Serdemetan (JNJ-26854165)

For research use only. Not for use in humans.

目录号:S1172

Serdemetan (JNJ-26854165) Chemical Structure

CAS No. 881202-45-5

Serdemetan (JNJ-26854165)是一种HDM2泛素连接酶拮抗剂,作用于p53野生型细胞,诱导早期凋亡,在缺乏功能性p53的细胞中,抑制细胞增殖而延迟细胞凋亡。

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RMB 903.65 现货
RMB 3012.66 现货
RMB 7931.79 现货
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客户使用Selleck生产的Serdemetan (JNJ-26854165)发表文献12篇:

客户使用该产品的6个实验数据:

  • 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.

产品安全说明书

p53抑制剂选择性比较

生物活性

产品描述 Serdemetan (JNJ-26854165)是一种HDM2泛素连接酶拮抗剂,作用于p53野生型细胞,诱导早期凋亡,在缺乏功能性p53的细胞中,抑制细胞增殖而延迟细胞凋亡。
特性 JNJ 26854165是口服生物有效性的,小分子HDM2拮抗剂,具有有效的抗肿瘤活性。
靶点
p53 [1]
(Cell-free assay)
HDM2 [1]
(Cell-free assay)
Mdm2 [2]
(Cell-free assay)
体外研究

JNJ-26854165是新型激活p53的色胺衍生物,作为HDM2泛素连接酶拮抗剂。JNJ-26854165作用于白血病细胞系,抑制细胞生长,且诱导凋亡,作用于OCI-AML-3, MOLM-13,NALM-6和REH细胞72小时后,IC50值分别为0.24,0.33,0.32和0.44 µM。此外, JNJ-26854165作用于p53突变的细胞,加速蛋白酶调节的p21降解和抗p53对p21的转录诱导, 诱导S期延迟,且上调E2F1表达, 导致S期细胞优先凋亡。[1] JNJ-26854165是口服MDM2抑制剂,可以抑制MDM2-p53复合体与蛋白酶的相互作用,且通过与MDM2的RING域结合提高p53水平。[2]最新研究显示JNJ-26854165作用于四种人类癌细胞系:H460,A549,p53-WT-HCT116,和p53-null-HCT116,抑制无性繁殖生存。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KU-19-19 cell NX;oW3c6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEjvemVKdmirYnn0bY9vKG:oIHj1cYFvKEuXLUG5MVE6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC57M{KzOkDPxE1? NX\Zd29nW0GQR1XS
H4 cell M4jwcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoPXTY5pcWKrdHnvckBw\iCqdX3hckBJPCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwME[3NFch|ryP M2rkO3NCVkeHUh?=
KGN cell NXPoSGE5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUm3cmF4UW6qaXLpeIlwdiCxZjDoeY1idiCNR16gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlYzODVizszN MWPTRW5ITVJ?
786-0 cell NWm2U3VrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3vLPWlvcGmkaYTpc44hd2ZiaIXtZY4hPzh4LUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlczQTh7IN88US=> MVTTRW5ITVJ?
769-P cell NI\GV5JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2[2[2lvcGmkaYTpc44hd2ZiaIXtZY4hPzZ7LWCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlgzOjJ2IN88US=> MXHTRW5ITVJ?
K5 cell NVHTV49KT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXzJcohq[mm2aX;uJI9nKGi3bXHuJGs2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi5yMU[yOEDPxE1? NF7kWGtUSU6JRWK=
MLMA cell MmLkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHzUWGpKdmirYnn0bY9vKG:oIHj1cYFvKEuRU1OtNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvODN{MUeg{txO MVHTRW5ITVJ?
MLMA cell NGjPfoRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlPqTY5pcWKrdHnvckBw\iCqdX3hckBOVE2DIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj6yPFcxOyEQvF2= MlO4V2FPT0WU
EW-7 cell Mk\vS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVPtSoZuUW6qaXLpeIlwdiCxZjDoeY1idiCHVz23JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4{OjZ7NTFOwG0> MoDBV2FPT0WU
SW1088 cell NVfTcldRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVHoWVcxUW6qaXLpeIlwdiCxZjDoeY1idiCVV{GwPFgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjhyNkWxJO69VQ>? M{nK[XNCVkeHUh?=
MC-IXC cell NXr2NVN3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4nmUmlvcGmkaYTpc44hd2ZiaIXtZY4hVUNvSWjDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk45Pzd7MjFOwG0> NUfKR|FkW0GQR1XS
NCI-H2052 cell NV3aNpN6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml25TY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKwOVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjB6MUW3JO69VQ>? NGDVZohUSU6JRWK=
IGR-1 cell MlPNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXPYbpFmUW6qaXLpeIlwdiCxZjDoeY1idiCLR2KtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvOTJyMkig{txO M4HrPHNCVkeHUh?=
DSH1 cell NXzSephxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX3GPYtNUW6qaXLpeIlwdiCxZjDoeY1idiCGU1ixJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4zPDJ7NjFOwG0> NX3CW41iW0GQR1XS
PA-1 cell M{LJcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXXJcohq[mm2aX;uJI9nKGi3bXHuJHBCNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkOwNFU6|ryP Mmq3V2FPT0WU
SK-MEL-3 cell NYnwVYJtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX2zUZI3UW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNwM{GyNFch|ryP M1i1enNCVkeHUh?=
SW900 cell M1qwS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MknDTY5pcWKrdHnvckBw\iCqdX3hckBUXzlyMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuOFgzPTVizszN MWLTRW5ITVJ?
CAKI-1 cell MnLyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3TXW2lvcGmkaYTpc44hd2ZiaIXtZY4hS0GNST2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{42Ojd|ODFOwG0> M1e1PXNCVkeHUh?=
ES1 cell M1;zWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NED0eWVKdmirYnn0bY9vKG:oIHj1cYFvKEWVMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuOVI5QTdizszN M3PnTHNCVkeHUh?=
SK-N-DZ cell Mo\SS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3u2XWlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTj3EXkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvPjJ3OUWg{txO MWXTRW5ITVJ?
RH-1 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYnJcohq[mm2aX;uJI9nKGi3bXHuJHJJNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Lk[4OFY{KM7:TR?= MoW4V2FPT0WU
ES8 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUDQd3MxUW6qaXLpeIlwdiCxZjDoeY1idiCHU{igZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlY6PzB{IN88US=> Ml;CV2FPT0WU
NEC8 cell NGPUWXhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUjJcohq[mm2aX;uJI9nKGi3bXHuJG5GSzhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Lke2PVgzKM7:TR?= NGXFfWhUSU6JRWK=
LNCaP-Clone-FGC cell MlPzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2X5SGlvcGmkaYTpc44hd2ZiaIXtZY4hVE6FYWCtR4xwdmVvRlfDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{45OzV|NjFOwG0> NGrkZpFUSU6JRWK=
HCE-4 cell NHzxVGNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoiyTY5pcWKrdHnvckBw\iCqdX3hckBJS0VvNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPVgxPyEQvF2= MnvPV2FPT0WU
U-118-MG cell Mn7QS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXyybY44UW6qaXLpeIlwdiCxZjDoeY1idiCXLUGxPE1OTyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwMEGwOlYh|ryP MlHmV2FPT0WU
GI-ME-N cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYnJcohq[mm2aX;uJI9nKGi3bXHuJGdKNU2HLV6gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlA5Pzl4IN88US=> MV\TRW5ITVJ?
LB1047-RCC cell MorxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlfSTY5pcWKrdHnvckBw\iCqdX3hckBNSjFyNEetVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5zNkG0N{DPxE1? NEDIPWxUSU6JRWK=
HT-1080 cell MkXyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnOwTY5pcWKrdHnvckBw\iCqdX3hckBJXC1zMEiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4yQTl{MTFOwG0> MVjTRW5ITVJ?
NB69 cell NH;IbllIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYLGfGp6UW6qaXLpeIlwdiCxZjDoeY1idiCQQk[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4{PTB2NzFOwG0> MnPKV2FPT0WU
NCI-H1693 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVXFe3NiUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE3QTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkS0PFk2KM7:TR?= MYjTRW5ITVJ?
HSC-3 cell NYDafpRtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVvJcohq[mm2aX;uJI9nKGi3bXHuJGhUSy1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND60PVk{OyEQvF2= MnLvV2FPT0WU
MDA-MB-231 cell MmT5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkfMTY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtNlMyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC53NUi5PUDPxE1? NELKemZUSU6JRWK=
HOS cell NF;PSFVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXLoR41rUW6qaXLpeIlwdiCxZjDoeY1idiCKT2OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlc5PjNizszN Mm\NV2FPT0WU
BT-549 cell NVPa[pd[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH;RflBKdmirYnn0bY9vKG:oIHj1cYFvKEKWLUW0PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvPzh6NzFOwG0> NVLSS2k3W0GQR1XS
NB17 cell MoHHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkDhTY5pcWKrdHnvckBw\iCqdX3hckBPSjF5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND63PFk4PiEQvF2= M{\kZXNCVkeHUh?=
5637 cell MoPrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIH0R3JKdmirYnn0bY9vKG:oIHj1cYFvKDV4M{egZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlc6PjV{IN88US=> NGK4WYlUSU6JRWK=
OVCAR-8 cell MkDES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2XO[GlvcGmkaYTpc44hd2ZiaIXtZY4hV1[FQWKtPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQTJ2M{[g{txO NIjLcXBUSU6JRWK=
G-402 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGeyV2ZKdmirYnn0bY9vKG:oIHj1cYFvKEdvNECyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE46OzB|NTFOwG0> MmjtV2FPT0WU
BB30-HNC cell MnzNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{fie2lvcGmkaYTpc44hd2ZiaIXtZY4hSkJ|MD3IUmMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjB5MkG4JO69VQ>? NF\G[IxUSU6JRWK=
HCC1806 cell MkHiS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3XXfmlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMUiwOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvODh|M{mg{txO MlTDV2FPT0WU
COLO-800 cell M3\6bWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGL6XXlKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tPFAxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS5zMk[0JO69VQ>? MXfTRW5ITVJ?
FADU cell MoTPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVnHTHlsUW6qaXLpeIlwdiCxZjDoeY1idiCIQVTVJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4{PjV3NzFOwG0> MYTTRW5ITVJ?
NCI-H1651 cell NGGxSXVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIXhUZNKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVY2OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwM{m0NFkh|ryP NF;lZnBUSU6JRWK=
AGS cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF7vW4VKdmirYnn0bY9vKG:oIHj1cYFvKEGJUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuOFc4OTFizszN Mo[2V2FPT0WU
CHP-212 cell MlLFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1TGVWlvcGmkaYTpc44hd2ZiaIXtZY4hS0iSLUKxNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvOzl2MEmg{txO MVnTRW5ITVJ?
YAPC cell MoH1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWrJcohq[mm2aX;uJI9nKGi3bXHuJHlCWENiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkS3O|EyKM7:TR?= NHn2[3NUSU6JRWK=
GOTO cell M3LjeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVjmbVMxUW6qaXLpeIlwdiCxZjDoeY1idiCJT2TPJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU41QTV5NjFOwG0> NEDqOIRUSU6JRWK=
KYSE-510 cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmnrTY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUWxNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPTFzIN88US=> NHT0eIFUSU6JRWK=
NCI-H2342 cell MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVf4[HlZUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI{PDJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkWzNlc5KM7:TR?= NFHUPWFUSU6JRWK=
BFTC-905 cell MmDoS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGJHXENvOUC1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU43Ojh|NTFOwG0> MX3TRW5ITVJ?
EW-16 cell M4[0Umdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3vMSGlvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlczODl|IN88US=> NEm3cGFUSU6JRWK=
SK-MEL-30 cell NGnxOI1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYPJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2zNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPzR3NEOg{txO NXvJRYVGW0GQR1XS
HLE cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MknZTY5pcWKrdHnvckBw\iCqdX3hckBJVEViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13Lke3OFg6KM7:TR?= MmXTV2FPT0WU
T98G cell MlW0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NELDeodKdmirYnn0bY9vKG:oIHj1cYFvKFR7OFegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlc6PjN3IN88US=> MkHuV2FPT0WU
HUTU-80 cell M1P2XGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX7LfFFIUW6qaXLpeIlwdiCxZjDoeY1idiCKVWTVMVgxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS56NEKyPEDPxE1? Mmf3V2FPT0WU
NOS-1 cell NYjEdGZyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVvJcohq[mm2aX;uJI9nKGi3bXHuJG5QWy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT65OFc3PiEQvF2= MYHTRW5ITVJ?
SW780 cell NXe3bGRVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUmwcng{UW6qaXLpeIlwdiCxZjDoeY1idiCVV{e4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQTZ7NEmg{txO MmK0V2FPT0WU
KYSE-180 cell M3jIT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUjJcohq[mm2aX;uJI9nKGi3bXHuJGt[W0VvMUiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU46PzZ3NDFOwG0> MUnTRW5ITVJ?
MDA-MB-361 cell NUTDSJpPT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mon5TY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtN|YyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS57OE[0O{DPxE1? M162SXNCVkeHUh?=
SNU-C2B cell MlXhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoTWTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvQ{LCJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok4xOTF|ODFOwG0> M4PtOHNCVkeHUh?=
NCI-H661 cell MlTaS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIr5c21KdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IOlYyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Pi5yNkm0JO69VQ>? NF\4elZUSU6JRWK=
OE33 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVjJcohq[mm2aX;uJI9nKGi3bXHuJG9GOzNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD14LkG0N|g6KM7:TR?= NV7jTopuW0GQR1XS
TYK-nu cell M{jsS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2rNb2lvcGmkaYTpc44hd2ZiaIXtZY4hXFmNLX71JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok4zOTh4MzFOwG0> M4XSdXNCVkeHUh?=
COLO-792 cell NW\URW91T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2LnR2lvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz23PVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjJ3MkG5JO69VQ>? MX7TRW5ITVJ?
HEL cell NGnN[opIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1jOdGlvcGmkaYTpc44hd2ZiaIXtZY4hUEWOIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Nj6yOlc3KM7:TR?= MVXTRW5ITVJ?
D-566MG cell NH2zc3JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYLFdIFkUW6qaXLpeIlwdiCxZjDoeY1idiCGLUW2Om1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Pi5|M{S5NUDPxE1? M1T5[3NCVkeHUh?=
U031 cell M2\qV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYe3R3lPUW6qaXLpeIlwdiCxZjDoeY1idiCXMEOxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok41OThzNjFOwG0> NEDGcGFUSU6JRWK=
COR-L23 cell NIPZVoFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH:yNZpKdmirYnn0bY9vKG:oIHj1cYFvKEORUj3MNlMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjR|M{S2JO69VQ>? NHnnbXJUSU6JRWK=
NCI-H2452 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3nnOmlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyOFUzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Pi53MkK4NUDPxE1? NX7EVnBWW0GQR1XS
BB65-RCC cell NFThdZJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXzifWkxUW6qaXLpeIlwdiCxZjDoeY1idiCEQk[1MXJESyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTZwNkS1PUDPxE1? NFrUe3hUSU6JRWK=
CAL-33 cell NX;lZ|VkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mk\hTY5pcWKrdHnvckBw\iCqdX3hckBESUxvM{OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlY2PjZ3IN88US=> NF7Kb2tUSU6JRWK=

... 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
体内研究 JNJ-26854165按20 mg/kg剂量口服饲喂于三十六分之十七(47%)实体移植瘤和七分之五(71%) ALL移植瘤,持续5天,重复进行6周,导致EFS分布出现明显区别。[4]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[1]
- 合并
  • Cell lines: OCI-AML-3,MOLM-13,NB4和U937细胞
  • Concentrations: 0到10 μM
  • Incubation Time: 72 小时
  • Method: 细胞系维持在含10%热灭活胎牛血清(FCS)的RPMI 1640培养基上。急性骨髓性白血病(AML) 患者体内得到的OCI-AML-3, MOLM-13, NB4和 U937 细胞,慢性髓细胞性白血病(CML)患者体内得到的K562细胞,急性成淋巴细胞性白血病(ALL)患者体内得到的NALM-6, REH, P12-ICHIKAWA和PF-382细胞。OCI-AML-3, MOLM-13, NALM-6和 REH 细胞具有野生型p53, 然而NB4,U937,K562,P12-ICHIKAWA和PF-382细胞具有突变型p53,获得对数生长期细胞系,接种,用JNJ-26854165处理。白血病患者体内获得的白血病细胞中获得肝素外周血或骨髓样本。通过密度梯度离心纯化单核细胞,非黏着细胞悬浮在含10%FCS的RPMI 1640培养基上。正常骨髓衍生的干细胞接种在含MEM-α培养基的12孔板上,24小时后,加入AML细胞。为了研究骨髓干细胞作用于原代白血病细胞的效果,培养AML 细胞。在JNJ-26854165和 AraC的联合实验中,用0,2,5或 10 μM。JNJ-26854165 处理AML细胞系。在OCI-AML-3细胞中 JNJ-26854165与 AraC的浓度比为1:1,在其他细胞中为10:1。两种试剂同时加到细胞中,培养48小时。JNJ-26854165和Doxorubicin联用的实验中,两种试剂同时加到细胞中,培养48小时。用 0, 25, 50或 100 nM Doxorubicin处理细胞 (用0,100,200 或400 nM Doxorubicin 处理OCI-AML-3细胞和原代白血病细胞),Doxorubicin 与JNJ-26854165 的浓度比为1:10 (在OCI-AML-3细胞和原代白血病细胞中比为1:25)。通过台酚蓝染料重复计数,测评细胞活力。
    (Only for Reference)
动物实验:[4]
- 合并
  • Animal Models: 皮下注射kidney/rhabdoid肿瘤,肉瘤, 成神经细胞瘤, 和非恶性胶质瘤脑癌的雌性CB17SC scid-/-小鼠,携带神经胶质瘤的BALB/c nu/nu小鼠
  • Dosages: ≤20 mg/kg
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 66 mg/mL (200.96 mM)
Water Insoluble
Ethanol '2 mg/mL
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
1% DMSO+30% polyethylene glycol+1% Tween 80
30 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 328.41
化学式

C21H20N4

CAS号 881202-45-5
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

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

技术支持

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操作手册

如果有其他问题,请给我们留言。

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p53 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID