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 12 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 NYK0W|hlT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlWwTY5pcWKrdHnvckBw\iCqdX3hckBMXS1zOT2xPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvQTN{M{[g{txO MUDTRW5ITVJ?
H4 cell NV7lVJdQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYnJdIJ2UW6qaXLpeIlwdiCxZjDoeY1idiCKNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNFY4ODdizszN M3yxZXNCVkeHUh?=
KGN cell NIPGb21Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYPLd4w4UW6qaXLpeIlwdiCxZjDoeY1idiCNR16gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlYzODVizszN NUjaU5pkW0GQR1XS
786-0 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGXaZYNKdmirYnn0bY9vKG:oIHj1cYFvKDd6Nj2wJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU44Ojl6OTFOwG0> NXT2V|F1W0GQR1XS
769-P cell NYq4bnI2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVj3T5pxUW6qaXLpeIlwdiCxZjDoeY1idiB5NkmtVEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvQDJ{MkSg{txO NI\4cGJUSU6JRWK=
K5 cell M3jBXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV\CZ5RsUW6qaXLpeIlwdiCxZjDoeY1idiCNNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuNFE3OjRizszN M2HJenNCVkeHUh?=
MLMA cell M1LJVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX\pfHVvUW6qaXLpeIlwdiCxZjDoeY1idiCNT2PDMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjB|MkG3JO69VQ>? M1zHOHNCVkeHUh?=
MLMA cell MnPRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4X2U2lvcGmkaYTpc44hd2ZiaIXtZY4hVUyPQTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuNlg4ODNizszN MnHQV2FPT0WU
EW-7 cell M3\sSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIrJToRKdmirYnn0bY9vKG:oIHj1cYFvKEWZLUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlMzPjl3IN88US=> M1;DXXNCVkeHUh?=
SW1088 cell MmDuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXTJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTB6ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuPFA3PTFizszN M4[3TnNCVkeHUh?=
MC-IXC cell M3vUdmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH72cplKdmirYnn0bY9vKG:oIHj1cYFvKE2FLVnYR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQDd5OUKg{txO M4DvbXNCVkeHUh?=
NCI-H2052 cell Mk\wS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVG5VlAxUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIxPTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkC4NVU4KM7:TR?= M{jLeXNCVkeHUh?=
IGR-1 cell NGnUfHVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnXuTY5pcWKrdHnvckBw\iCqdX3hckBKT1JvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuNVIxOjhizszN NH;LdmRUSU6JRWK=
DSH1 cell MnzSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmTnTY5pcWKrdHnvckBw\iCqdX3hckBFW0hzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz6yOFI6PiEQvF2= M4jLXnNCVkeHUh?=
PA-1 cell MkfrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3TvXGlvcGmkaYTpc44hd2ZiaIXtZY4hWEFvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuN|AxPToQvF2= NVfLVFNtW0GQR1XS
SK-MEL-3 cell Mm\qS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWfJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4{OTJyNzFOwG0> NVXSdG92W0GQR1XS
SW900 cell NV6xfmV2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlvqTY5pcWKrdHnvckBw\iCqdX3hckBUXzlyMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuOFgzPTVizszN NVfncXAyW0GQR1XS
CAKI-1 cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{G5[2lvcGmkaYTpc44hd2ZiaIXtZY4hS0GNST2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{42Ojd|ODFOwG0> NUnBXZQyW0GQR1XS
ES1 cell M{\TNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF;jNI1KdmirYnn0bY9vKG:oIHj1cYFvKEWVMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuOVI5QTdizszN MWPTRW5ITVJ?
SK-N-DZ cell M{L2cmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnTnTY5pcWKrdHnvckBw\iCqdX3hckBUUy2QLVTaJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{43OjV7NTFOwG0> NFvyW5NUSU6JRWK=
RH-1 cell NHOyUmxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MojoTY5pcWKrdHnvckBw\iCqdX3hckBTUC1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz62PFQ3OyEQvF2= M4HMR3NCVkeHUh?=
ES8 cell M2DqTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4jwZ2lvcGmkaYTpc44hd2ZiaIXtZY4hTVN6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz62PVcxOiEQvF2= MWXTRW5ITVJ?
NEC8 cell MkPhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFPoe4pKdmirYnn0bY9vKG:oIHj1cYFvKE6HQ{igZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlc3QTh{IN88US=> NXW2T3lrW0GQR1XS
LNCaP-Clone-FGC cell M1TlfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MknCTY5pcWKrdHnvckBw\iCqdX3hckBNVkOjUD3DcI9v\S2IR1OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlg{PTN4IN88US=> MmjMV2FPT0WU
HCE-4 cell MmrVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXLjd|czUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1WtOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQThyNzFOwG0> MYjTRW5ITVJ?
U-118-MG cell NFXJT2pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHTK[ZBKdmirYnn0bY9vKG:oIHj1cYFvKFVvMUG4MW1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5yMUC2OkDPxE1? MUjTRW5ITVJ?
GI-ME-N cell NUCzPFd{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2HIeGlvcGmkaYTpc44hd2ZiaIXtZY4hT0lvTVWtUkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvODh5OU[g{txO NGGwR|FUSU6JRWK=
LB1047-RCC cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWjZSHpZUW6qaXLpeIlwdiCxZjDoeY1idiCOQkGwOFcuWkOFIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND6xOlE1OyEQvF2= MYPTRW5ITVJ?
HT-1080 cell NVz6WFY{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVrJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTFyOECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlE6QTJzIN88US=> MXHTRW5ITVJ?
NB69 cell NX;Nb4tOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmC5TY5pcWKrdHnvckBw\iCqdX3hckBPSjZ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND6zOVA1PyEQvF2= MnizV2FPT0WU
NCI-H1693 cell NFXtSWNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4XNXWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOlk{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC52NEi5OUDPxE1? NH3aWW5USU6JRWK=
HSC-3 cell NXKxboh2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYPJcohq[mm2aX;uJI9nKGi3bXHuJGhUSy1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND60PVk{OyEQvF2= MmG3V2FPT0WU
MDA-MB-231 cell M4jUN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4DvNmlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVI{OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwNUW4PVkh|ryP MVnTRW5ITVJ?
HOS cell M3:5R2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmjFTY5pcWKrdHnvckBw\iCqdX3hckBJV1NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12Lke4OlMh|ryP NYfMUnBNW0GQR1XS
BT-549 cell M{DJfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX7Jcohq[mm2aX;uJI9nKGi3bXHuJGJVNTV2OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuO|g5PyEQvF2= Mn7yV2FPT0WU
NB17 cell NXu1SYc2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYPTcFNVUW6qaXLpeIlwdiCxZjDoeY1idiCQQkG3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE44QDl5NjFOwG0> M2PQSHNCVkeHUh?=
5637 cell MoDtS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3i4[GlvcGmkaYTpc44hd2ZiaIXtZY4hPTZ|NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuO|k3PTJizszN M4fTR3NCVkeHUh?=
OVCAR-8 cell MYHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{DyRmlvcGmkaYTpc44hd2ZiaIXtZY4hV1[FQWKtPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQTJ2M{[g{txO NFKyU|hUSU6JRWK=
G-402 cell NG\BcWlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXPJcohq[mm2aX;uJI9nKGi3bXHuJGcuPDB{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND65N|A{PSEQvF2= Mkf4V2FPT0WU
BB30-HNC cell NH73bWpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYnkVHltUW6qaXLpeIlwdiCxZjDoeY1idiCEQkOwMWhPSyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwMEeyNVgh|ryP M33VOnNCVkeHUh?=
HCC1806 cell Mn;rS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFX6XZFKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{G4NFYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjB6M{O5JO69VQ>? M1HufHNCVkeHUh?=
COLO-800 cell NGHQb|VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVPJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vOECwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4yOjZ2IN88US=> NEHiboxUSU6JRWK=
FADU cell M3jCT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH\IN2lKdmirYnn0bY9vKG:oIHj1cYFvKE[DRGWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlM3PTV5IN88US=> NEX1cXpUSU6JRWK=
NCI-H1651 cell MkO3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1;jVmlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOlUyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS5|OUSwPUDPxE1? NFHLWINUSU6JRWK=
AGS cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWnUNnJ3UW6qaXLpeIlwdiCxZjDoeY1idiCDR2OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlQ4PzFzIN88US=> MX\TRW5ITVJ?
CHP-212 cell MmjpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV\XbHNrUW6qaXLpeIlwdiCxZjDoeY1idiCFSGCtNlEzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS5|OUSwPUDPxE1? M{G1bXNCVkeHUh?=
YAPC cell NWnHRYkxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NG\VenhKdmirYnn0bY9vKG:oIHj1cYFvKFmDUFOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlQ4PzFzIN88US=> M1vmS3NCVkeHUh?=
GOTO cell NIjyR2dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnzlTY5pcWKrdHnvckBw\iCqdX3hckBIV1SRIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT60PVU4PiEQvF2= M3G0XHNCVkeHUh?=
KYSE-510 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXfJcohq[mm2aX;uJI9nKGi3bXHuJGt[W0VvNUGwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU42OTFizszN MlzoV2FPT0WU
NCI-H2342 cell NGnLcodIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmHnTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKzOFIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjV|Mke4JO69VQ>? NUjTVZdyW0GQR1XS
BFTC-905 cell MoHUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYLJcohq[mm2aX;uJI9nKGi3bXHuJGJHXENvOUC1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU43Ojh|NTFOwG0> NETIWpNUSU6JRWK=
EW-16 cell M17ZbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4ewN2lvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlczODl|IN88US=> M1H0[3NCVkeHUh?=
SK-MEL-30 cell MlLmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUnPW|RzUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOzBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13Lke0OVQ{KM7:TR?= MkjIV2FPT0WU
HLE cell NGLKUIRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFrhU4tKdmirYnn0bY9vKG:oIHj1cYFvKEiORTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuO|c1QDlizszN Mo\MV2FPT0WU
T98G cell Moj5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF23SItKdmirYnn0bY9vKG:oIHj1cYFvKFR7OFegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlc6PjN3IN88US=> MWTTRW5ITVJ?
HUTU-80 cell NEL1boRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3HQb2lvcGmkaYTpc44hd2ZiaIXtZY4hUFWWVT24NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQDR{Mkig{txO NUDiUmR[W0GQR1XS
NOS-1 cell M3f3WWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3fOVmlvcGmkaYTpc44hd2ZiaIXtZY4hVk:VLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlk1PzZ4IN88US=> M1TOTnNCVkeHUh?=
SW780 cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkTWTY5pcWKrdHnvckBw\iCqdX3hckBUXzd6MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuPVY6PDlizszN NELBOJdUSU6JRWK=
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CAL-33 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVG5W2hZUW6qaXLpeIlwdiCxZjDoeY1idiCFQVytN|Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjZ3Nk[1JO69VQ>? MUjTRW5ITVJ?
Assay
Methods Test Index PMID
Western blot p53 / HDM2 / HDMX / p21 / Noxa / Puma ; ABCA1 / ABCG1 / NPC1 / NPC2 / HMGcoR ; MDM2 / p-MDM2 / p53 ; Bcr-abl / p-Bcr-abl / p-CrkL / STAT5 / p-STAT5 / STAT3 / p-STAT3 20736344 23820125 27999193
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
  • (Only for Reference)
Animal Research:[4]
  • 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 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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