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 61 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 MkDNT4lv[XOnIHHzd4F6 M4DpZp4yKM7:TR?= NGq0SXBxemW4ZX70d{BifXSxcHjvd5Bpd3K7bHH0bY9vKG:oIFHMTy=> NI\rN2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
KARPAS-299 NWPxdW5KT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3K3NZ4yOCEQvF2= MUfJR|UxRTNibl2= NW[1S41lRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
SR MmfRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVzUc5pThjFyIN88US=> MYPJR|UxRTZwOTDuUS=> NFjLcnE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
HDLM-2 NWjy[nRYT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHLwZWx,OTBizszN NXPPNW5rUUN3ME6xNEwxODBibl2= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
NB-1 NX;qcZBwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFW5SWh,OTBizszN M3f1XmlEPTB;ND61JI5O MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
KELLY MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MljnglExKM7:TR?= NHHKO5dKSzVyPU[yJI5O NED4W|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
SK-N-FI NW\rfXN3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYrhWXhwhjFyIN88US=> NVWxZWUzUUN3ME6xNEwxODBibl2= M37HeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
NCI-H2228 NYq3S5Z[T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NV;L[WxLhjFyIN88US=> NGDPdGVKSzVyPUWzJI5O NYn2NZFFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
Calu-3 NEL4SGZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEnCdo5,OTBizszN MlfWTWM2OD1-MUCsNFAxKG6P NEDX[WQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
PC-1 NX7tfW02T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Ml;YglExKM7:TR?= M{nOPGlEPTB-MUCsNFAxKG6P NFXmboM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
NCI-H23 NX;tZ2RWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnvJglExKM7:TR?= MVfJR|UxRTN4MECgcm0> NWTHfYdNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
Calu-1 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWLUR|hkhjFyIN88US=> MVvJR|UxRjFyLECwNEBvVQ>? NXn5N2FwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
NCI-H2009 NGrheVdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUP+NVAh|ryP MX7JR|UxRjFyLECwNEBvVQ>? NIm4bXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
NCI-H1993 MoXxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlHSglExKM7:TR?= NF[ydYJKSzVyPkGwMFAxOCCwTR?= M4\ENVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
MKN-45 MULHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{nVUJ4yOCEQvF2= MX;JR|UxRjFyLECwNEBvVQ>? NVrIPHpRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
SNU-5 NGXiW|lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4WzTp4yOCEQvF2= MXjJR|UxRTF6MECgcm0> NWO1SZY{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
KATO-III MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUDQTmprhjFyIN88US=> M1zSOGlEPTB;N{mwNEBvVQ>? NHKzVVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
SK-BR-3 MmixS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2\6O54yOCEQvF2= MkLaTWM2OD5zMDywNFAhdk1? Ml3SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
BT-483 MlzmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX6xSotZhjFyIN88US=> NHfkNlRKSzVyPkGwMFAxOCCwTR?= MoCwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
PC-3 NWf1S5BKT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4WxU54yOCEQvF2= MlzyTWM2OD5zMDywNFAhdk1? MkfsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
22Rv1 MmfvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFXhXoZ,OTBizszN NFHmXYNKSzVyPkGwMFAxOCCwTR?= MkfaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
U-87 MG NFfpNHNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3jaXJ4yOCEQvF2= NXzpNGYyUUN3ME6xNEwxODBibl2= NWewNYVWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
H3122 Ml;sS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2j5SZ4yOCEQvF2= MXHJR|UxRTN|IH7N NIXzfoI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC5OlQxOCd-MkWwPVY1ODB:L3G+
LC-2/ad MVjBdI9xfG:|aYOgZZN{[Xl? MVn+NUDPxE1? MYfEUXNQ MnfvbY5lfWOnczDhdI9xfG:|aYO= MmXyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|NEmzNFcoRjJ3M{S5N|A4RC:jPh?=
LC-2/ad NH3ObGtHfW6ldHnvckBie3OjeR?= NVj4VI1thjFizszN NXzUVpR6TE2VTx?= Mkn5bY5pcWKrdIOgeIhmKE2DUFugd4lodmGuaX7nJJBifGi5YYm= NFXwdXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO0PVMxPyd-MkWzOFk{ODd:L3G+
Ba/F3 M2fUTWZ2dmO2aX;uJIF{e2G7 M1jsfJ4yKM7:TR?= NFnlephFVVOR NXLzT49je3WycILld5NmeyCyaH;zdIhwenmuYYTpc44hd2ZiRWLLJIFv\CCrbnPy[YF{\XNidHjlJIFjfW6mYX7j[UBw\iCESV2= NX;QPZZTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOFk{ODdpPkK1N|Q6OzB5PD;hQi=>
SNU-2535 MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NITqelN,OTBizszN MnPCTWM2OD1|Mz6xJI5O NUTZRmR4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4OFk3OzdpPkK2PFQ6PjN5PD;hQi=>
SNU-2535 NYXKbmdvU2mwYYPlJIF{e2G7 Mn\VglEh|ryP MXXpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGOSzDhcoQhcXS|IHTve45{fHKnYX2gcY9t\WO3bHXzJGVTUzFxMjDhcoQhSUuW MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh2OU[zO{c,OjZ6NEm2N|c9N2F-
Ba/F3 MY\GeY5kfGmxbjDhd5NigQ>? MUK3NkBpenN? Mm\pTY5pcWKrdHnvckBw\iCHTVy0MWFNUyCFMUG1OnkhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKG2xdYPlJGJiN0Z|IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFczKGi{czDifUBOXFNiYYPzZZktKEmFNUCgQUAxNjByMjFOwG0v MkfJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
Ba/F3 MonHSpVv[3Srb36gZZN{[Xl? NUPQO4dEPzJiaILz M3fXVWlvcGmkaYTpc44hd2ZiRV3MOE1CVEtiU{GyNFZ[KG23dHHueEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCvb4Xz[UBD[S:IMzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCLQ{WwJF0hOC5yMEKg{txONg>? NUHk[ZM{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OlgzQDlpPkK2OVY5Ojh7PD;hQi=>
Ba/F3 NWn0VZF4TnWwY4Tpc44h[XO|YYm= MUO3NkBpenN? NIK5dIFKdmirYnn0bY9vKG:oIIfpcIQhfHmyZTDFUWw1NUGOSzCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBud3W|ZTDCZU9HOyClZXzsd{Bie3Onc4Pl[EBieyClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgUXRUKGG|c3H5MEBKSzVyIE2gNE4xODJizszNMi=> M4m4bFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
KARPAS299 M3zrfWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NUi5T25FQTZiaILz MYLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEuDUmDBV|I6QSClZXzsd{Bi\nSncjC5OkBpenNiYomgZ4VtdCClb4XueIlv\yCjc4PhfUwhUUN3MDC9JFAvODB|IN88UU4> MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ{NUmxO{c,OjJ{MkW5NVc9N2F-
Ba/F3 MlS2SpVv[3Srb36gZZN{[Xl? MYW3NkBpenN? NUXW[5NNUW6qaXLpeIlwdiCxZjDFUWw1NUGOSzDGNVE4PExibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIH3veZNmKEKjL1[zJINmdGy|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSCPVGOgZZN{[XluIFnDOVAhRSByLkCwN{DPxE1w M1rWW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
Ba/F3 M{TxW2Z2dmO2aX;uJIF{e2G7 NXLtO2NCPzJiaILz Mkj0TY5pcWKrdHnvckBw\iCHTVy0MWFNUyCJMUK2PWEhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKG2xdYPlJGJiN0Z|IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFczKGi{czDifUBOXFNiYYPzZZktKEmFNUCgQUAxNjByOTFOwG0v NH3ETno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
NCI-H3122 M1LST2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 M4HSeVczKGi{cx?= MYTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IN|EzOiClZXzsd{Bi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCOdX3pcoV{[2WwdDDD[YxtKF[rYXLpcIl1gSCDc4PhfUwhTUN3MDC9JFAvODB7IN88UU4> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
KARPAS299 MWHBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M2nRNFczKGi{cx?= NF3RPW5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvBVnBCWzJ7OTDj[YxteyCjZoTldkA4OiCqcoOgZpkhW1KEL1PDT{05KGG|c3H5MEBKSzVyIE2gNE4xOTVizszNMi=> NH\tNms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{GzNVA3Pid-MkexN|ExPjZ:L3G+
NCI-H3122 NHzTNWdCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NFn2RoU4OiCqcoO= NELNOYVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOzF{MjDj[YxteyCjZoTldkA4OiCqcoOgZpkhW1KEL1PDT{05KGG|c3H5MEBKSzVyIE2gNE4xOTd2IN88UU4> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF|MUC2Okc,OjdzM{GwOlY9N2F-
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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.
Animal Research:[1]
  • Animal Models: SCID or nude mice bearing NCI-H2228
  • Dosages: 20 mg/kg
  • Administration: Oral administration

Solubility (25°C)

In vitro

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

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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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