Alectinib (CH5424802)

Catalog No.S2762 Synonyms: AF-802, RG-7853

For research use only.

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.

Alectinib (CH5424802) Chemical Structure

CAS No. 1256580-46-7

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

Purity & Quality Control

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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 Ki 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=
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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)

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
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

In vivo Formulation Calculator (Clear solution)

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%DMSO %

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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.

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Molarity Calculator

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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

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