Serdemetan (JNJ-26854165)

目录号：S1172 Purity: 99.58%

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

CAS: 881202-45-5

规格	价格	库存
5mg	903.65	现货
25mg	3012.66	现货
100mg	7931.79	现货
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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

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细胞实验数据示例

细胞系	实验类型	活性描述
KU-19-19 cell	Growth inhibition assay	Inhibition of human KU-19-19 cell growth in a cell viability assay, IC50=0.93236 μM
H4 cell	Growth inhibition assay	Inhibition of human H4 cell growth in a cell viability assay, IC50=1.06707 μM
KGN cell	Growth inhibition assay	Inhibition of human KGN cell growth in a cell viability assay, IC50=1.6205 μM
786-0 cell	Growth inhibition assay	Inhibition of human 786-0 cell growth in a cell viability assay, IC50=1.72989 μM
769-P cell	Growth inhibition assay	Inhibition of human 769-P cell growth in a cell viability assay, IC50=1.82224 μM
K5 cell	Growth inhibition assay	Inhibition of human K5 cell growth in a cell viability assay, IC50=2.01624 μM
MLMA cell	Growth inhibition assay	Inhibition of human KOSC-2 cell growth in a cell viability assay, IC50=2.03217 μM
MLMA cell	Growth inhibition assay	Inhibition of human MLMA cell growth in a cell viability assay, IC50=2.28703 μM
EW-7 cell	Growth inhibition assay	Inhibition of human EW-7 cell growth in a cell viability assay, IC50=2.32695 μM
SW1088 cell	Growth inhibition assay	Inhibition of human SW1088 cell growth in a cell viability assay, IC50=2.80651 μM
MC-IXC cell	Growth inhibition assay	Inhibition of human MC-IXC cell growth in a cell viability assay, IC50=2.87792 μM
NCI-H2052 cell	Growth inhibition assay	Inhibition of human NCI-H2052 cell growth in a cell viability assay, IC50=3.08157 μM
IGR-1 cell	Growth inhibition assay	Inhibition of human IGR-1 cell growth in a cell viability assay, IC50=3.12028 μM
DSH1 cell	Growth inhibition assay	Inhibition of human DSH1 cell growth in a cell viability assay, IC50=3.24296 μM
PA-1 cell	Growth inhibition assay	Inhibition of human PA-1 cell growth in a cell viability assay, IC50=3.30059μM
SK-MEL-3 cell	Growth inhibition assay	Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=3.31207 μM
SW900 cell	Growth inhibition assay	Inhibition of human SW900 cell growth in a cell viability assay, IC50=3.48255 μM
CAKI-1 cell	Growth inhibition assay	Inhibition of human CAKI-1 cell growth in a cell viability assay, IC50=3.52738 μM
ES1 cell	Growth inhibition assay	Inhibition of human ES1 cell growth in a cell viability assay, IC50=3.52897 μM
SK-N-DZ cell	Growth inhibition assay	Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50=3.62595 μM
RH-1 cell	Growth inhibition assay	Inhibition of human RH-1 cell growth in a cell viability assay, IC50=3.68463 μM
ES8 cell	Growth inhibition assay	Inhibition of human ES8 cell growth in a cell viability assay, IC50=3.69702 μM
NEC8 cell	Growth inhibition assay	Inhibition of human NEC8 cell growth in a cell viability assay, IC50=3.76982 μM
LNCaP-Clone-FGC cell	Growth inhibition assay	Inhibition of human LNCaP-Clone-FGC cell growth in a cell viability assay, IC50=3.83536 μM
HCE-4 cell	Growth inhibition assay	Inhibition of human HCE-4 cell growth in a cell viability assay, IC50=3.9807 μM
U-118-MG cell	Growth inhibition assay	Inhibition of human U-118-MG cell growth in a cell viability assay, IC50=4.01066 μM
GI-ME-N cell	Growth inhibition assay	Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50=4.08796 μM
LB1047-RCC cell	Growth inhibition assay	Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=4.16143 μM
HT-1080 cell	Growth inhibition assay	Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=4.19921 μM
NB69 cell	Growth inhibition assay	Inhibition of human NB69 cell growth in a cell viability assay, IC50=4.35047 μM
NCI-H1693 cell	Growth inhibition assay	Inhibition of human NCI-H1693 cell growth in a cell viability assay, IC50=4.44895 μM
HSC-3 cell	Growth inhibition assay	Inhibition of human HSC-3 cell growth in a cell viability assay, IC50=4.49933 μM
MDA-MB-231 cell	Growth inhibition assay	Inhibition of human MDA-MB-231 cell growth in a cell viability assay, IC50=4.55899 μM
HOS cell	Growth inhibition assay	Inhibition of human HOS cell growth in a cell viability assay, IC50=4.7863 μM
BT-549 cell	Growth inhibition assay	Inhibition of human BT-549 cell growth in a cell viability assay, IC50=4.7887 μM
NB17 cell	Growth inhibition assay	Inhibition of human NB17 cell growth in a cell viability assay, IC50=4.78976 μM
5637 cell	Growth inhibition assay	Inhibition of human 5637 cell growth in a cell viability assay, IC50=4.79652 μM
OVCAR-8 cell	Growth inhibition assay	Inhibition of human OVCAR-8 cell growth in a cell viability assay, IC50=4.92436 μM
G-402 cell	Growth inhibition assay	Inhibition of human G-402 cell growth in a cell viability assay, IC50=4.93035 μM
BB30-HNC cell	Growth inhibition assay	Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=5.07218 μM
HCC1806 cell	Growth inhibition assay	Inhibition of human HCC1806 cell growth in a cell viability assay, IC50=5.08339 μM
COLO-800 cell	Growth inhibition assay	Inhibition of human COLO-800 cell growth in a cell viability assay, IC50=5.1264 μM
FADU cell	Growth inhibition assay	Inhibition of human FADU cell growth in a cell viability assay, IC50=5.36557 μM
NCI-H1651 cell	Growth inhibition assay	Inhibition of human NCI-H1651 cell growth in a cell viability assay, IC50=5.39409 μM
AGS cell	Growth inhibition assay	Inhibition of human AGS cell growth in a cell viability assay, IC50=5.47711 μM
CHP-212 cell	Growth inhibition assay	Inhibition of human CHP-212 cell growth in a cell viability assay, IC50=5.39409 μM
YAPC cell	Growth inhibition assay	Inhibition of human YAPC cell growth in a cell viability assay, IC50=5.47711 μM
GOTO cell	Growth inhibition assay	Inhibition of human GOTO cell growth in a cell viability assay, IC50=5.49576 μM
KYSE-510 cell	Growth inhibition assay	Inhibition of human KYSE-510 cell growth in a cell viability assay, IC50=5.511 μM
NCI-H2342 cell	Growth inhibition assay	Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=5.53278 μM
BFTC-905 cell	Growth inhibition assay	Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=5.62835 μM
EW-16 cell	Growth inhibition assay	Inhibition of human EW-16 cell growth in a cell viability assay, IC50=5.72093 μM
SK-MEL-30 cell	Growth inhibition assay	Inhibition of human SK-MEL-30 cell growth in a cell viability assay, IC50=5.74543 μM
HLE cell	Growth inhibition assay	Inhibition of human HLE cell growth in a cell viability assay, IC50=5.77489 μM
T98G cell	Growth inhibition assay	Inhibition of human T98G cell growth in a cell viability assay, IC50=5.79635 μM
HUTU-80 cell	Growth inhibition assay	Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=5.84228 μM
NOS-1 cell	Growth inhibition assay	Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=5.94766 μM
SW780 cell	Growth inhibition assay	Inhibition of human SW780 cell growth in a cell viability assay, IC50=5.96949 μM
KYSE-180 cell	Growth inhibition assay	Inhibition of human KYSE-180 cell growth in a cell viability assay, IC50=5.97654 μM
MDA-MB-361 cell	Growth inhibition assay	Inhibition of human MDA-MB-361 cell growth in a cell viability assay, IC50=5.98647 μM
SNU-C2B cell	Growth inhibition assay	Inhibition of human SNU-C2B cell growth in a cell viability assay, IC50=6.01138 μM
NCI-H661 cell	Growth inhibition assay	Inhibition of human NCI-H661 cell growth in a cell viability assay, IC50=6.0694 μM
OE33 cell	Growth inhibition assay	Inhibition of human OE33 cell growth in a cell viability assay, IC50=6.14389 μM
TYK-nu cell	Growth inhibition assay	Inhibition of human TYK-nu cell growth in a cell viability assay, IC50=6.21863 μM
COLO-792 cell	Growth inhibition assay	Inhibition of human COLO-792 cell growth in a cell viability assay, IC50=6.25219 μM
HEL cell	Growth inhibition assay	Inhibition of human HEL cell growth in a cell viability assay, IC50=6.2676 μM
D-566MG cell	Growth inhibition assay	Inhibition of human D-566MG cell growth in a cell viability assay, IC50=6.33491 μM
U031 cell	Growth inhibition assay	Inhibition of human U031 cell growth in a cell viability assay, IC50=6.41816 μM
COR-L23 cell	Growth inhibition assay	Inhibition of human COR-L23 cell growth in a cell viability assay, IC50=6.43346 μM
NCI-H2452 cell	Growth inhibition assay	Inhibition of human NCI-H2452 cell growth in a cell viability assay, IC50=6.52281 μM
BB65-RCC cell	Growth inhibition assay	Inhibition of human BB65-RCC cell growth in a cell viability assay, IC50=6.6459 μM
CAL-33 cell	Growth inhibition assay	Inhibition of human CAL-33 cell growth in a cell viability assay, IC50=6.65665 μM
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	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
	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
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT00676910	Completed	Neoplasms	Johnson & Johnson Pharmaceutical Research & Development L.L.C.	November 2006	Phase 1

参考文献
https://pubmed.ncbi.nlm.nih.gov/20406950/ https://pubmed.ncbi.nlm.nih.gov/21937165/ https://pubmed.ncbi.nlm.nih.gov/21922647/ http://0-www.ncbi.nlm.nih.gov.elis.tmu.edu.tw/pubmed/21922647 + 展开

参考文献

https://pubmed.ncbi.nlm.nih.gov/20406950/
https://pubmed.ncbi.nlm.nih.gov/21937165/
https://pubmed.ncbi.nlm.nih.gov/21922647/

http://0-www.ncbi.nlm.nih.gov.elis.tmu.edu.tw/pubmed/21922647

+ 展开

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)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

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 (6.08 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解配方批次：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
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	3.300mg/ml (10.05mM)	以 1 mL 工作液为例,取50μL66mg/ml的澄清DMSO储备液加到400μLPEG300中,混合均匀使其澄清;向上述体系中加入50μLTween80,混合均匀使其澄清;然后继续加入500μLddH2O定容至1mL。工作液请现配现用!
澄清溶液	5% DMSO 1 95% Corn oil 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	0.400mg/ml (1.22mM)	以1 mL工作液为例，取50μL 8mg/ml的澄清DMSO储备液加到950μL玉米油中，混合均匀。工作液请现配现用！

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

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 μL 动物数量只

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，注：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：取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：取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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