aX;uJI9nKEWPTEStRWxMKEZzMUe0UEBufXSjboSgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO\|ZXSgbY4hdW:3c3WgRoEwTjNiY3XscJMh[XO\|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgO\|IhcHK\|IHL5JG1VWyCjc4PhfUwhUUN3MDC9JFAvODB\|IN88UU4>	MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
Ba/F3	NHHP[plHfW6ldHnvckBie3OjeR?=		NGXXVY44OiCqcoO=		MofVTY5pcWKrdHnvckBw\iCHTVy0MWFNUyCJMUK2PWEhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKG2xdYPlJGJiN0Z\|IHPlcIx{KGG\|c3Xzd4VlKGG\|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFczKGi{czDifUBOXFNiYYPzZZktKEmFNUCgQUAxNjByOTFOwG0v	M4WzbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
NCI-H3122	M2L0emFvfGmycn;sbYZmemG2aY\lJIF{e2G7		MVG3NkBpenN?		MVPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IN\|EzOiClZXzsd{Bi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCOdX3pcoV{[2WwdDDD[YxtKF[rYXLpcIl1gSCDc4PhfUwhTUN3MDC9JFAvODB7IN88UU4>	M1jNRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
KARPAS299	NGPiO2pCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NV;vSHNnPzJiaILz		MYLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEuDUmDBV\|I6QSClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDN0OFSz24JIF{e2G7LDDJR\|UxKD1iMD6wNVUh\|ryPLh?=	NYTQT2pnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexN\|ExPjZpPkK3NVMyODZ4PD;hQi=>
NCI-H3122	MnjqRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NIju[pE4OiCqcoO=		M2LHN2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg{OTJ{IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJxQ1PLMVgh[XO\|YYmsJGlEPTBiPTCwMlAyPzRizszNMi=>	NHXkeG09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{GzNVA3Pid-MkexN\|ExPjZ:L3G+
SUP-M2	NXX0Oph{SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		NYPwWohLPzJiaILz		MXLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOXUD3NNkBk\WyuczDh[pRmeiB5MjDodpMh[nliU2LCM2NEUy16IHHzd4F6NCCLQ{WwJF0hOC5yMUe5JO69VS5?	M1vyNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUOxNFY3Lz5{N{GzNVA3PjxxYU6=
NCI-H3122	M37GdWZ2dmO2aX;uJIF{e2G7		NIPST3Q4OiCqcoO=		NHPsOpdKdmirYnn0bY9vKG:oIFHMT{BmgHC{ZYPz[YQhcW5iaIXtZY4hVkOLLVizNVIzKGOnbHzzJIF{e2W\|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IGPSRk9ES0tvODDhd5NigSxiSVO1NEA:KDBwMEG5JO69VS5?	NGXCRng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{GzNVA3Pid-MkexN\|ExPjZ:L3G+
NCI-H3122	NFXJWoFCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NUTM[oNOPzJiaILz		M3O1OmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgRWxMNWSncHXu[IVvfCCqdX3hckBPS0lvSEOxNlIh[2WubIOgZYZ1\XJiN{KgbJJ{NCCLQ{WwJF0hOC5yMUmg{txONg>?	NX[2cWlnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0O\|Y4PDlpPkK2OFc3PzR7PD;hQi=>
SU-DHL1	NEH6W2tCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		M2DOZ\|czKGi{cx?=		M{THcWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2WtSGhNOSClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDN0OFSz24JIF{e2G7LDDJR\|UxKD1iMD6wNlA2KM7:TT6=	M4PNfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUOxNFY3Lz5{N{GzNVA3PjxxYU6=
NIH/3T3	NWDVXYNsSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		M3LQXFczKGi{cx?=		MXvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKE6LSD:zWFMh[2WubIOg[ZhxemW\|c3nu[{B4cWymIIT5dIUhTU2OND3BUGsh[W[2ZYKgO\|IhcHK\|IHL5JHNTSi:FQ1utPEBie3OjeTygTWM2OCB;IECuNFMzOyEQvF2u	Mli3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzM{GwOlYoRjJ5MUOxNFY3RC:jPh?=
Ba/F3	M33BOmZ2dmO2aX;uJIF{e2G7		NXvPWGFqPzJiaILz		MX\Jcohq[mm2aX;uJI9nKEWPTEStRWxMKDFzNUHUbY5{KG23dHHueEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCvb4Xz[UBD[S:IMzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCLQ{WwJF0hOC5yN{Kg{txONg>?	MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
Ba/F3	Mmq1SpVv[3Srb36gZZN{[Xl?		M2rreFczKGi{cx?=		MVXJcohq[mm2aX;uJI9nKEWPTEStRWxMKExzMUm2UUBufXSjboSgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO\|ZXSgbY4hdW:3c3WgRoEwTjNiY3XscJMh[XO\|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgO\|IhcHK\|IHL5JG1VWyCjc4PhfUwhUUN3MDC9JFAvODlizszNMi=>	M{\qfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
NIH/3T3	NIfuV5ZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		M3qw[FczKGi{cx?=		MkTyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDtc5V{\SCQSVivN3Q{KGOnbHzzJIV5eHKnc4PpcochTU2OND3BUGshVDFzOU[gcZV1[W62IHHmeIVzKDd{IHjyd{BjgSCVUlKvR2NMNThiYYPzZZktKEmFNUCgQUAxNjF\|MjFOwG0v	MkDFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzM{GwOlYoRjJ5MUOxNFY3RC:jPh?=
Ba/F3	NWPJS5pWTnWwY4Tpc44h[XO\|YYm=		M3;kOFczKGi{cx?=		MWnJcohq[mm2aX;uJI9nKEWPTEStRWxMKExzMUWyVkBufXSjboSgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO\|ZXSgbY4hdW:3c3WgRoEwTjNiY3XscJMh[XO\|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgO\|IhcHK\|IHL5JG1VWyCjc4PhfUwhUUN3MDC9JFAvOTZ7IN88UU4>	NUDNZWFtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OlgzQDlpPkK2OVY5Ojh7PD;hQi=>
Ba/F3	M3:xeWZ2dmO2aX;uJIF{e2G7		MVi3NkBpenN?		MUfJcohq[mm2aX;uJI9nKEWPTEStRWxMKEdzMkCyVkBufXSjboSgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO\|ZXSgbY4hdW:3c3WgRoEwTjNiY3XscJMh[XO\|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgO\|IhcHK\|IHL5JG1VWyCjc4PhfUwhUUN3MDC9JFAvOjB5IN88UU4>	Mlu2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
DFCI114	NIXLTmZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NEj0SHQ4OiCqcoO=		NH21Z5FCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFTGR2kyOTRiY3XscJMh\XiycnXzd4lv\yCHTVy0MWFNUyCJMUK2PWEhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKEy3bXnu[ZNk\W62IFPlcIwhXmmjYnnsbZR6KEG\|c3H5MEBGSzVyIE2gNE4zODdizszNMi=>	NXznTZN7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OlgzQDlpPkK2OVY5Ojh7PD;hQi=>
CHLA20	M3v5b2FvfGmycn;sbYZmemG2aY\lJIF{e2G7		NFTs[VY4OiCqcoO=		M4\6[mFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ1jMRVIxKGOnbHzzJIV5eHKnc4PpcochTU2OND3BUGshWjF{N{XRJI12fGGwdDDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BNfW2rbnXzZ4VvfCCFZXzsJHZq[WKrbHn0fUBCe3OjeTygSWM2OCB;IECuOFMh\|ryPLh?=	MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
Kelly	M{TmT2FvfGmycn;sbYZmemG2aY\lJIF{e2G7		NHLUNFA4OiCqcoO=		M3:4TWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS3XscJkh[2WubIOg[ZhxemW\|c3nu[{BGVUx2LVHMT{BHOTF5NFygcZV1[W62IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJGx2dWmwZYPj[Y51KEOnbHygWoli[mmuaYT5JGF{e2G7LDDFR\|UxKD1iMD60N\|Qh\|ryPLh?=	NF\FdIs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
DFCI76	NGrERYxCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NEW4SWg4OiCqcoO=		M3nMVGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRF\DTVc3KGOnbHzzJIV5eHKnc4PpcochTU2OND3BUGshVDFzNULSJI12fGGwdDDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BNfW2rbnXzZ4VvfCCFZXzsJHZq[WKrbHn0fUBCe3OjeTygSWM2OCB;IECuOVEyKM7:TT6=	NED4S4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
LAN5	NUjzWWdTSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		NHLSO2k4OiCqcoO=		MVLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyDTkWgZ4VtdHNiZYjwdoV{e2mwZzDFUWw1NUGOSzDSNVI4PVFibYX0ZY51KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIFz1cYlv\XOlZX70JGNmdGxiVnnhZoltcXS7IFHzd4F6NCCHQ{WwJF0hOC54MUeg{txONg>?	MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
SMS-KCNR	MUPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		NEXUZ\|A4OiCqcoO=		MVfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOPUz3LR25TKGOnbHzzJIV5eHKnc4PpcochTU2OND3BUGshWjF{N{XRJI12fGGwdDDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BNfW2rbnXzZ4VvfCCFZXzsJHZq[WKrbHn0fUBCe3OjeTygSWM2OCB;IECuO\|Y2KM7:TT6=	M324SlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
SK-N-SH	Mk\RRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NEjpOJY4OiCqcoO=		M4XnXWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utUk1UUCClZXzsd{BmgHC{ZYPzbY5oKEWPTEStRWxMKEZzMUe0UEBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hVHWvaX7ld4NmdnRiQ3XscEBXcWGkaXzpeJkhSXO\|YYmsJGVEPTBiPTCwMlg4OiEQvF2u	NHTXboc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
SH-SY5Y	MV3BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		MWm3NkBpenN?		MnfkRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCVSD3TXVV[KGOnbHzzJIV5eHKnc4PpcochTU2OND3BUGshTjFzN{TMJI12fGGwdDDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BNfW2rbnXzZ4VvfCCFZXzsJHZq[WKrbHn0fUBCe3OjeTygSWM2OCB;IEGuNVUh\|ryPLh?=	NIfDbGM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
SK-N-BE(2)	NVPWSopRSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MkfFO\|IhcHK\|		NV;NdGM6SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1PNUKHKEKpJINmdGy\|IHX4dJJme3Orbnege4lt\CC2eYDlJGVOVDRvQVzLJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKEy3bXnu[ZNk\W62IFPlcIwhXmmjYnnsbZR6KEG\|c3H5MEBGSzVyIE2gNU42PTRizszNMi=>	NIC0d4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
LAN1	NH;pNnhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NVLrXXRCPzJiaILz		NEjSRmpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzBUlEh[2WubIOg[ZhxemW\|c3nu[{BGVUx2LVHMT{BHOTF5NFygcZV1[W62IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJGx2dWmwZYPj[Y51KEOnbHygWoli[mmuaYT5JGF{e2G7LDDFR\|UxKD1iMj6wNFQh\|ryPLh?=	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
SK-N-AS	MlvkRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		MUi3NkBpenN?		NFHQRnVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMW4uSVNiY3XscJMh\XiycnXzd4lv\yC5aXzkJJR6eGViRV3MOE1CVEtiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gUJVucW6nc3PlcpQhS2WubDDWbYFjcWyrdImgRZN{[XluIFXDOVAhRSB{LkGzPUDPxE1w	NF20WVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
SK-N-FI	NYrCRZdVSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MYi3NkBpenN?		M{DGRWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utUk1HUSClZXzsd{BmgHC{ZYPzbY5oKHerbHSgeJlx\SCHTVy0MWFNUyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDMeY1qdmW\|Y3XueEBE\WyuIG\pZYJqdGm2eTDBd5NigSxiRVO1NEA:KDJwNECxJO69VS5?	MmjrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
NIH/3T3	M3rLb2FvfGm2dX3vdkBie3OjeR?=	M{TicVUxKG2pL3vn	M17EZ\|ExKGSjeYO=		MWXBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6\|dDDtc5V{\SCQSVivN3Q{KGOnbHzzJIV5eHKnc4PpcochTU2OND3BUGshVDFzOU\NJI12fGGwdDD4[Y5w\3KjZoTl[EBqdiCwdXTlJI1wfXOnIHHzd4V{e2WmIHHzJJR2dW:{IIP0ZZNqeyCjdDC1NEBu\y:tZzygdI8heWRiYXTtbY5qe3SncnXkJIZweiBzMDDkZZl{	M2n5[\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUOxNFY3Lz5{N{GzNVA3PjxxYU6=
NIH/3T3	M4X3cmFvfGm2dX3vdkBie3OjeR?=	M3n2WFUxKG2pL3vn	Mn3tNVAh\GG7cx?=		NFPKeGpCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBud3W\|ZTDOTWgwO1R\|IHPlcIx{KGW6cILld5NqdmdiRV3MOE1CVEtiTEGxPVZOKG23dHHueEB5\W6xZ4Lh[pRm\CCrbjDueYRmKG2xdYPlJIF{e2W\|c3XkJIF{KHCjcoTpZYwhfHWvb4KgdoVoemW\|c3nvckBifCB3MDDt[{9s\yxicH:gdYQh[WSvaX7pd5RmemWmIH\vdkAyOCCmYYnz	NUTsbFNXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexN\|ExPjZpPkK3NVMyODZ4PD;hQi=>

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

In vivo

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]

Protocol (from reference)

Kinase Assay:^[1]	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.
Cell Research:^[1]	Cell lines: NSCLC, A549 and HCC827 cell lines Concentrations: 0-1 μM Incubation Time: 5 days Method: 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. (Only for Reference)
Animal Research:^[1]	Animal Models: SCID or nude mice bearing NCI-H2228 Dosages: 20 mg/kg Administration: Oral administration (Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	0.5 mg/mL warmed (1.03 mM)
	Water	Insoluble
	Ethanol	Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight	482.62
Formula	C₃₀H₃₄N₄O₂
CAS No.	1256580-46-7
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CCC1=CC2=C(C=C1N3CCC(CC3)N4CCOCC4)C(C5=C(C2=O)C6=C(N5)C=C(C=C6)C#N)(C)C

Download Alectinib (CH5424802) SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

Clinical Trial Information

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

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

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):