JNJ-26854165 (Serdemetan)

Name: JNJ-26854165 (Serdemetan)
Brand: Selleck Chemicals
SKU: S1172
Rating: 5 (8 reviews)

For research use only.

Catalog No.S1172

8 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.

Selleck's JNJ-26854165 (Serdemetan) has been cited by 8 publications

Cell, 2019, 36(2):179-193

PubMed: 28162770 ( click the link to review the publication )

Cancer Cell, 2019, 36(2):179-193

PubMed: 31378681 ( click the link to review the publication )

Circulation, 2020, 10.1161/CIRCULATIONAHA.120.048191

PubMed: 32755395 ( click the link to review the publication )

BMC Pharmacol Toxicol, 2017, 18(1):40

PubMed: 28577368 ( click the link to review the publication )

Sci Signal, 2016, 9(448):ra98

PubMed: 27703031 ( click the link to review the publication )

Mol Ther, 2015, 23(5):857-65

PubMed: 25648263 ( click the link to review the publication )

Sci Rep, 2014, 4:4664

PubMed: 24722541 ( click the link to review the publication )

Head Neck, 2014, 10.1002/hed.23822

PubMed: 24986420 ( click the link to review the publication )

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

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	Activity Description	PMID
KU-19-19 cell	NEC2O\|ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MXTJcohq[mm2aX;uJI9nKGi3bXHuJGtWNTF7LUG5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE46OzJ\|NjFOwG0>	M332SHNCVkeHUh?=
H4 cell	MlnDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MlTzTY5pcWKrdHnvckBw\iCqdX3hckBJPCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTFwME[3NFch\|ryP	M1ewZ3NCVkeHUh?=
KGN cell	M1\WOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	MmnCTY5pcWKrdHnvckBw\iCqdX3hckBMT05iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLk[yNFUh\|ryP	MkPtV2FPT0WU
786-0 cell	NHLZTlVIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MVfJcohq[mm2aX;uJI9nKGi3bXHuJFc5Pi1yIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MT63Nlk5QSEQvF2=	MlXXV2FPT0WU
769-P cell	NFnYWGdIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MYTJcohq[mm2aX;uJI9nKGi3bXHuJFc3QS2SIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MT64NlIzPCEQvF2=	MkfOV2FPT0WU
K5 cell	NWnOcmJxT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MWLJcohq[mm2aX;uJI9nKGi3bXHuJGs2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi5yMU[yOEDPxE1?	M4e2bXNCVkeHUh?=
MLMA cell	Ml:5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NX;ycW46UW6qaXLpeIlwdiCxZjDoeY1idiCNT2PDMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjB\|MkG3JO69VQ>?	M3PaWHNCVkeHUh?=
MLMA cell	NYjHXGZMT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NXPFVWVHUW6qaXLpeIlwdiCxZjDoeY1idiCPTF3BJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4zQDdyMzFOwG0>	M2HwTnNCVkeHUh?=
EW-7 cell	NIPYVo5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NWq0[FBXUW6qaXLpeIlwdiCxZjDoeY1idiCHVz23JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4{OjZ7NTFOwG0>	Mn\QV2FPT0WU
SW1088 cell	MnrUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M1PtV2lvcGmkaYTpc44hd2ZiaIXtZY4hW1dzMEi4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk45ODZ3MTFOwG0>	NXjaO4E6W0GQR1XS
MC-IXC cell	M17KRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NEflZ4ZKdmirYnn0bY9vKG:oIHj1cYFvKE2FLVnYR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQDd5OUKg{txO	NWHxNIRYW0GQR1XS
NCI-H2052 cell	NVHFe5d6T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M1;GN2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFUzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy5yOEG1O{DPxE1?	MX3TRW5ITVJ?
IGR-1 cell	NXrheIs6T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NXXRUXBNUW6qaXLpeIlwdiCxZjDoeY1idiCLR2KtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvOTJyMkig{txO	MYLTRW5ITVJ?
DSH1 cell	MorPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M4S3SmlvcGmkaYTpc44hd2ZiaIXtZY4hTFOKMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUOuNlQzQTZizszN	MUPTRW5ITVJ?
PA-1 cell	MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NE\DRXdKdmirYnn0bY9vKG:oIHj1cYFvKFCDLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlMxODV7zszN	MoDxV2FPT0WU
SK-MEL-3 cell	M4PzPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	M4TQUGlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjNzMkC3JO69VQ>?	NULXSocxW0GQR1XS
SW900 cell	NX\QdJJtT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M3nyUmlvcGmkaYTpc44hd2ZiaIXtZY4hW1d7MECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlQ5OjV3IN88US=>	NUT1TYFrW0GQR1XS
CAKI-1 cell	M2r0d2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7	MUDJcohq[mm2aX;uJI9nKGi3bXHuJGNCU0lvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUOuOVI4OzhizszN	NIPYO5NUSU6JRWK=
ES1 cell	NGD3enpIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NVvMOIY5UW6qaXLpeIlwdiCxZjDoeY1idiCHU{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlUzQDl5IN88US=>	MkPRV2FPT0WU
SK-N-DZ cell	MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MUjJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU5vRGqgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlYzPTl3IN88US=>	NXe4WoZyW0GQR1XS
RH-1 cell	NHzoNopIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NYexeZU{UW6qaXLpeIlwdiCxZjDoeY1idiCUSD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{43QDR4MzFOwG0>	NInaeGJUSU6JRWK=
ES8 cell	MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M1zrcWlvcGmkaYTpc44hd2ZiaIXtZY4hTVN6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;Mz62PVcxOiEQvF2=	M1LYTHNCVkeHUh?=
NEC8 cell	M1H6O2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7	M3zh[2lvcGmkaYTpc44hd2ZiaIXtZY4hVkWFODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUOuO\|Y6QDJizszN	MXnTRW5ITVJ?
LNCaP-Clone-FGC cell	MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NEL2fGpKdmirYnn0bY9vKG:oIHj1cYFvKEyQQ3HQMWNtd26nLV\HR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQDN3M{[g{txO	NFrYfYNUSU6JRWK=
HCE-4 cell	MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NWPnfIp2UW6qaXLpeIlwdiCxZjDoeY1idiCKQ1WtOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQThyNzFOwG0>	M1LlNXNCVkeHUh?=
U-118-MG cell	NWq2eoQ5T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MnnmTY5pcWKrdHnvckBw\iCqdX3hckBWNTFzOD3NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvODFyNk[g{txO	M1vheHNCVkeHUh?=
GI-ME-N cell	NHf3cHBIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MXfJcohq[mm2aX;uJI9nKGi3bXHuJGdKNU2HLV6gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlA5Pzl4IN88US=>	Ml;RV2FPT0WU
LB1047-RCC cell	MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M3vnR2lvcGmkaYTpc44hd2ZiaIXtZY4hVEJzMES3MXJESyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTRwMU[xOFMh\|ryP	NITwbFFUSU6JRWK=
HT-1080 cell	M4qxT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NH3OUlRKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUGwPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjF7OUKxJO69VQ>?	NGHpb5JUSU6JRWK=
NB69 cell	M3G2cWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	Mm\2TY5pcWKrdHnvckBw\iCqdX3hckBPSjZ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;ND6zOVA1PyEQvF2=	M37kNXNCVkeHUh?=
NCI-H1693 cell	NWG4W41WT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MUHJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMU[5N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvPDR6OUWg{txO	M3XoU3NCVkeHUh?=
HSC-3 cell	NVHjS3Z[T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NWC1Om1OUW6qaXLpeIlwdiCxZjDoeY1idiCKU1OtN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvPDl7M{Og{txO	NH;Y[lJUSU6JRWK=
MDA-MB-231 cell	Mn;qS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MnLGTY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtNlMyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC53NUi5PUDPxE1?	MWLTRW5ITVJ?
HOS cell	MlXyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M{\DWmlvcGmkaYTpc44hd2ZiaIXtZY4hUE:VIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;ND63PFY{KM7:TR?=	MmjsV2FPT0WU
BT-549 cell	M{D3Omdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	M{e3RWlvcGmkaYTpc44hd2ZiaIXtZY4hSlRvNUS5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE44QDh5IN88US=>	NUnwVXB3W0GQR1XS
NB17 cell	NWfPTY5MT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NWnuPYdQUW6qaXLpeIlwdiCxZjDoeY1idiCQQkG3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE44QDl5NjFOwG0>	NULRR2h2W0GQR1XS
5637 cell	MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NEOxU5dKdmirYnn0bY9vKG:oIHj1cYFvKDV4M{egZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlc6PjV{IN88US=>	MX;TRW5ITVJ?
OVCAR-8 cell	MknmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MmnSTY5pcWKrdHnvckBw\iCqdX3hckBQXkODUj24JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE46OjR\|NjFOwG0>	NInTT3FUSU6JRWK=
G-402 cell	Mnm0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MUPJcohq[mm2aX;uJI9nKGi3bXHuJGcuPDB{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;ND65N\|A{PSEQvF2=	MVnTRW5ITVJ?
BB30-HNC cell	M3zXVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	Moj6TY5pcWKrdHnvckBw\iCqdX3hckBDSjNyLVjOR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvODd{MUig{txO	M4rHPHNCVkeHUh?=
HCC1806 cell	MkX6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NFXZToFKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{G4NFYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjB6M{O5JO69VQ>?	NHPzWnRUSU6JRWK=
COLO-800 cell	M4TvXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NXHDd4EzUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVgxOCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTVwMUK2OEDPxE1?	NVvKOFFmW0GQR1XS
FADU cell	MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NIGxcIhKdmirYnn0bY9vKG:oIHj1cYFvKE[DRGWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlM3PTV5IN88US=>	NHnSb25USU6JRWK=
NCI-H1651 cell	M2PlU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7	MVHJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMU[1NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvOzl2MEmg{txO	NGTiNoVUSU6JRWK=
AGS cell	MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MoHtTY5pcWKrdHnvckBw\iCqdX3hckBCT1NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkS3O\|EyKM7:TR?=	NX;rNo57W0GQR1XS
CHP-212 cell	Mmi4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NGrRfpZKdmirYnn0bY9vKG:oIHj1cYFvKEOKUD2yNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjN7NEC5JO69VQ>?	M1\XcHNCVkeHUh?=
YAPC cell	NX71[ZNOT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NWf3XoZ[UW6qaXLpeIlwdiCxZjDoeY1idiC\QWDDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU41PzdzMTFOwG0>	NXHYOVJbW0GQR1XS
GOTO cell	M3jmUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NFrjTmNKdmirYnn0bY9vKG:oIHj1cYFvKEeRVF:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlQ6PTd4IN88US=>	Mm\nV2FPT0WU
KYSE-510 cell	M2rQV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7	M1G2ZWlvcGmkaYTpc44hd2ZiaIXtZY4hU1mVRT21NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjVzMTFOwG0>	NVTMfJlJW0GQR1XS
NCI-H2342 cell	NEHEfo9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NVuwZ\|FsUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI{PDJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkWzNlc5KM7:TR?=	NF3TRphUSU6JRWK=
BFTC-905 cell	MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MXrJcohq[mm2aX;uJI9nKGi3bXHuJGJHXENvOUC1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU43Ojh\|NTFOwG0>	NED5RVBUSU6JRWK=
EW-16 cell	M{Pobmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NGT3e3hKdmirYnn0bY9vKG:oIHj1cYFvKEWZLUG2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU44OjB7MzFOwG0>	NGHUNo5USU6JRWK=
SK-MEL-30 cell	NEDUZmlIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NYLMPGJYUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOzBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13Lke0OVQ{KM7:TR?=	MV\TRW5ITVJ?
HLE cell	MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M3HkUmlvcGmkaYTpc44hd2ZiaIXtZY4hUEyHIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;NT63O\|Q5QSEQvF2=	MVzTRW5ITVJ?
T98G cell	MnvJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MVHJcohq[mm2aX;uJI9nKGi3bXHuJHQ6QEdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13Lke5OlM2KM7:TR?=	NHribmtUSU6JRWK=
HUTU-80 cell	MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NFXxZnNKdmirYnn0bY9vKG:oIHj1cYFvKEiXVGWtPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njh2MkK4JO69VQ>?	MUfTRW5ITVJ?
NOS-1 cell	MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M1TtS2lvcGmkaYTpc44hd2ZiaIXtZY4hVk:VLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlk1PzZ4IN88US=>	NYfo[HllW0GQR1XS
SW780 cell	NWfLenh1T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M3KyWWlvcGmkaYTpc44hd2ZiaIXtZY4hW1d5OECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlk3QTR7IN88US=>	M2LEXnNCVkeHUh?=
KYSE-180 cell	NFPHW5hIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MWLJcohq[mm2aX;uJI9nKGi3bXHuJGt[W0VvMUiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU46PzZ3NDFOwG0>	MY\TRW5ITVJ?
MDA-MB-361 cell	M4PGTWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NXjmVlFMUW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuOzZzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;NT65PFY1PyEQvF2=	NVPxcYw{W0GQR1XS
SNU-C2B cell	NVXnc3AzT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NHTiUHlKdmirYnn0bY9vKG:oIHj1cYFvKFOQVT3DNmIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjBzMUO4JO69VQ>?	MUXTRW5ITVJ?
NCI-H661 cell	NGXFZohIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	M4PQVGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi2OlEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjB4OUSg{txO	MkTFV2FPT0WU
OE33 cell	NV75bGR3T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NF61RYZKdmirYnn0bY9vKG:oIHj1cYFvKE:HM{OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlE1Ozh7IN88US=>	NV;nT5Y2W0GQR1XS
TYK-nu cell	NVnKcXJrT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NHfqdJlKdmirYnn0bY9vKG:oIHj1cYFvKFS\Sz3ueUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvOjF6NkOg{txO	NIiyfIlUSU6JRWK=
COLO-792 cell	MorMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MX;Jcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vN{myJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok4zPTJzOTFOwG0>	M2jZOXNCVkeHUh?=
HEL cell	MkHSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MWnJcohq[mm2aX;uJI9nKGi3bXHuJGhGVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTZwMk[3OkDPxE1?	MoSzV2FPT0WU
D-566MG cell	NYjLVHdVT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NV3IU2dxUW6qaXLpeIlwdiCxZjDoeY1idiCGLUW2Om1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Pi5\|M{S5NUDPxE1?	NHLsOnRUSU6JRWK=
U031 cell	MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NWXFO25TUW6qaXLpeIlwdiCxZjDoeY1idiCXMEOxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok41OThzNjFOwG0>	NX;Ic3hIW0GQR1XS
COR-L23 cell	MnvkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MWLJcohq[mm2aX;uJI9nKGi3bXHuJGNQWi2OMkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlQ{OzR4IN88US=>	M2L3PHNCVkeHUh?=
NCI-H2452 cell	MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MmLDTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEK0OVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjV{MkixJO69VQ>?	NEHBWJJUSU6JRWK=
BB65-RCC cell	NVTYZpo4T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MU\Jcohq[mm2aX;uJI9nKGi3bXHuJGJDPjVvUlPDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok43PDV7IN88US=>	NIf5O5JUSU6JRWK=
CAL-33 cell	M3rRdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	Mni5TY5pcWKrdHnvckBw\iCqdX3hckBESUxvM{OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlY2PjZ3IN88US=>	M4eySHNCVkeHUh?=

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p53 / HDM2 / HDMX / p21 / Noxa / Puma ; PubMed: 20736344 Mol Cancer Ther 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 J Pharmacol Exp Ther U266 and JeKo-1 cells were treated with JNJ-26854165 and cells harvested at the indicated time points. MDM2 / p-MDM2 / p53 ; PubMed: 27999193 Oncotarget 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 Oncotarget 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 J Pharmacol Exp Ther 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 Oncotarget 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]

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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]

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Animal Models: CB17SC scid^-/- female mice.
Dosages: ≤20 mg/kg
Administration: Administered via p.o.
(Only for Reference)

References

[4] Smith MA, et al. Pediatr Blood Cancer, 2012, 59(2), 329-332.

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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 Download JNJ-26854165 (Serdemetan) SDF

Molecular Weight	328.41
Formula	C₂₁H₂₀N₄
CAS No.	881202-45-5
Storage	3 years-20°C powder 2 years-80°C 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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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

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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 DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，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.

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Molarity Calculator

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

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The Serial Dilution Calculator Equation

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Computed Result

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Molecular Weight Calculator

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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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