Serdemetan (JNJ-26854165)

For research use only.

Catalog No.S1172

11 publications

Serdemetan (JNJ-26854165) Chemical Structure

CAS No. 881202-45-5

Serdemetan (JNJ-26854165) 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 Serdemetan (JNJ-26854165) has been cited by 11 publications

6 Customer Reviews

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

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

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

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

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

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

Purity & Quality Control

Choose Selective p53 Inhibitors

Biological Activity

Description Serdemetan (JNJ-26854165) 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 M1P3c2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MknCTY5pcWKrdHnvckBw\iCqdX3hckBMXS1zOT2xPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvQTN{M{[g{txO NIXkXIRUSU6JRWK=
H4 cell NV3KfndjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGPu[2NKdmirYnn0bY9vKG:oIHj1cYFvKEh2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6wOlcxPyEQvF2= MUDTRW5ITVJ?
KGN cell MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEXPRWhKdmirYnn0bY9vKG:oIHj1cYFvKEuJTjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOlIxPSEQvF2= NWi1XpJqW0GQR1XS
786-0 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVHJcohq[mm2aX;uJI9nKGi3bXHuJFc5Pi1yIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63Nlk5QSEQvF2= Mny0V2FPT0WU
769-P cell NXq0O2Z[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEXXZ5hKdmirYnn0bY9vKG:oIHj1cYFvKDd4OT3QJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU45OjJ{NDFOwG0> NWXUN4ZRW0GQR1XS
K5 cell M1n3emdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYLoWolmUW6qaXLpeIlwdiCxZjDoeY1idiCNNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuNFE3OjRizszN MnjLV2FPT0WU
MLMA cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYrJcohq[mm2aX;uJI9nKGi3bXHuJGtQW0NvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuNFMzOTdizszN NFrWe4VUSU6JRWK=
MLMA cell MnjKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH7GdIpKdmirYnn0bY9vKG:oIHj1cYFvKE2OTVGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlI5PzB|IN88US=> MoDNV2FPT0WU
EW-7 cell M17ONmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGVYNTdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkOyOlk2KM7:TR?= MXfTRW5ITVJ?
SW1088 cell NWHOdWtoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYLJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTB6ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuPFA3PTFizszN M3rJUXNCVkeHUh?=
MC-IXC cell MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVfJcohq[mm2aX;uJI9nKGi3bXHuJG1ENUm[QzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuPFc4QTJizszN MlL4V2FPT0WU
NCI-H2052 cell Mm[yS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWXJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkC1NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvODhzNUeg{txO NFS1ZldUSU6JRWK=
IGR-1 cell MnyzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NG[yeJNKdmirYnn0bY9vKG:oIHj1cYFvKEmJUj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4yOjB{ODFOwG0> M{H3NHNCVkeHUh?=
DSH1 cell NXfadmJDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVLJcohq[mm2aX;uJI9nKGi3bXHuJGRUUDFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkK0Nlk3KM7:TR?= M4Lwb3NCVkeHUh?=
PA-1 cell Ml7HS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mnm5TY5pcWKrdHnvckBw\iCqdX3hckBRSS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz6zNFA2Qc7:TR?= M3viO3NCVkeHUh?=
SK-MEL-3 cell MkjIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NE\VWJBKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy5|MUKwO{DPxE1? NUOzW49EW0GQR1XS
SW900 cell NWHpZ|hZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYXJcohq[mm2aX;uJI9nKGi3bXHuJHNYQTByIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz60PFI2PSEQvF2= Mli4V2FPT0WU
CAKI-1 cell NVPyZpdZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M121fmlvcGmkaYTpc44hd2ZiaIXtZY4hS0GNST2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{42Ojd|ODFOwG0> NX7PR2lqW0GQR1XS
ES1 cell NUHhXWg{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Moq4TY5pcWKrdHnvckBw\iCqdX3hckBGWzFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkWyPFk4KM7:TR?= NYnDZ|Q2W0GQR1XS
SK-N-DZ cell NXjJfY9XT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXHKfGluUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3OMWRbKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy54MkW5OUDPxE1? M325NXNCVkeHUh?=
RH-1 cell NUSwcG5QT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGfQcYRKdmirYnn0bY9vKG:oIHj1cYFvKFKKLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlY5PDZ|IN88US=> NEe3V2RUSU6JRWK=
ES8 cell MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUPUWJFnUW6qaXLpeIlwdiCxZjDoeY1idiCHU{igZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlY6PzB{IN88US=> MkO0V2FPT0WU
NEC8 cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWfJcohq[mm2aX;uJI9nKGi3bXHuJG5GSzhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Lke2PVgzKM7:TR?= NGHtPGFUSU6JRWK=
LNCaP-Clone-FGC cell M{PENGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3Pqc2lvcGmkaYTpc44hd2ZiaIXtZY4hVE6FYWCtR4xwdmVvRlfDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{45OzV|NjFOwG0> MWfTRW5ITVJ?
HCE-4 cell NIS2[WxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NULyNnMxUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1WtOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQThyNzFOwG0> NFTtZ5ZUSU6JRWK=
U-118-MG cell MnLrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVjJcohq[mm2aX;uJI9nKGi3bXHuJHUuOTF6LV3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4xOTB4NjFOwG0> M3v1fnNCVkeHUh?=
GI-ME-N cell M{jEe2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mom4TY5pcWKrdHnvckBw\iCqdX3hckBIUS2PRT3OJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4xQDd7NjFOwG0> NIfCVVZUSU6JRWK=
LB1047-RCC cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{DYVGlvcGmkaYTpc44hd2ZiaIXtZY4hVEJzMES3MXJESyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwMU[xOFMh|ryP Mn\kV2FPT0WU
HT-1080 cell M1;LN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1SwWGlvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMUC4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvOTl7MkGg{txO MofoV2FPT0WU
NB69 cell NFztW3dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXPJcohq[mm2aX;uJI9nKGi3bXHuJG5DPjliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkO1NFQ4KM7:TR?= M1fSUHNCVkeHUh?=
NCI-H1693 cell MoLuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF;pNXRKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVY6OyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwNES4PVUh|ryP M2C4VHNCVkeHUh?=
HSC-3 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYPJcohq[mm2aX;uJI9nKGi3bXHuJGhUSy1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND60PVk{OyEQvF2= NGiyNIZUSU6JRWK=
MDA-MB-231 cell MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlzNTY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtNlMyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC53NUi5PUDPxE1? NHHHWFhUSU6JRWK=
HOS cell NXz4WJkyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFzmUFdKdmirYnn0bY9vKG:oIHj1cYFvKEiRUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuO|g3OyEQvF2= NH;I[m5USU6JRWK=
BT-549 cell NUjXcpFDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWS1cmw4UW6qaXLpeIlwdiCxZjDoeY1idiCEVD21OFkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njd6OEeg{txO M{HucHNCVkeHUh?=
NB17 cell NVTMTos2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVHpd4QyUW6qaXLpeIlwdiCxZjDoeY1idiCQQkG3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE44QDl5NjFOwG0> MlzPV2FPT0WU
5637 cell M3rEbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml3XTY5pcWKrdHnvckBw\iCqdX3hckA2PjN5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND63PVY2OiEQvF2= Mne5V2FPT0WU
OVCAR-8 cell MoS5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MULJcohq[mm2aX;uJI9nKGi3bXHuJG9XS0GULUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlkzPDN4IN88US=> NIDVZXZUSU6JRWK=
G-402 cell NEHMfm1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVHETFRpUW6qaXLpeIlwdiCxZjDoeY1idiCJLUSwNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQTNyM{Wg{txO MW\TRW5ITVJ?
BB30-HNC cell MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlLDTY5pcWKrdHnvckBw\iCqdX3hckBDSjNyLVjOR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvODd{MUig{txO MUfTRW5ITVJ?
HCC1806 cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{LidmlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMUiwOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvODh|M{mg{txO MXLTRW5ITVJ?
COLO-800 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUHJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vOECwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4yOjZ2IN88US=> NUGwU2NSW0GQR1XS
FADU cell M4P4cGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mki1TY5pcWKrdHnvckBw\iCqdX3hckBHSUSXIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT6zOlU2PyEQvF2= MkXsV2FPT0WU
NCI-H1651 cell NYDCRpNTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHG1XodKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVY2OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwM{m0NFkh|ryP M{L6bXNCVkeHUh?=
AGS cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVnJcohq[mm2aX;uJI9nKGi3bXHuJGFIWyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwNEe3NVEh|ryP NFT3WI1USU6JRWK=
CHP-212 cell NGLHc|ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3z4SGlvcGmkaYTpc44hd2ZiaIXtZY4hS0iSLUKxNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvOzl2MEmg{txO M16wN3NCVkeHUh?=
YAPC cell NIXXXZFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NU\Xc5FIUW6qaXLpeIlwdiCxZjDoeY1idiC\QWDDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU41PzdzMTFOwG0> NXrSU|Y4W0GQR1XS
GOTO cell M3fsRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGLhfnlKdmirYnn0bY9vKG:oIHj1cYFvKEeRVF:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlQ6PTd4IN88US=> MYPTRW5ITVJ?
KYSE-510 cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1yzcWlvcGmkaYTpc44hd2ZiaIXtZY4hU1mVRT21NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjVzMTFOwG0> M4mwOXNCVkeHUh?=
NCI-H2342 cell MnexS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYTJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkO0NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPTN{N{ig{txO M2juT3NCVkeHUh?=
BFTC-905 cell M4rsOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnjMTY5pcWKrdHnvckBw\iCqdX3hckBDTlSFLUmwOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPjJ6M{Wg{txO MUjTRW5ITVJ?
EW-16 cell NUTMUIFYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFLIb|VKdmirYnn0bY9vKG:oIHj1cYFvKEWZLUG2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU44OjB7MzFOwG0> MmPjV2FPT0WU
SK-MEL-30 cell MYHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVHJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2zNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPzR3NEOg{txO MonDV2FPT0WU
HLE cell NED4NVVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NX\vNWc2UW6qaXLpeIlwdiCxZjDoeY1idiCKTFWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlc4PDh7IN88US=> M2HENXNCVkeHUh?=
T98G cell NWXqcnZYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEjBe2tKdmirYnn0bY9vKG:oIHj1cYFvKFR7OFegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlc6PjN3IN88US=> NHvIcYNUSU6JRWK=
HUTU-80 cell NUPMWFR1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF24S3NKdmirYnn0bY9vKG:oIHj1cYFvKEiXVGWtPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njh2MkK4JO69VQ>? NIDQdG1USU6JRWK=
NOS-1 cell Mn\RS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV74bG5bUW6qaXLpeIlwdiCxZjDoeY1idiCQT2OtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQTR5Nk[g{txO MoPNV2FPT0WU
SW780 cell M3jqdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV;6eHMzUW6qaXLpeIlwdiCxZjDoeY1idiCVV{e4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQTZ7NEmg{txO NH25V4pUSU6JRWK=
KYSE-180 cell NYfmS2VJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV3H[XFEUW6qaXLpeIlwdiCxZjDoeY1idiCNWWPFMVE5OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwOUe2OVQh|ryP MorpV2FPT0WU
MDA-MB-361 cell NEfyR2VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlG4TY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtN|YyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS57OE[0O{DPxE1? NFfzfpRUSU6JRWK=
SNU-C2B cell M3PNXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkPJTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvQ{LCJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok4xOTF|ODFOwG0> M4L4XnNCVkeHUh?=
NCI-H661 cell MnrKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3vEN2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi2OlEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjB4OUSg{txO NVrPUohiW0GQR1XS
OE33 cell M33xe2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3KwemlvcGmkaYTpc44hd2ZiaIXtZY4hV0V|MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[uNVQ{QDlizszN MVPTRW5ITVJ?
TYK-nu cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYXQbZhDUW6qaXLpeIlwdiCxZjDoeY1idiCWWVutcpUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjJzOE[zJO69VQ>? MW\TRW5ITVJ?
COLO-792 cell NXjiOWl6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmK3TY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLUe5NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvOjV{MUmg{txO NX7VOnR1W0GQR1XS
HEL cell M{Djb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NG\yXoJKdmirYnn0bY9vKG:oIHj1cYFvKEiHTDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[uNlY4PiEQvF2= NH\HPYVUSU6JRWK=
D-566MG cell NUPGTGlST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGi4cWdKdmirYnn0bY9vKG:oIHj1cYFvKERvNU[2UWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjN|NEmxJO69VQ>? M3vDRnNCVkeHUh?=
U031 cell NWTafWV7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF7ycGVKdmirYnn0bY9vKG:oIHj1cYFvKFVyM{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlQyQDF4IN88US=> NV;3T|dqW0GQR1XS
COR-L23 cell MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXXJcohq[mm2aX;uJI9nKGi3bXHuJGNQWi2OMkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlQ{OzR4IN88US=> NIeyOm5USU6JRWK=
NCI-H2452 cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVvJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkS1NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvPTJ{OEGg{txO M3XKcnNCVkeHUh?=
BB65-RCC cell MlT0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3XzemlvcGmkaYTpc44hd2ZiaIXtZY4hSkJ4NT3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjZ2NUmg{txO MUDTRW5ITVJ?
CAL-33 cell NXj1dWY{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWTJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC1|MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[uOlU3PjVizszN NFvOW4xUSU6JRWK=

... 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.
  • Dosages: ≤20 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 66 mg/mL (200.96 mM)
Water Insoluble
Ethanol '2 mg/mL
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 C1=CC=C2C(=C1)C(=CN2)CCNC3=CC=C(C=C3)NC4=CC=NC=C4

In vivo Formulation Calculator (Clear solution)

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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)

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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).

Dilution Calculator

Dilution Calculator

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

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

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

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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00676910 Completed Drug: JNJ-26854165 Neoplasms Johnson & Johnson Pharmaceutical Research & Development L.L.C. November 2006 Phase 1

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.

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p53 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID