Serdemetan (JNJ-26854165)

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。

Serdemetan (JNJ-26854165) Chemical Structure

Serdemetan (JNJ-26854165) Chemical Structure

CAS: 881202-45-5

规格 价格 库存 购买数量
5mg RMB 903.65 现货
25mg RMB 3012.66 现货
100mg RMB 7931.79 现货
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客户使用Selleck的Serdemetan (JNJ-26854165)发表文献13

客户使用该产品的6个实验数据

产品质控

批次: S117202 DMSO] 66 mg/mL] false] Ethanol] 2 mg/mL] false] Water] Insoluble] false 纯度: 99.58%
99.58

Serdemetan (JNJ-26854165)相关产品

相关信号通路图

p53抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
KU-19-19 cell Growth inhibition assay Inhibition of human KU-19-19 cell growth in a cell viability assay, IC50=0.93236 μM SANGER
H4 cell Growth inhibition assay Inhibition of human H4 cell growth in a cell viability assay, IC50=1.06707 μM SANGER
KGN cell Growth inhibition assay Inhibition of human KGN cell growth in a cell viability assay, IC50=1.6205 μM SANGER
786-0 cell Growth inhibition assay Inhibition of human 786-0 cell growth in a cell viability assay, IC50=1.72989 μM SANGER
769-P cell Growth inhibition assay Inhibition of human 769-P cell growth in a cell viability assay, IC50=1.82224 μM SANGER
K5 cell Growth inhibition assay Inhibition of human K5 cell growth in a cell viability assay, IC50=2.01624 μM SANGER
MLMA cell Growth inhibition assay Inhibition of human KOSC-2 cell growth in a cell viability assay, IC50=2.03217 μM SANGER
MLMA cell Growth inhibition assay Inhibition of human MLMA cell growth in a cell viability assay, IC50=2.28703 μM SANGER
EW-7 cell Growth inhibition assay Inhibition of human EW-7 cell growth in a cell viability assay, IC50=2.32695 μM SANGER
SW1088 cell Growth inhibition assay Inhibition of human SW1088 cell growth in a cell viability assay, IC50=2.80651 μM SANGER
MC-IXC cell Growth inhibition assay Inhibition of human MC-IXC cell growth in a cell viability assay, IC50=2.87792 μM SANGER
NCI-H2052 cell Growth inhibition assay Inhibition of human NCI-H2052 cell growth in a cell viability assay, IC50=3.08157 μM SANGER
IGR-1 cell Growth inhibition assay Inhibition of human IGR-1 cell growth in a cell viability assay, IC50=3.12028 μM SANGER
DSH1 cell Growth inhibition assay Inhibition of human DSH1 cell growth in a cell viability assay, IC50=3.24296 μM SANGER
PA-1 cell Growth inhibition assay Inhibition of human PA-1 cell growth in a cell viability assay, IC50=3.30059μM SANGER
SK-MEL-3 cell Growth inhibition assay Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=3.31207 μM SANGER
SW900 cell Growth inhibition assay Inhibition of human SW900 cell growth in a cell viability assay, IC50=3.48255 μM SANGER
CAKI-1 cell Growth inhibition assay Inhibition of human CAKI-1 cell growth in a cell viability assay, IC50=3.52738 μM SANGER
ES1 cell Growth inhibition assay Inhibition of human ES1 cell growth in a cell viability assay, IC50=3.52897 μM SANGER
SK-N-DZ cell Growth inhibition assay Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50=3.62595 μM SANGER
RH-1 cell Growth inhibition assay Inhibition of human RH-1 cell growth in a cell viability assay, IC50=3.68463 μM SANGER
ES8 cell Growth inhibition assay Inhibition of human ES8 cell growth in a cell viability assay, IC50=3.69702 μM SANGER
NEC8 cell Growth inhibition assay Inhibition of human NEC8 cell growth in a cell viability assay, IC50=3.76982 μM SANGER
LNCaP-Clone-FGC cell Growth inhibition assay Inhibition of human LNCaP-Clone-FGC cell growth in a cell viability assay, IC50=3.83536 μM SANGER
HCE-4 cell Growth inhibition assay Inhibition of human HCE-4 cell growth in a cell viability assay, IC50=3.9807 μM SANGER
U-118-MG cell Growth inhibition assay Inhibition of human U-118-MG cell growth in a cell viability assay, IC50=4.01066 μM SANGER
GI-ME-N cell Growth inhibition assay Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50=4.08796 μM SANGER
LB1047-RCC cell Growth inhibition assay Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=4.16143 μM SANGER
HT-1080 cell Growth inhibition assay Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=4.19921 μM SANGER
NB69 cell Growth inhibition assay Inhibition of human NB69 cell growth in a cell viability assay, IC50=4.35047 μM SANGER
NCI-H1693 cell Growth inhibition assay Inhibition of human NCI-H1693 cell growth in a cell viability assay, IC50=4.44895 μM SANGER
HSC-3 cell Growth inhibition assay Inhibition of human HSC-3 cell growth in a cell viability assay, IC50=4.49933 μM SANGER
MDA-MB-231 cell Growth inhibition assay Inhibition of human MDA-MB-231 cell growth in a cell viability assay, IC50=4.55899 μM SANGER
HOS cell Growth inhibition assay Inhibition of human HOS cell growth in a cell viability assay, IC50=4.7863 μM SANGER
BT-549 cell Growth inhibition assay Inhibition of human BT-549 cell growth in a cell viability assay, IC50=4.7887 μM SANGER
NB17 cell Growth inhibition assay Inhibition of human NB17 cell growth in a cell viability assay, IC50=4.78976 μM SANGER
5637 cell Growth inhibition assay Inhibition of human 5637 cell growth in a cell viability assay, IC50=4.79652 μM SANGER
OVCAR-8 cell Growth inhibition assay Inhibition of human OVCAR-8 cell growth in a cell viability assay, IC50=4.92436 μM SANGER
G-402 cell Growth inhibition assay Inhibition of human G-402 cell growth in a cell viability assay, IC50=4.93035 μM SANGER
BB30-HNC cell Growth inhibition assay Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=5.07218 μM SANGER
HCC1806 cell Growth inhibition assay Inhibition of human HCC1806 cell growth in a cell viability assay, IC50=5.08339 μM SANGER
COLO-800 cell Growth inhibition assay Inhibition of human COLO-800 cell growth in a cell viability assay, IC50=5.1264 μM SANGER
FADU cell Growth inhibition assay Inhibition of human FADU cell growth in a cell viability assay, IC50=5.36557 μM SANGER
NCI-H1651 cell Growth inhibition assay Inhibition of human NCI-H1651 cell growth in a cell viability assay, IC50=5.39409 μM SANGER
AGS cell Growth inhibition assay Inhibition of human AGS cell growth in a cell viability assay, IC50=5.47711 μM SANGER
CHP-212 cell Growth inhibition assay Inhibition of human CHP-212 cell growth in a cell viability assay, IC50=5.39409 μM SANGER
YAPC cell Growth inhibition assay Inhibition of human YAPC cell growth in a cell viability assay, IC50=5.47711 μM SANGER
GOTO cell Growth inhibition assay Inhibition of human GOTO cell growth in a cell viability assay, IC50=5.49576 μM SANGER
KYSE-510 cell Growth inhibition assay Inhibition of human KYSE-510 cell growth in a cell viability assay, IC50=5.511 μM SANGER
NCI-H2342 cell Growth inhibition assay Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=5.53278 μM SANGER
BFTC-905 cell Growth inhibition assay Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=5.62835 μM SANGER
EW-16 cell Growth inhibition assay Inhibition of human EW-16 cell growth in a cell viability assay, IC50=5.72093 μM SANGER
SK-MEL-30 cell Growth inhibition assay Inhibition of human SK-MEL-30 cell growth in a cell viability assay, IC50=5.74543 μM SANGER
HLE cell Growth inhibition assay Inhibition of human HLE cell growth in a cell viability assay, IC50=5.77489 μM SANGER
T98G cell Growth inhibition assay Inhibition of human T98G cell growth in a cell viability assay, IC50=5.79635 μM SANGER
HUTU-80 cell Growth inhibition assay Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=5.84228 μM SANGER
NOS-1 cell Growth inhibition assay Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=5.94766 μM SANGER
SW780 cell Growth inhibition assay Inhibition of human SW780 cell growth in a cell viability assay, IC50=5.96949 μM SANGER
KYSE-180 cell Growth inhibition assay Inhibition of human KYSE-180 cell growth in a cell viability assay, IC50=5.97654 μM SANGER
MDA-MB-361 cell Growth inhibition assay Inhibition of human MDA-MB-361 cell growth in a cell viability assay, IC50=5.98647 μM SANGER
SNU-C2B cell Growth inhibition assay Inhibition of human SNU-C2B cell growth in a cell viability assay, IC50=6.01138 μM SANGER
NCI-H661 cell Growth inhibition assay Inhibition of human NCI-H661 cell growth in a cell viability assay, IC50=6.0694 μM SANGER
OE33 cell Growth inhibition assay Inhibition of human OE33 cell growth in a cell viability assay, IC50=6.14389 μM SANGER
TYK-nu cell Growth inhibition assay Inhibition of human TYK-nu cell growth in a cell viability assay, IC50=6.21863 μM SANGER
COLO-792 cell Growth inhibition assay Inhibition of human COLO-792 cell growth in a cell viability assay, IC50=6.25219 μM SANGER
HEL cell Growth inhibition assay Inhibition of human HEL cell growth in a cell viability assay, IC50=6.2676 μM SANGER
D-566MG cell Growth inhibition assay Inhibition of human D-566MG cell growth in a cell viability assay, IC50=6.33491 μM SANGER
U031 cell Growth inhibition assay Inhibition of human U031 cell growth in a cell viability assay, IC50=6.41816 μM SANGER
COR-L23 cell Growth inhibition assay Inhibition of human COR-L23 cell growth in a cell viability assay, IC50=6.43346 μM SANGER
NCI-H2452 cell Growth inhibition assay Inhibition of human NCI-H2452 cell growth in a cell viability assay, IC50=6.52281 μM SANGER
BB65-RCC cell Growth inhibition assay Inhibition of human BB65-RCC cell growth in a cell viability assay, IC50=6.6459 μM SANGER
CAL-33 cell Growth inhibition assay Inhibition of human CAL-33 cell growth in a cell viability assay, IC50=6.65665 μM SANGER
点击查看更多细胞系数据

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(In Vitro)
体外研究活性 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]
细胞实验 细胞系 OCI-AML-3,MOLM-13,NB4和U937细胞
浓度 0到10 μM
孵育时间 72 小时
方法 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。
实验图片 检测方法 检测指标 实验图片 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
Growth inhibition assay Cell viability 23820125
Immunofluorescence p53 27999193
体内研究(In Vivo)
体内研究活性 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]
动物实验 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00676910 Completed
Neoplasms
Johnson & Johnson Pharmaceutical Research & Development L.L.C.
November 2006 Phase 1

化学信息&溶解度

分子量 328.41 分子式

C21H20N4

CAS号 881202-45-5 SDF Download Serdemetan (JNJ-26854165) SDF
Smiles C1=CC=C2C(=C1)C(=CN2)CCNC3=CC=C(C=C3)NC4=CC=NC=C4
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 66 mg/mL ( 200.96 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 2 mg/mL

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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