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.

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 Mki3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmT1TY5pcWKrdHnvckBw\iCqdX3hckBMXS1zOT2xPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvQTN{M{[g{txO MknSV2FPT0WU
H4 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{fHfWlvcGmkaYTpc44hd2ZiaIXtZY4hUDRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkC2O|A4KM7:TR?= MXXTRW5ITVJ?
KGN cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1rSS2lvcGmkaYTpc44hd2ZiaIXtZY4hU0eQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT62NlA2KM7:TR?= NXnleHVNW0GQR1XS
786-0 cell NIXxb45Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFHvXFhKdmirYnn0bY9vKG:oIHj1cYFvKDd6Nj2wJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU44Ojl6OTFOwG0> MVLTRW5ITVJ?
769-P cell MmDTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn3MTY5pcWKrdHnvckBw\iCqdX3hckA4PjlvUDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPFIzOjRizszN NHXpXppUSU6JRWK=
K5 cell NHHTVXRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUjJcohq[mm2aX;uJI9nKGi3bXHuJGs2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi5yMU[yOEDPxE1? MUDTRW5ITVJ?
MLMA cell NXn3cZltT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3TafWlvcGmkaYTpc44hd2ZiaIXtZY4hU0:VQz2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4xOzJzNzFOwG0> MmXEV2FPT0WU
MLMA cell NEHEbGFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWHJcohq[mm2aX;uJI9nKGi3bXHuJG1NVUFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkK4O|A{KM7:TR?= NULQN4tkW0GQR1XS
EW-7 cell Ml60S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoHpTY5pcWKrdHnvckBw\iCqdX3hckBGXy15IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj6zNlY6PSEQvF2= MWfTRW5ITVJ?
SW1088 cell NF;u[opIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHPwZXBKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUC4PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQDB4NUGg{txO NUT2dFN{W0GQR1XS
MC-IXC cell M4Dp[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXy3XoRlUW6qaXLpeIlwdiCxZjDoeY1idiCPQz3JXGMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjh5N{myJO69VQ>? NFrxTnJUSU6JRWK=
NCI-H2052 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGHI[lhKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlA2OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNwMEixOVch|ryP Mn:0V2FPT0WU
IGR-1 cell M4T0VGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIXk[JNKdmirYnn0bY9vKG:oIHj1cYFvKEmJUj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4yOjB{ODFOwG0> MlXLV2FPT0WU
DSH1 cell NFrwVWFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1;jdGlvcGmkaYTpc44hd2ZiaIXtZY4hTFOKMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuNlQzQTZizszN NILUXHZUSU6JRWK=
PA-1 cell NHfWO5NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkT3TY5pcWKrdHnvckBw\iCqdX3hckBRSS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz6zNFA2Qc7:TR?= NUjwXHUyW0GQR1XS
SK-MEL-3 cell M3nPb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2HiOWlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjNzMkC3JO69VQ>? M361TnNCVkeHUh?=
SW900 cell NUj4ZndpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYHINHJvUW6qaXLpeIlwdiCxZjDoeY1idiCVV{mwNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvPDh{NUWg{txO MnT3V2FPT0WU
CAKI-1 cell M3S2XWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWXJcohq[mm2aX;uJI9nKGi3bXHuJGNCU0lvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuOVI4OzhizszN MV\TRW5ITVJ?
ES1 cell MYHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEXjWm1KdmirYnn0bY9vKG:oIHj1cYFvKEWVMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuOVI5QTdizszN M3;XV3NCVkeHUh?=
SK-N-DZ cell Ml6yS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mme5TY5pcWKrdHnvckBw\iCqdX3hckBUUy2QLVTaJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{43OjV7NTFOwG0> NIj5eHBUSU6JRWK=
RH-1 cell M37Q[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV7tfWNNUW6qaXLpeIlwdiCxZjDoeY1idiCUSD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{43QDR4MzFOwG0> Mki4V2FPT0WU
ES8 cell MnPkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH;3SVVKdmirYnn0bY9vKG:oIHj1cYFvKEWVODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuOlk4ODJizszN NHPid4dUSU6JRWK=
NEC8 cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWnJcohq[mm2aX;uJI9nKGi3bXHuJG5GSzhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Lke2PVgzKM7:TR?= NGHiPXNUSU6JRWK=
LNCaP-Clone-FGC cell M{TsdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWjvdWNwUW6qaXLpeIlwdiCxZjDoeY1idiCOTlPhVE1EdG:wZT3GS2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Njh|NUO2JO69VQ>? MYPTRW5ITVJ?
HCE-4 cell M1jOVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlLPTY5pcWKrdHnvckBw\iCqdX3hckBJS0VvNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPVgxPyEQvF2= MYnTRW5ITVJ?
U-118-MG cell NYG5V2ltT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoDMTY5pcWKrdHnvckBw\iCqdX3hckBWNTFzOD3NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvODFyNk[g{txO NIPmPHZUSU6JRWK=
GI-ME-N cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NU\KeYdQUW6qaXLpeIlwdiCxZjDoeY1idiCJST3NSU1PKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5yOEe5OkDPxE1? M4\yfHNCVkeHUh?=
LB1047-RCC cell NEHhfGJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVnyXoJCUW6qaXLpeIlwdiCxZjDoeY1idiCOQkGwOFcuWkOFIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND6xOlE1OyEQvF2= NXXZWI1rW0GQR1XS
HT-1080 cell Ml3yS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1T2VWlvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMUC4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvOTl7MkGg{txO MV7TRW5ITVJ?
NB69 cell NHH2NWJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWfJVYM1UW6qaXLpeIlwdiCxZjDoeY1idiCQQk[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4{PTB2NzFOwG0> M1TLc3NCVkeHUh?=
NCI-H1693 cell Mny0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWPJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMU[5N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvPDR6OUWg{txO M4\0RXNCVkeHUh?=
HSC-3 cell NFfXSHJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3riTWlvcGmkaYTpc44hd2ZiaIXtZY4hUFOFLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlQ6QTN|IN88US=> NHK2U|VUSU6JRWK=
MDA-MB-231 cell NEXLN4pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFn0V2RKdmirYnn0bY9vKG:oIHj1cYFvKE2GQT3NRk0zOzFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkW1PFk6KM7:TR?= NVriW3JEW0GQR1XS
HOS cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmPOTY5pcWKrdHnvckBw\iCqdX3hckBJV1NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12Lke4OlMh|ryP NX\xWHNKW0GQR1XS
BT-549 cell MkfPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NULhZ2JjUW6qaXLpeIlwdiCxZjDoeY1idiCEVD21OFkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njd6OEeg{txO NHLHPJpUSU6JRWK=
NB17 cell Mn7yS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{TscWlvcGmkaYTpc44hd2ZiaIXtZY4hVkJzNzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuO|g6PzZizszN NV;ZRng{W0GQR1XS
5637 cell MnK5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIi5XnRKdmirYnn0bY9vKG:oIHj1cYFvKDV4M{egZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlc6PjV{IN88US=> NWXhVZhwW0GQR1XS
OVCAR-8 cell MmrxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NU\hd5NsUW6qaXLpeIlwdiCxZjDoeY1idiCRVlPBVk05KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC57MkSzOkDPxE1? MkfIV2FPT0WU
G-402 cell NGK5ZVJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWTJcohq[mm2aX;uJI9nKGi3bXHuJGcuPDB{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND65N|A{PSEQvF2= MVHTRW5ITVJ?
BB30-HNC cell MkjPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1X2[mlvcGmkaYTpc44hd2ZiaIXtZY4hSkJ|MD3IUmMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjB5MkG4JO69VQ>? NVTvT2J6W0GQR1XS
HCC1806 cell MnnzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mk\RTY5pcWKrdHnvckBw\iCqdX3hckBJS0NzOEC2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4xQDN|OTFOwG0> NIq1VFJUSU6JRWK=
COLO-800 cell MknSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWTJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vOECwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4yOjZ2IN88US=> NULQcG9jW0GQR1XS
FADU cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NG\DeWpKdmirYnn0bY9vKG:oIHj1cYFvKE[DRGWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlM3PTV5IN88US=> M3;kXHNCVkeHUh?=
NCI-H1651 cell NYjHelZUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWfGfGpiUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE3PTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkO5OFA6KM7:TR?= NEHwdZFUSU6JRWK=
AGS cell Mn\uS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1POS2lvcGmkaYTpc44hd2ZiaIXtZY4hSUeVIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT60O|cyOSEQvF2= MWHTRW5ITVJ?
CHP-212 cell M37CXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHrzcZdKdmirYnn0bY9vKG:oIHj1cYFvKEOKUD2yNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjN7NEC5JO69VQ>? NUjPXVhlW0GQR1XS
YAPC cell NFPNPFZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{Dt[GlvcGmkaYTpc44hd2ZiaIXtZY4hYUGSQzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuOFc4OTFizszN M33TTXNCVkeHUh?=
GOTO cell MmnpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVPkfGZQUW6qaXLpeIlwdiCxZjDoeY1idiCJT2TPJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU41QTV5NjFOwG0> NFrSU5pUSU6JRWK=
KYSE-510 cell MoDlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXrZT2N1UW6qaXLpeIlwdiCxZjDoeY1idiCNWWPFMVUyOCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwNUGxJO69VQ>? M{naeXNCVkeHUh?=
NCI-H2342 cell MmjFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXXJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkO0NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPTN{N{ig{txO M4LYfnNCVkeHUh?=
BFTC-905 cell NYrxO5NlT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUfYZ2FTUW6qaXLpeIlwdiCxZjDoeY1idiCERmTDMVkxPSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwNkK4N|Uh|ryP MYrTRW5ITVJ?
EW-16 cell NGDRU5dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2HpfGlvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlczODl|IN88US=> M2f6bnNCVkeHUh?=
SK-MEL-30 cell NYn6fo9TT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYTJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2zNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPzR3NEOg{txO NH;JPVBUSU6JRWK=
HLE cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF\aRZVKdmirYnn0bY9vKG:oIHj1cYFvKEiORTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuO|c1QDlizszN NXK1WlFXW0GQR1XS
T98G cell NE\JPGZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHHlOmFKdmirYnn0bY9vKG:oIHj1cYFvKFR7OFegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlc6PjN3IN88US=> M1jFW3NCVkeHUh?=
HUTU-80 cell MkDxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH3q[otKdmirYnn0bY9vKG:oIHj1cYFvKEiXVGWtPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njh2MkK4JO69VQ>? NV;s[|E1W0GQR1XS
NOS-1 cell Ml7TS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXnTXm5bUW6qaXLpeIlwdiCxZjDoeY1idiCQT2OtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQTR5Nk[g{txO NIrrWXVUSU6JRWK=
SW780 cell NUjWZVFOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHfhZZpKdmirYnn0bY9vKG:oIHj1cYFvKFOZN{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU46Pjl2OTFOwG0> MknqV2FPT0WU
KYSE-180 cell NVzBSW1lT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M17G[GlvcGmkaYTpc44hd2ZiaIXtZY4hU1mVRT2xPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njl5NkW0JO69VQ>? MnPaV2FPT0WU
MDA-MB-361 cell MonCS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUDJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2zOlEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njl6NkS3JO69VQ>? NY\jfVlvW0GQR1XS
SNU-C2B cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWXJcohq[mm2aX;uJI9nKGi3bXHuJHNPXS2FMlKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlAyOTN6IN88US=> MYXTRW5ITVJ?
NCI-H661 cell NI\CSVJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlvwTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSE[2NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvODZ7NDFOwG0> NIrBSXBUSU6JRWK=
OE33 cell NI\ROYlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXXJcohq[mm2aX;uJI9nKGi3bXHuJG9GOzNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD14LkG0N|g6KM7:TR?= NGDDdXhUSU6JRWK=
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COLO-792 cell M4rOVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHr2VmtKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tO|kzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Pi5{NUKxPUDPxE1? MUHTRW5ITVJ?
HEL cell M3;sRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{[0[2lvcGmkaYTpc44hd2ZiaIXtZY4hUEWOIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Nj6yOlc3KM7:TR?= MVvTRW5ITVJ?
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COR-L23 cell NHfPVppIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{W0cWlvcGmkaYTpc44hd2ZiaIXtZY4hS0:ULVyyN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvPDN|NE[g{txO Ml\nV2FPT0WU
NCI-H2452 cell NHHSWlBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGftfG5KdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlQ2OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTZwNUKyPFEh|ryP NYXVSVRpW0GQR1XS
BB65-RCC cell NEi1NGtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWPzcFFxUW6qaXLpeIlwdiCxZjDoeY1idiCEQk[1MXJESyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTZwNkS1PUDPxE1? NG\pdo1USU6JRWK=
CAL-33 cell NYjhWlk2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUDJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC1|MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[uOlU3PjVizszN NYnI[oRvW0GQR1XS

... 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)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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:

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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 SDS / 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 )

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

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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