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Alectinib (CH5424802)

For research use only.

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

49 publications

Alectinib (CH5424802) Chemical Structure

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.

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Selleck's Alectinib (CH5424802) has been cited by 49 publications

Purity & Quality Control

Choose Selective ALK Inhibitors

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 NF7WOJFMcW6jc3WgZZN{[Xl? MVf+NUDPxE1? M2jlRZBz\X[nboTzJIF2fG:yaH;zdIhwenmuYYTpc44hd2ZiQVzL NFvwVHE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
KARPAS-299 M4DIUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkSxglExKM7:TR?= MW\JR|UxRTNibl2= M1O4RlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
SR NIL1bpdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYr+NVAh|ryP M3rme2lEPTB;Nj65JI5O M4LRb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
HDLM-2 MlfNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX;F[JlEhjFyIN88US=> NFnjeVlKSzVyPkGwMFAxOCCwTR?= M4f5WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
NB-1 NXS3ZoxQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{njep4yOCEQvF2= MVLJR|UxRTRwNTDuUS=> M3j5N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
KELLY MmnWS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MojCglExKM7:TR?= NHy3fpVKSzVyPU[yJI5O MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
SK-N-FI NGPJfJZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVr+NVAh|ryP MlHSTWM2OD5zMDywNFAhdk1? NGT3RXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
NCI-H2228 M3nDemdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYD1Opp5hjFyIN88US=> M{fCUWlEPTB;NUOgcm0> MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5NUi2Okc,OjF3N{W4OlY9N2F-
Calu-3 NVXHNpFQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYDEXG96hjFyIN88US=> NF:1dGlKSzVyPU6xNEwxODBibl2= MkSwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
PC-1 NHHtWo5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NG[5cXV,OTBizszN M1;hTGlEPTB-MUCsNFAxKG6P NUTyPWx7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
NCI-H23 NVvLRYV3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVXuc4ljhjFyIN88US=> NFTEd2dKSzVyPUO2NFAhdk1? M2nyc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
Calu-1 MlLES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHHQPJV,OTBizszN MVHJR|UxRjFyLECwNEBvVQ>? M3vTWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
NCI-H2009 Mn\0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFfN[GZ,OTBizszN NHPjeZFKSzVyPkGwMFAxOCCwTR?= NWn2fFRtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
NCI-H1993 M33EVmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFPNd2l,OTBizszN Mn3DTWM2OD5zMDywNFAhdk1? MkK4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
MKN-45 M3jpWmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlfrglExKM7:TR?= Ml3lTWM2OD5zMDywNFAhdk1? NGLYV5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
SNU-5 MoTJS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHzk[XZ,OTBizszN MnHxTWM2OD1zOECwJI5O M13ObFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe1PFY3Lz5{MUW3OVg3PjxxYU6=
KATO-III MoXWS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml;jglExKM7:TR?= M2jQTGlEPTB;N{mwNEBvVQ>? NXfib|JqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
SK-BR-3 MnW5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MV7+NVAh|ryP NVjITm5EUUN3ME6xNEwxODBibl2= NEe5WY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
BT-483 M4\F[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4KwcZ4yOCEQvF2= M2f4UmlEPTB-MUCsNFAxKG6P MmG4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
PC-3 MnvyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYD+NVAh|ryP M2j1SmlEPTB-MUCsNFAxKG6P MkfSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{W4OlYoRjJzNUe1PFY3RC:jPh?=
22Rv1 MYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnXtglExKM7:TR?= M{XlcGlEPTB-MUCsNFAxKG6P NIe1[4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OVg3Pid-MkG1O|U5PjZ:L3G+
U-87 MG M3LQV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVzZUoc5hjFyIN88US=> MnTVTWM2OD5zMDywNFAhdk1? NVPt[mZPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1O|U5PjZpPkKxOVc2QDZ4PD;hQi=>
H3122 Mm\1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MU\+NVAh|ryP Mn3BTWM2OD1|MzDuUS=> MlPKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyOU[0NFAoRjJ3MEm2OFAxRC:jPh?=
LC-2/ad MVfBdI9xfG:|aYOgZZN{[Xl? NI[5dHd,OSEQvF2= MWPEUXNQ MYTpcoR2[2W|IHHwc5B1d3Orcx?= MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN2OUOwO{c,OjV|NEmzNFc9N2F-
LC-2/ad MoXkSpVv[3Srb36gZZN{[Xl? Mn7UglEh|ryP M1vOOWROW09? M1HLZolvcGmkaYTzJJRp\SCPQWDLJJNq\26jbHnu[{Bx[XSqd3H5 NY[0codRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOFk{ODdpPkK1N|Q6OzB5PD;hQi=>
Ba/F3 MmXSSpVv[3Srb36gZZN{[Xl? NUfCSW9HhjFizszN NIq2OHBFVVOR MV7zeZBxemW|c3XzJJBpd3OyaH;yfYxifGmxbjDv[kBGWktiYX7kJIlv[3KnYYPld{B1cGViYXL1coRidmOnIH;mJGJKVQ>? NHLLd5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO0PVMxPyd-MkWzOFk{ODd:L3G+
SNU-2535 NFvCSIlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUH+NVAh|ryP M1ryd2lEPTB;M{OuNUBvVQ>? NYfCcWtqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4OFk3OzdpPkK2PFQ6PjN5PD;hQi=>
SNU-2535 NFfzXlFMcW6jc3WgZZN{[Xl? NH;yeml,OSEQvF2= MU\pcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGOSzDhcoQhcXS|IHTve45{fHKnYX2gcY9t\WO3bHXzJGVTUzFxMjDhcoQhSUuW M{S3V|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OES5OlM4Lz5{Nki0PVY{PzxxYU6=
Ba/F3 M3jITGZ2dmO2aX;uJIF{e2G7 MUm3NkBpenN? NFvBRWJKdmirYnn0bY9vKG:oIFXNUFQuSUyNIFOxNVU3YSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSmFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiSVO1NEA:KDBwMECyJO69VS5? MorFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
Ba/F3 NHO2VXhHfW6ldHnvckBie3OjeR?= NHfiUXg4OiCqcoO= M13HT2lvcGmkaYTpc44hd2ZiRV3MOE1CVEtiU{GyNFZ[KG23dHHueEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCvb4Xz[UBD[S:IMzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCLQ{WwJF0hOC5yMEKg{txONg>? NGexT|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
Ba/F3 MXfGeY5kfGmxbjDhd5NigQ>? NHLtSIg4OiCqcoO= MlzHTY5pcWKrdHnvckBw\iC5aXzkJJR6eGViRV3MOE1CVEtiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gcY92e2ViQnGvSlMh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDD2bYFjcWyrdImgZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygTWM2OCB;IECuNFAzKM7:TT6= NIfhZZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
KARPAS299 M4DzcmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NX\ROFZPQTZiaILz NYe1WYZDSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLRXJRSVN{OUmgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KGOnbHygZ492dnSrbnegZZN{[XluIFnDOVAhRSByLkCwN{DPxE1w NH;HSGM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKyOVkyPyd-MkKyNlU6OTd:L3G+
Ba/F3 MVTGeY5kfGmxbjDhd5NigQ>? M1jRT|czKGi{cx?= NUPKU|NUUW6qaXLpeIlwdiCxZjDFUWw1NUGOSzDGNVE4PExibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIH3veZNmKEKjL1[zJINmdGy|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSCPVGOgZZN{[XluIFnDOVAhRSByLkCwN{DPxE1w M1jxRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
Ba/F3 NXXn[49DTnWwY4Tpc44h[XO|YYm= MnHjO|IhcHK| M2qzc2lvcGmkaYTpc44hd2ZiRV3MOE1CVEtiR{GyOllCKG23dHHueEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCvb4Xz[UBD[S:IMzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCLQ{WwJF0hOC5yMEmg{txONg>? MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
NCI-H3122 M3i0N2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 Mn\uO|IhcHK| MnXpRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFMyOjJiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9iTIXtbY5me2OnboSgR4VtdCCYaXHibYxqfHliQYPzZZktKEWFNUCgQUAxNjByOTFOwG0v MmXrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
KARPAS299 M{\JNmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 Mkf1O|IhcHK| NFjPZ2VCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvBVnBCWzJ7OTDj[YxteyCjZoTldkA4OiCqcoOgZpkhW1KEL1PDT{05KGG|c3H5MEBKSzVyIE2gNE4xOTVizszNMi=> NGO0[mg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{GzNVA3Pid-MkexN|ExPjZ:L3G+
NCI-H3122 M1zod2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 MUe3NkBpenN? NW\XUGpbSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDNzMkKgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQj;DR2suQCCjc4PhfUwhUUN3MDC9JFAvODF5NDFOwG0v NXX1OodFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexN|ExPjZpPkK3NVMyODZ4PD;hQi=>
SUP-M2 NGL3OHlCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MX[3NkBpenN? MV7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOXUD3NNkBk\WyuczDh[pRmeiB5MjDodpMh[nliU2LCM2NEUy16IHHzd4F6NCCLQ{WwJF0hOC5yMUe5JO69VS5? NVfnUFdURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexN|ExPjZpPkK3NVMyODZ4PD;hQi=>
NCI-H3122 M2m3PGZ2dmO2aX;uJIF{e2G7 MkXvO|IhcHK| Mn64TY5pcWKrdHnvckBw\iCDTFug[ZhxemW|c3XkJIlvKGi3bXHuJG5EUS2KM{GyNkBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCVUlKvR2NMNThiYYPzZZktKEmFNUCgQUAxNjBzOTFOwG0v M2Sw[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUOxNFY3Lz5{N{GzNVA3PjxxYU6=
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SU-DHL1 MmDIRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NF62Uo04OiCqcoO= Ml\jRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVVT3ETGwyKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIwS0ONLUigZZN{[XluIFnDOVAhRSByLkCyNFUh|ryPLh?= NUTqVlZiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexN|ExPjZpPkK3NVMyODZ4PD;hQi=>
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Ba/F3 MmPRSpVv[3Srb36gZZN{[Xl? MWi3NkBpenN? NUjnUllxUW6qaXLpeIlwdiCxZjDFUWw1NUGOSzDHNVIxOlJibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIH3veZNmKEKjL1[zJINmdGy|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSCPVGOgZZN{[XluIFnDOVAhRSByLkKwO{DPxE1w MnHBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
DFCI114 MUXBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M1nvdVczKGi{cx?= M3XJemFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRF\DTVEyPCClZXzsd{BmgHC{ZYPzbY5oKEWPTEStRWxMKEdzMk[5RUBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hVHWvaX7ld4NmdnRiQ3XscEBXcWGkaXzpeJkhSXO|YYmsJGVEPTBiPTCwMlIxPyEQvF2u NXfDbY9XRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OlgzQDlpPkK2OVY5Ojh7PD;hQi=>
CHLA20 NGXw[HpCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MVi3NkBpenN? NFL4W5hCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPIUGEzOCClZXzsd{BmgHC{ZYPzbY5oKEWPTEStRWxMKFJzMke1VUBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hVHWvaX7ld4NmdnRiQ3XscEBXcWGkaXzpeJkhSXO|YYmsJGVEPTBiPTCwMlQ{KM7:TT6= M4C1OlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
Kelly NUX0PVI4SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M1HuWlczKGi{cx?= MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEunbHz5JINmdGy|IHX4dJJme3OrbnegSW1NPC2DTFugSlEyPzSOIH31eIFvfCCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDMeY1qdmW|Y3XueEBE\WyuIG\pZYJqdGm2eTDBd5NigSxiRVO1NEA:KDBwNEO0JO69VS5? M4fnXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
DFCI76 NFjoRVdCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MYe3NkBpenN? M2PkUGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRF\DTVc3KGOnbHzzJIV5eHKnc4PpcochTU2OND3BUGshVDFzNULSJI12fGGwdDDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BNfW2rbnXzZ4VvfCCFZXzsJHZq[WKrbHn0fUBCe3OjeTygSWM2OCB;IECuOVEyKM7:TT6= NV3VdYZjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OlgzQDlpPkK2OVY5Ojh7PD;hQi=>
LAN5 NGXv[mpCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MUW3NkBpenN? NFuxVIhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzBUlUh[2WubIOg[ZhxemW|c3nu[{BGVUx2LVHMT{BTOTJ5NWGgcZV1[W62IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJGx2dWmwZYPj[Y51KEOnbHygWoli[mmuaYT5JGF{e2G7LDDFR|UxKD1iMD62NVch|ryPLh?= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
SMS-KCNR MWDBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MlX5O|IhcHK| M4P3[WFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU13TMWtEVlJiY3XscJMh\XiycnXzd4lv\yCHTVy0MWFNUyCUMUK3OXEhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKEy3bXnu[ZNk\W62IFPlcIwhXmmjYnnsbZR6KEG|c3H5MEBGSzVyIE2gNE44PjVizszNMi=> MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
SK-N-SH M{DDfWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MXO3NkBpenN? MmDkRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3OMXNJKGOnbHzzJIV5eHKnc4PpcochTU2OND3BUGshTjFzN{TMJI12fGGwdDDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BNfW2rbnXzZ4VvfCCFZXzsJHZq[WKrbHn0fUBCe3OjeTygSWM2OCB;IECuPFczKM7:TT6= M3PkSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
SH-SY5Y NI\iU|ZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NXftXoZjPzJiaILz MVjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOKLWPZOXkh[2WubIOg[ZhxemW|c3nu[{BGVUx2LVHMT{BHOTF5NFygcZV1[W62IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJGx2dWmwZYPj[Y51KEOnbHygWoli[mmuaYT5JGF{e2G7LDDFR|UxKD1iMT6xOUDPxE1w NUS0[mFYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OlgzQDlpPkK2OVY5Ojh7PD;hQi=>
SK-N-BE(2) NETGO2dCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MUC3NkBpenN? M4m2WmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utUk1DTSh{KTDj[YxteyCneIDy[ZN{cW6pIIfpcIQhfHmyZTDFUWw1NUGOSzDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BNfW2rbnXzZ4VvfCCFZXzsJHZq[WKrbHn0fUBCe3OjeTygSWM2OCB;IEGuOVU1KM7:TT6= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
LAN1 M2mzWmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 Mof5O|IhcHK| MkfHRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCOQV6xJINmdGy|IHX4dJJme3OrbnegSW1NPC2DTFugSlEyPzSOIH31eIFvfCCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDMeY1qdmW|Y3XueEBE\WyuIG\pZYJqdGm2eTDBd5NigSxiRVO1NEA:KDJwMEC0JO69VS5? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
SK-N-AS M{PsNGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M{LvNVczKGi{cx?= M1n1dWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utUk1CWyClZXzsd{BmgHC{ZYPzbY5oKHerbHSgeJlx\SCHTVy0MWFNUyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDMeY1qdmW|Y3XueEBE\WyuIG\pZYJqdGm2eTDBd5NigSxiRVO1NEA:KDJwMUO5JO69VS5? NGXp[pY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
SK-N-FI NHLK[3RCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MnfVO|IhcHK| MVPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLV6tSmkh[2WubIOg[ZhxemW|c3nu[{B4cWymIIT5dIUhTU2OND3BUGsh[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9iTIXtbY5me2OnboSgR4VtdCCYaXHibYxqfHliQYPzZZktKEWFNUCgQUAzNjRyMTFOwG0v NHf5PJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
NIH/3T3 MXnBcpRqfHWvb4KgZZN{[Xl? NWrwfW1zPTBibXevb4c> MkOwNVAh\GG7cx?= M{XWcGFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIF7JTE8{XDNiY3XscJMh\XiycnXzd4lv\yCHTVy0MWFNUyCOMUG5Om0hdXW2YX70JJhmdm:pcnHmeIVlKGmwIH71[IUhdW:3c3WgZZN{\XO|ZXSgZZMhfHWvb4Kgd5Rie2m|IHH0JFUxKG2pL3vnMEBxdyCzZDDh[I1qdmm|dHXy[YQh\m:{IEGwJIRigXN? M{HYWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUOxNFY3Lz5{N{GzNVA3PjxxYU6=
NIH/3T3 NXPzVJRwSW62aYT1cY9zKGG|c3H5 MlS4OVAhdWdxa3e= Ml24NVAh\GG7cx?= M4XOfGFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIF7JTE8{XDNiY3XscJMh\XiycnXzd4lv\yCHTVy0MWFNUyCOMUG5Om0hdXW2YX70JJhmdm:pcnHmeIVlKGmwIH71[IUhdW:3c3WgZZN{\XO|ZXSgZZMheGG{dHnhcEB1fW2xcjDy[Ydz\XO|aX;uJIF1KDVyIH3nM4toNCCybzDx[EBi\G2rbnnzeIVz\WRiZn;yJFExKGSjeYO= M2Hld|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUOxNFY3Lz5{N{GzNVA3PjxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pALK / ALK / pAKT / AKT / pERK / ERK / pS6 / S6 ; 

PubMed: 25228534     


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     


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     


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     


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     


(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
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

Kinase Assay:[1]
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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]
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  • 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]
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  • 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 powder
in solvent
Synonyms 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

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 ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04644315 Not yet recruiting Drug: Alectinib Solid Tumors Hoffmann-La Roche January 4 2021 Phase 2
NCT04111705 Recruiting Drug: Lorlatinib Non Small Cell Lung Cancer Metastatic Intergroupe Francophone de Cancerologie Thoracique August 5 2020 Phase 2
NCT03445000 Recruiting Drug: Alectinib Non-small Cell Lung Cancer|Non-small Cell Lung Cancer Metastatic|Non-small Cell Lung Cancer Recurrent European Thoracic Oncology Platform|Hoffmann-La Roche November 6 2018 Phase 2

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID