Serdemetan (JNJ-26854165)

Catalog No.S1172

For research use only.

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.

Serdemetan (JNJ-26854165) Chemical Structure

CAS No. 881202-45-5

Selleck's Serdemetan (JNJ-26854165) has been cited by 13 publications

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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 Mom5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MU\Jcohq[mm2aX;uJI9nKGi3bXHuJGtWNTF7LUG5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE46OzJ|NjFOwG0> MmfvV2FPT0WU
H4 cell NFnubpNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYHJcohq[mm2aX;uJI9nKGi3bXHuJGg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5yNkewO{DPxE1? NYrQW5o5W0GQR1XS
KGN cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFvrTGhKdmirYnn0bY9vKG:oIHj1cYFvKEuJTjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOlIxPSEQvF2= MnvIV2FPT0WU
786-0 cell M{H4XWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3\1PWlvcGmkaYTpc44hd2ZiaIXtZY4hPzh4LUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlczQTh7IN88US=> MnXPV2FPT0WU
769-P cell NIHJcJBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2LIdWlvcGmkaYTpc44hd2ZiaIXtZY4hPzZ7LWCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlgzOjJ2IN88US=> NFWzbVlUSU6JRWK=
K5 cell NFi5SZRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MljETY5pcWKrdHnvckBw\iCqdX3hckBMPSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwMEG2NlQh|ryP MmfyV2FPT0WU
MLMA cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWLJcohq[mm2aX;uJI9nKGi3bXHuJGtQW0NvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuNFMzOTdizszN NWP4U|E2W0GQR1XS
MLMA cell MoXkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2rIcmlvcGmkaYTpc44hd2ZiaIXtZY4hVUyPQTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuNlg4ODNizszN MlfQV2FPT0WU
EW-7 cell NHvZOmNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUHzbXI2UW6qaXLpeIlwdiCxZjDoeY1idiCHVz23JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4{OjZ7NTFOwG0> M3TKUnNCVkeHUh?=
SW1088 cell Ml76S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFLzcIZKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUC4PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQDB4NUGg{txO MlvvV2FPT0WU
MC-IXC cell NVG0dFZvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1qxR2lvcGmkaYTpc44hd2ZiaIXtZY4hVUNvSWjDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk45Pzd7MjFOwG0> NYLJcIZDW0GQR1XS
NCI-H2052 cell NX7hU5VRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmrqTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKwOVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjB6MUW3JO69VQ>? NHfSd3RUSU6JRWK=
IGR-1 cell NYTvNYZLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYDJcohq[mm2aX;uJI9nKGi3bXHuJGlIWi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz6xNlAzQCEQvF2= M2f1TXNCVkeHUh?=
DSH1 cell Mli5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3jETmlvcGmkaYTpc44hd2ZiaIXtZY4hTFOKMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuNlQzQTZizszN MkP3V2FPT0WU
PA-1 cell MmGzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2HjVGlvcGmkaYTpc44hd2ZiaIXtZY4hWEFvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuN|AxPToQvF2= NELTXHpUSU6JRWK=
SK-MEL-3 cell NV\4cHF{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlztTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvOzF{MEeg{txO NVrlS49UW0GQR1XS
SW900 cell Mn3yS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NELPNHVKdmirYnn0bY9vKG:oIHj1cYFvKFOZOUCwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{41QDJ3NTFOwG0> NV3hd3psW0GQR1XS
CAKI-1 cell NGDFb3hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1rm[2lvcGmkaYTpc44hd2ZiaIXtZY4hS0GNST2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{42Ojd|ODFOwG0> MXrTRW5ITVJ?
ES1 cell MknGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUTJcohq[mm2aX;uJI9nKGi3bXHuJGVUOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNwNUK4PVch|ryP M4r2fHNCVkeHUh?=
SK-N-DZ cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkniTY5pcWKrdHnvckBw\iCqdX3hckBUUy2QLVTaJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{43OjV7NTFOwG0> MkG0V2FPT0WU
RH-1 cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUHKU2JrUW6qaXLpeIlwdiCxZjDoeY1idiCUSD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{43QDR4MzFOwG0> NIPUOFBUSU6JRWK=
ES8 cell NIKzO3JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2n5VWlvcGmkaYTpc44hd2ZiaIXtZY4hTVN6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz62PVcxOiEQvF2= NWDBSnNiW0GQR1XS
NEC8 cell M3HMVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIO2NIJKdmirYnn0bY9vKG:oIHj1cYFvKE6HQ{igZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlc3QTh{IN88US=> MXXTRW5ITVJ?
LNCaP-Clone-FGC cell M{DwT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkK5TY5pcWKrdHnvckBw\iCqdX3hckBNVkOjUD3DcI9v\S2IR1OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlg{PTN4IN88US=> M3i1dXNCVkeHUh?=
HCE-4 cell NHm4WmpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWnrTG1wUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1WtOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQThyNzFOwG0> Mlu2V2FPT0WU
U-118-MG cell NF7JenVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkHlTY5pcWKrdHnvckBw\iCqdX3hckBWNTFzOD3NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvODFyNk[g{txO MnKwV2FPT0WU
GI-ME-N cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF3XVG9KdmirYnn0bY9vKG:oIHj1cYFvKEeLLV3FMW4h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjB6N{m2JO69VQ>? MWLTRW5ITVJ?
LB1047-RCC cell NE\HS2tIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnTvTY5pcWKrdHnvckBw\iCqdX3hckBNSjFyNEetVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5zNkG0N{DPxE1? MUXTRW5ITVJ?
HT-1080 cell MmHES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkXnTY5pcWKrdHnvckBw\iCqdX3hckBJXC1zMEiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4yQTl{MTFOwG0> MVPTRW5ITVJ?
NB69 cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml;hTY5pcWKrdHnvckBw\iCqdX3hckBPSjZ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND6zOVA1PyEQvF2= NEDEd5dUSU6JRWK=
NCI-H1693 cell NXLxPJlLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4TkNGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOlk{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC52NEi5OUDPxE1? NXfSfVVtW0GQR1XS
HSC-3 cell M2jyU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIHt[XNKdmirYnn0bY9vKG:oIHj1cYFvKEiVQz2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE41QTl|MzFOwG0> NWTmNVJwW0GQR1XS
MDA-MB-231 cell MmXtS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXrJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2yN|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjV3OEm5JO69VQ>? Mnf1V2FPT0WU
HOS cell MlrUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4H4[GlvcGmkaYTpc44hd2ZiaIXtZY4hUE:VIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND63PFY{KM7:TR?= NHvjeGdUSU6JRWK=
BT-549 cell M2HMfGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{naXGlvcGmkaYTpc44hd2ZiaIXtZY4hSlRvNUS5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE44QDh5IN88US=> M3zzW3NCVkeHUh?=
NB17 cell MnT3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXz2UYpkUW6qaXLpeIlwdiCxZjDoeY1idiCQQkG3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE44QDl5NjFOwG0> NH6wZYpUSU6JRWK=
5637 cell NH;QOIlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEDmO4FKdmirYnn0bY9vKG:oIHj1cYFvKDV4M{egZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlc6PjV{IN88US=> NGDBZphUSU6JRWK=
OVCAR-8 cell MkfFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2DHNmlvcGmkaYTpc44hd2ZiaIXtZY4hV1[FQWKtPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQTJ2M{[g{txO M1TVSXNCVkeHUh?=
G-402 cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWLkVllNUW6qaXLpeIlwdiCxZjDoeY1idiCJLUSwNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQTNyM{Wg{txO NH3MSVFUSU6JRWK=
BB30-HNC cell M33yVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXfJcohq[mm2aX;uJI9nKGi3bXHuJGJDOzBvSF7DJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4xPzJzODFOwG0> NWjrU49tW0GQR1XS
HCC1806 cell NFjpNYtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M13ORmlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMUiwOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvODh|M{mg{txO M37OWHNCVkeHUh?=
COLO-800 cell MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGHT[2FKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tPFAxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS5zMk[0JO69VQ>? M1KwO3NCVkeHUh?=
FADU cell NWr3dVVoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3nmT2lvcGmkaYTpc44hd2ZiaIXtZY4hTkGGVTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuN|Y2PTdizszN M{jC[XNCVkeHUh?=
NCI-H1651 cell NIXn[nJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NV7TXZpkUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE3PTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkO5OFA6KM7:TR?= NUWzZpN[W0GQR1XS
AGS cell NUfKbXF6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlLHTY5pcWKrdHnvckBw\iCqdX3hckBCT1NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkS3O|EyKM7:TR?= MXzTRW5ITVJ?
CHP-212 cell M{PKS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4jiVGlvcGmkaYTpc44hd2ZiaIXtZY4hS0iSLUKxNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvOzl2MEmg{txO M3n1c3NCVkeHUh?=
YAPC cell NVPGUFNjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVjJcohq[mm2aX;uJI9nKGi3bXHuJHlCWENiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkS3O|EyKM7:TR?= MWjTRW5ITVJ?
GOTO cell NYCwb3FRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn7CTY5pcWKrdHnvckBw\iCqdX3hckBIV1SRIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT60PVU4PiEQvF2= MnO5V2FPT0WU
KYSE-510 cell NF7FNVdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkPITY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUWxNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPTFzIN88US=> MX;TRW5ITVJ?
NCI-H2342 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2PlTmlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyN|QzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS53M{K3PEDPxE1? NGK5T4RUSU6JRWK=
BFTC-905 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFnHOZRKdmirYnn0bY9vKG:oIHj1cYFvKEKIVFOtPVA2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS54MkizOUDPxE1? Ml:2V2FPT0WU
EW-16 cell M3W1PGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVnJcohq[mm2aX;uJI9nKGi3bXHuJGVYNTF4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT63NlA6OyEQvF2= M13tc3NCVkeHUh?=
SK-MEL-30 cell M2\qbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYHJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2zNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPzR3NEOg{txO MW\TRW5ITVJ?
HLE cell MlP0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFf2dGFKdmirYnn0bY9vKG:oIHj1cYFvKEiORTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuO|c1QDlizszN MnvnV2FPT0WU
T98G cell M1\vT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NI[0OZJKdmirYnn0bY9vKG:oIHj1cYFvKFR7OFegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlc6PjN3IN88US=> NELTeGdUSU6JRWK=
HUTU-80 cell NH\u[GdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2XiVmlvcGmkaYTpc44hd2ZiaIXtZY4hUFWWVT24NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQDR{Mkig{txO MVPTRW5ITVJ?
NOS-1 cell MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYHtOmo5UW6qaXLpeIlwdiCxZjDoeY1idiCQT2OtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQTR5Nk[g{txO MlSxV2FPT0WU
SW780 cell M3\FeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWXJcohq[mm2aX;uJI9nKGi3bXHuJHNYPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT65Olk1QSEQvF2= MUPTRW5ITVJ?
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BB65-RCC cell M1WxcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHLjdHpKdmirYnn0bY9vKG:oIHj1cYFvKEKENkWtVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Pi54NEW5JO69VQ>? NWHJOYNjW0GQR1XS
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Assay
Methods Test Index PMID
Western blot Bcr-abl / p-Bcr-abl / p-CrkL / STAT5 / p-STAT5 / STAT3 / p-STAT3 ; MDM2 / p-MDM2 / p53 ; ABCA1 / ABCG1 / NPC1 / NPC2 / HMGcoR ; p53 / HDM2 / HDMX / p21 / Noxa / Puma 27999193 23820125 20736344
Growth inhibition assay Cell viability 23820125
Immunofluorescence p53 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 (from reference)

Cell Research:[1]
  • 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
Animal Research:[4]
  • Animal Models: CB17SC scid-/- female mice.
  • Dosages: ≤20 mg/kg
  • Administration: Administered via p.o.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 328.41
Formula

C21H20N4

CAS No. 881202-45-5
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

(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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