JNJ-26854165 (Serdemetan)

For research use only. Not for use in humans.

Catalog No.S1172

7 publications

JNJ-26854165 (Serdemetan) Chemical Structure

Molecular Weight(MW): 328.41

JNJ-26854165 (Serdemetan) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53. Phase 1.

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Selleck's JNJ-26854165 (Serdemetan) has been cited by 7 publications

6 Customer Reviews

  • Mol Pharmacol 2014 85(3), 408-19. JNJ-26854165 (Serdemetan) purchased from Selleck.

    Sci Rep 2014 4, 4663. JNJ-26854165 (Serdemetan) purchased from Selleck.

  • Sci Rep 2014 4, 4663. JNJ-26854165 (Serdemetan) purchased from Selleck.

    Sci Rep 2014 4, 4663. JNJ-26854165 (Serdemetan) purchased from Selleck.

  • J Nat Med 2013 10.1007/s11418-014-0825-0. JNJ-26854165 (Serdemetan) purchased from Selleck.

    Curr Protoc Chem Biol 2013 5(3), 195-212. JNJ-26854165 (Serdemetan) purchased from Selleck.

Purity & Quality Control

Choose Selective p53 Inhibitors

Biological Activity

Description JNJ-26854165 (Serdemetan) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53. Phase 1.
Targets
p53 [1]
(Cell-free assay)
HDM2 [1]
(Cell-free assay)
Mdm2 [2]
(Cell-free assay)
In vitro

JNJ 26854165 is a novel tryptamine derivative which activates p53 and acts as a HDM2 ubiquitin ligase antagonist. JNJ 26854165 inhibits cell growth and induces apoptosis in leukemia cell lines with IC50 values of 0.24, 0.33, 0.32 and 0.44 μM at 72 hours for OCI-AML-3, MOLM-13, NALM-6 and REH cells, respectively. In addition, JNJ 26854165 accelerates proteasome-mediated degradation of p21 and antagonizes the transcriptional induction of p21 by p53. It also induces S-phase delay and upregulates E2F1 expression in p53 mutant cells, resulting in preferential apoptosis of S-phase cells. [1] JNJ 26854165 is an oral Mdm2 inhibitor which can inhibit the interaction of Mdm2-p53 complex with the proteasome and increase p53 levels by binding to RING domain of Mdm2. [2] A recent study shows that JNJ 26854165 inhibits clonogenic survival in four human cancer cell lines: H460, A549, p53-WT-HCT116, and p53-null-HCT116. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KU-19-19 cell M3[0OWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV23SpRVUW6qaXLpeIlwdiCxZjDoeY1idiCNVT2xPU0yQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwOUOyN|Yh|ryP NF;DR5RUSU6JRWK=
H4 cell MnfUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGfXOWZKdmirYnn0bY9vKG:oIHj1cYFvKEh2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6wOlcxPyEQvF2= MW\TRW5ITVJ?
KGN cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVvJcohq[mm2aX;uJI9nKGi3bXHuJGtIViClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNkKwOUDPxE1? NWTpbmJyW0GQR1XS
786-0 cell M1rMPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV7Jcohq[mm2aX;uJI9nKGi3bXHuJFc5Pi1yIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63Nlk5QSEQvF2= M2jKS3NCVkeHUh?=
769-P cell NF35cHNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn3mTY5pcWKrdHnvckBw\iCqdX3hckA4PjlvUDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPFIzOjRizszN MYfTRW5ITVJ?
K5 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYLqNYtCUW6qaXLpeIlwdiCxZjDoeY1idiCNNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuNFE3OjRizszN M4LlOXNCVkeHUh?=
MLMA cell M2\1OGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGmy[WZKdmirYnn0bY9vKG:oIHj1cYFvKEuRU1OtNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvODN{MUeg{txO MUnTRW5ITVJ?
MLMA cell M3vjWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVPJcohq[mm2aX;uJI9nKGi3bXHuJG1NVUFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkK4O|A{KM7:TR?= M4XWXHNCVkeHUh?=
EW-7 cell NHPGU|VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYXJcohq[mm2aX;uJI9nKGi3bXHuJGVYNTdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkOyOlk2KM7:TR?= MXnTRW5ITVJ?
SW1088 cell NYT0d4t5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NG\tfVFKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUC4PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQDB4NUGg{txO NVj4VXhIW0GQR1XS
MC-IXC cell Mkj6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEPIVWdKdmirYnn0bY9vKG:oIHj1cYFvKE2FLVnYR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQDd5OUKg{txO NHOxNGxUSU6JRWK=
NCI-H2052 cell M2nBNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3ftVGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFUzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy5yOEG1O{DPxE1? M2PZXXNCVkeHUh?=
IGR-1 cell NILRdFRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYrYfnk2UW6qaXLpeIlwdiCxZjDoeY1idiCLR2KtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvOTJyMkig{txO MmTVV2FPT0WU
DSH1 cell NWjSU2JRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml7XTY5pcWKrdHnvckBw\iCqdX3hckBFW0hzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz6yOFI6PiEQvF2= MojBV2FPT0WU
PA-1 cell NXrXZnJYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MW\Jcohq[mm2aX;uJI9nKGi3bXHuJHBCNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkOwNFU6|ryP NXPFNoJVW0GQR1XS
SK-MEL-3 cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHi4V4xKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy5|MUKwO{DPxE1? NFnCXmJUSU6JRWK=
SW900 cell NXnsd4dwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXfJN3NJUW6qaXLpeIlwdiCxZjDoeY1idiCVV{mwNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvPDh{NUWg{txO MUTTRW5ITVJ?
CAKI-1 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{K1SmlvcGmkaYTpc44hd2ZiaIXtZY4hS0GNST2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{42Ojd|ODFOwG0> MYjTRW5ITVJ?
ES1 cell M2nPSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUXubnlVUW6qaXLpeIlwdiCxZjDoeY1idiCHU{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlUzQDl5IN88US=> NYTJOJl1W0GQR1XS
SK-N-DZ cell MmT3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV\iOGNPUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3OMWRbKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy54MkW5OUDPxE1? M2W1RnNCVkeHUh?=
RH-1 cell NWjORWJvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGTFZZVKdmirYnn0bY9vKG:oIHj1cYFvKFKKLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlY5PDZ|IN88US=> Mlf0V2FPT0WU
ES8 cell NGHQcm9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUHmc4l4UW6qaXLpeIlwdiCxZjDoeY1idiCHU{igZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlY6PzB{IN88US=> NXHxZVg3W0GQR1XS
NEC8 cell MlzTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mo\rTY5pcWKrdHnvckBw\iCqdX3hckBPTUN6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz63Olk5OiEQvF2= NIeyS4dUSU6JRWK=
LNCaP-Clone-FGC cell NHPFOnhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MknkTY5pcWKrdHnvckBw\iCqdX3hckBNVkOjUD3DcI9v\S2IR1OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlg{PTN4IN88US=> M1LJWnNCVkeHUh?=
HCE-4 cell MU\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkXETY5pcWKrdHnvckBw\iCqdX3hckBJS0VvNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPVgxPyEQvF2= M2npT3NCVkeHUh?=
U-118-MG cell M3vQUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NI\C[GxKdmirYnn0bY9vKG:oIHj1cYFvKFVvMUG4MW1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5yMUC2OkDPxE1? MYXTRW5ITVJ?
GI-ME-N cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mlq5TY5pcWKrdHnvckBw\iCqdX3hckBIUS2PRT3OJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4xQDd7NjFOwG0> MW\TRW5ITVJ?
LB1047-RCC cell NGGzc|dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHuwNXhKdmirYnn0bY9vKG:oIHj1cYFvKEyEMUC0O{1TS0NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkG2NVQ{KM7:TR?= MlLNV2FPT0WU
HT-1080 cell MoPzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NE\Jfo9KdmirYnn0bY9vKG:oIHj1cYFvKEiWLUGwPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjF7OUKxJO69VQ>? MWnTRW5ITVJ?
NB69 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2DtU2lvcGmkaYTpc44hd2ZiaIXtZY4hVkJ4OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuN|UxPDdizszN NEfZVGZUSU6JRWK=
NCI-H1693 cell NXqyZYxIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2jQcWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOlk{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC52NEi5OUDPxE1? MWnTRW5ITVJ?
HSC-3 cell NVzFSHFTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MojFTY5pcWKrdHnvckBw\iCqdX3hckBJW0NvMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuOFk6OzNizszN NGjzdmhUSU6JRWK=
MDA-MB-231 cell M1vyUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYLJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2yN|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjV3OEm5JO69VQ>? M2r2WHNCVkeHUh?=
HOS cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXHJcohq[mm2aX;uJI9nKGi3bXHuJGhQWyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwN{i2N{DPxE1? NEHK[nVUSU6JRWK=
BT-549 cell Mmn5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH;pdIxKdmirYnn0bY9vKG:oIHj1cYFvKEKWLUW0PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvPzh6NzFOwG0> NXq4bVkxW0GQR1XS
NB17 cell MnrvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1nNTmlvcGmkaYTpc44hd2ZiaIXtZY4hVkJzNzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuO|g6PzZizszN MmXvV2FPT0WU
5637 cell MnXKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUjJcohq[mm2aX;uJI9nKGi3bXHuJFU3OzdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12Lke5OlUzKM7:TR?= MkLuV2FPT0WU
OVCAR-8 cell M4LtUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlvRTY5pcWKrdHnvckBw\iCqdX3hckBQXkODUj24JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE46OjR|NjFOwG0> MVLTRW5ITVJ?
G-402 cell NULyPW1oT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NI\jZXdKdmirYnn0bY9vKG:oIHj1cYFvKEdvNECyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE46OzB|NTFOwG0> MkHJV2FPT0WU
BB30-HNC cell MkXPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mme5TY5pcWKrdHnvckBw\iCqdX3hckBDSjNyLVjOR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvODd{MUig{txO M1zEcXNCVkeHUh?=
HCC1806 cell Mn7jS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnPVTY5pcWKrdHnvckBw\iCqdX3hckBJS0NzOEC2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4xQDN|OTFOwG0> M3T3V3NCVkeHUh?=
COLO-800 cell NGjCc3VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHrCUG1KdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tPFAxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS5zMk[0JO69VQ>? M4K0OHNCVkeHUh?=
FADU cell NEO0WFlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mmm4TY5pcWKrdHnvckBw\iCqdX3hckBHSUSXIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT6zOlU2PyEQvF2= NXX6b|RGW0GQR1XS
NCI-H1651 cell MorsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEDmOXdKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVY2OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwM{m0NFkh|ryP MnyzV2FPT0WU
AGS cell NFnidmRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnnhTY5pcWKrdHnvckBw\iCqdX3hckBCT1NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkS3O|EyKM7:TR?= MnPGV2FPT0WU
CHP-212 cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVHJcohq[mm2aX;uJI9nKGi3bXHuJGNJWC1{MUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlM6PDB7IN88US=> MYnTRW5ITVJ?
YAPC cell M3GzVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NITuVXpKdmirYnn0bY9vKG:oIHj1cYFvKFmDUFOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlQ4PzFzIN88US=> M3PRVHNCVkeHUh?=
GOTO cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV7yRpNPUW6qaXLpeIlwdiCxZjDoeY1idiCJT2TPJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU41QTV5NjFOwG0> M{Xl[HNCVkeHUh?=
KYSE-510 cell MnjvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF7Ce5dKdmirYnn0bY9vKG:oIHj1cYFvKEu\U1WtOVExKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS53MUGg{txO M3vD[HNCVkeHUh?=
NCI-H2342 cell M1nlfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYPJdpR3UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI{PDJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkWzNlc5KM7:TR?= Ml7IV2FPT0WU
BFTC-905 cell MortS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWfJcohq[mm2aX;uJI9nKGi3bXHuJGJHXENvOUC1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU43Ojh|NTFOwG0> MnfoV2FPT0WU
EW-16 cell NVXZSpM6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX7COXdRUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPzJyOUOg{txO Ml2yV2FPT0WU
SK-MEL-30 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnTSTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytN|Ah[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njd2NUSzJO69VQ>? M2LWOHNCVkeHUh?=
HLE cell NX62SY1HT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnLtTY5pcWKrdHnvckBw\iCqdX3hckBJVEViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13Lke3OFg6KM7:TR?= M4O3cXNCVkeHUh?=
T98G cell M1LLNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3zBcmlvcGmkaYTpc44hd2ZiaIXtZY4hXDl6RzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuO|k3OzVizszN NGrZZphUSU6JRWK=
HUTU-80 cell NH:2OJJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXHPT|RrUW6qaXLpeIlwdiCxZjDoeY1idiCKVWTVMVgxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS56NEKyPEDPxE1? NIP5OnJUSU6JRWK=
NOS-1 cell NF;Jb|hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3nsUGlvcGmkaYTpc44hd2ZiaIXtZY4hVk:VLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlk1PzZ4IN88US=> NVy0XG95W0GQR1XS
SW780 cell M{XTVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXPKcGZtUW6qaXLpeIlwdiCxZjDoeY1idiCVV{e4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQTZ7NEmg{txO MnGzV2FPT0WU
KYSE-180 cell NHrYUIxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkXqTY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUG4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQTd4NUSg{txO Mk\IV2FPT0WU
MDA-MB-361 cell NHvu[JZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MY\Jcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2zOlEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njl6NkS3JO69VQ>? NEXZXHlUSU6JRWK=
SNU-C2B cell M4nObWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mnf4TY5pcWKrdHnvckBw\iCqdX3hckBUVlVvQ{LCJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok4xOTF|ODFOwG0> NUi5UFFkW0GQR1XS
NCI-H661 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIDrWmZKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IOlYyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Pi5yNkm0JO69VQ>? M4TIS3NCVkeHUh?=
OE33 cell MkPhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWrJcohq[mm2aX;uJI9nKGi3bXHuJG9GOzNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD14LkG0N|g6KM7:TR?= NWDCR49RW0GQR1XS
TYK-nu cell M2SzcWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXjJcohq[mm2aX;uJI9nKGi3bXHuJHR[Uy2wdTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[uNlE5PjNizszN M{mzenNCVkeHUh?=
COLO-792 cell NHfDZ4tIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmTITY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLUe5NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvOjV{MUmg{txO MYTTRW5ITVJ?
HEL cell NF\TfZZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGXONo1KdmirYnn0bY9vKG:oIHj1cYFvKEiHTDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[uNlY4PiEQvF2= NIOyN2lUSU6JRWK=
D-566MG cell NF;3eGpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHS1THZKdmirYnn0bY9vKG:oIHj1cYFvKERvNU[2UWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjN|NEmxJO69VQ>? M4PEd3NCVkeHUh?=
U031 cell Ml3oS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NETufFFKdmirYnn0bY9vKG:oIHj1cYFvKFVyM{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlQyQDF4IN88US=> NGW5W|FUSU6JRWK=
COR-L23 cell NHHjdo9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVnJcohq[mm2aX;uJI9nKGi3bXHuJGNQWi2OMkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlQ{OzR4IN88US=> NGjqUndUSU6JRWK=
NCI-H2452 cell MlW1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX\lOWRUUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI1PTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD14LkWyNlgyKM7:TR?= MWHTRW5ITVJ?
BB65-RCC cell MmXPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{GzOWlvcGmkaYTpc44hd2ZiaIXtZY4hSkJ4NT3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjZ2NUmg{txO MmjFV2FPT0WU
CAL-33 cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MU\Jcohq[mm2aX;uJI9nKGi3bXHuJGNCVC1|MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[uOlU3PjVizszN MWnTRW5ITVJ?

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p53 / HDM2 / HDMX / p21 / Noxa / Puma ; 

PubMed: 20736344     


OCI-AML-3 and MOLM-13 cells were incubated with a range of concentrations of JNJ-26854165 for 18 hours.

ABCA1 / ABCG1 / NPC1 / NPC2 / HMGcoR ; 

PubMed: 23820125     


U266 and JeKo-1 cells were treated with JNJ-26854165 and cells harvested at the indicated time points.

MDM2 / p-MDM2 / p53 ; 

PubMed: 27999193     


K562 cells was harvested at 48 h after treatment with various JNJ-165 concentrations, and then nuclear and cytoplasmic extracts were prepared to check the levels of p53, MDM2 and p-MDM2 by Western blotting. Actin and LaminB were used as loading control respectively.

Bcr-abl / p-Bcr-abl / p-CrkL / STAT5 / p-STAT5 / STAT3 / p-STAT3 ; 

PubMed: 27999193     


CML cell lines were treated with JNJ-165 at the indicated doses for 48 h. Whole-cell lysates were extracted to assess the levels of BCR-ABL and phosphorylated (p)-BCR-ABL (Tyr177), and then were analyzed for BCR-ABL downstream signaling mediators p-CrkL (Try207), total Stat5, p-Stat5 (Tyr694), total Stat3, and p-Stat3 (Ser727) expression by Western blot analysis. The expression of β-actin was used as loading control. The data are representative of three determinations with identical results.

20736344 23820125 27999193
Growth inhibition assay
Cell viability; 

PubMed: 23820125     


MCL (B) and MM (C) cell lines were seeded in 96-well plates for viability analyses using WST-1 and treated with JNJ-26854165 for 72 hours. Results are expressed as the percentage of cell viability in relation to the vehicle-treated sample for each cell line, which was arbitrarily set at 100%

23820125
Immunofluorescence
p53; 

PubMed: 27999193     


Two-color fluorescence microscope analysis of antibody against p53 protein (green) and nuclei (DAPI staining, blue) showed nuclear accumulation of p53 in K562 cells with treatment of 1 μM JNJ-165, but not in control-treated cells after 48 h. Images were taken on a fluorescence microscopy (100×).

27999193
In vivo JNJ 26854165 leads to significant differences in EFS distribution in 17 of the 36 (47%) evaluable solid tumor xenografts and in 5 of 7 (71%) of the evaluable ALL xenografts using a dose of 20 mg/kg administered via oral gavage daily for 5 days, repeated for 6 weeks. [4]

Protocol

Cell Research:[1]
- Collapse
  • Cell lines: OCI-AML-3, MOLM-13, NB4 and U937 cells
  • Concentrations: 0-10 μM
  • Incubation Time: 72 hours
  • Method: Cell lines are maintained in RPMI 1640 medium containing 10% heat-inactivated fetal calf serum (FCS). OCI-AML-3, MOLM-13, NB4 and U937 cells are derived from acute myelogenous leukemia (AML) patients, K562 from a chronic myelogenous leukemia (CML) patient in blast crisis, and NALM-6, REH, P12-ICHIK
    (Only for Reference)
Animal Research:[4]
- Collapse
  • Animal Models: CB17SC scid-/- female mice.
  • Formulation: JNJ-26854165 is dissolved in DMSO and then diluted in water.
  • Dosages: ≤20 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 66 mg/mL (200.96 mM)
Ethanol 2 mg/mL (6.08 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
30 mg/mL

* 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 328.41
Formula

C21H20N4

CAS No. 881202-45-5
Storage powder
in solvent
Synonyms N/A
Smiles C(CC1=C[NH]C2=CC=CC=C12)NC3=CC=C(NC4=CC=NC=C4)C=C3

Bio Calculators

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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)

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*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).

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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 )

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

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Mass Concentration Volume Molecular Weight

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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p53 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID