Eprenetapopt (APR-246)

别名: PRIMA-1MET

Eprenetapopt (APR-246, PRIMA-1MET)是一种小分子有机化合物,可以恢复肿瘤抑制功能,主要靶向 突变型p53 ,在多种癌细胞类型中诱导细胞死亡。APR-246 可诱导凋亡和自噬。

Eprenetapopt (APR-246) Chemical Structure

Eprenetapopt (APR-246) Chemical Structure

CAS: 5291-32-7

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1040.13 现货
5mg RMB 795.04 现货
25mg RMB 3252.25 现货
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产品质控

批次: 纯度: 99.69%
99.06

Eprenetapopt (APR-246)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
SKBR3 Cell cycle assay 5 µM 2 weeks lapatinib in combination with APR-246 caused a lower level of G1 arrest and an increase in the sub-G1 fraction 30743996
UMSCC10A Cell viability assay 0-50 μM 72 h suppressed cell survival and bore a modest effect on the killing of HNSCC cells 29348462
FaDu Cell viability assay 0-50 μM 72 h suppressed cell survival and bore a modest effect on the killing of HNSCC cells 29348462
MDA-MB-468 Cell viability assay IC50=5 μM 30196236
BT549 Cell viability assay IC50=3.1 μM 30196236
RS4;11 Cell viability assay high sensitivity and cell death induction in all TP53mut leukemias, but low APR-246 sensitivity in TP53wt ALL 31073076
KOPN-8 Cell viability assay high sensitivity and cell death induction in all TP53mut leukemias, but low APR-246 sensitivity in TP53wt ALL 31073076
MUTZ-5 Cell viability assay high sensitivity and cell death induction in all TP53mut leukemias, but low APR-246 sensitivity in TP53wt ALL 31073076
EU-3 Cell viability assay high sensitivity and cell death induction in all TP53mut leukemias, but low APR-246 sensitivity in TP53wt ALL 31073076
UoCB-6 Cell viability assay high sensitivity and cell death induction in all TP53mut leukemias, but low APR-246 sensitivity in TP53wt ALL 31073076
NALM-6 Cell viability assay high sensitivity and cell death induction in all TP53mut leukemias, but low APR-246 sensitivity in TP53wt ALL 31073076
MDA-MB-231 Cell viability assay IC50=4.1 μM 30196236
HCC1143 Cell viability assay IC50=6.8 μM 30196236
MDA-MB-453 Cell viability assay IC50=0.9 μM 30196236
SKBR3 Cell viability assay IC50=5.1 μM 30196236
UACC812 Cell viability assay IC50=11.3 μM 30196236
MCF7 Cell viability assay IC50=31.1 μM 30196236
MCF10A Cell viability assay IC50=5.2 μM 30196236
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
点击查看更多细胞系数据

生物活性

产品描述 Eprenetapopt (APR-246, PRIMA-1MET)是一种小分子有机化合物,可以恢复肿瘤抑制功能,主要靶向 突变型p53 ,在多种癌细胞类型中诱导细胞死亡。APR-246 可诱导凋亡和自噬。
靶点
Mutant p53 [2]
体外研究(In Vitro)
体外研究活性 APR-246 (PRIMA-1MET)是处于临床一期的化合物,能够恢复突变型p53的活性,并诱导凋亡。APR-246是一种前体药物,能够转化为活性化合物methylene quinuclidinone (MQ, 一种Michael 受体,通过半胱氨酸与突变型p53结合并恢复p53野生型构象)。在耐药性卵巢癌细胞中,APR-246能够完全恢复p53突变体对cisplatin和doxorubicin的敏感性。它不仅重激活p53,也能以剂量依赖方式降低细胞内谷胱甘肽的水平。APR-246通过诱导ROS、ER胁迫和抑制TrxR1,引起p53依赖性细胞凋亡。在骨髓癌细胞中,APR-246通过破坏GSH/ROS的平衡,不受p53的影响下,诱导细胞凋亡[1]。PRIMA-1Met/APR-246在体内能够有效地抑制表达突变型p53的SCLC细胞的生长并诱导期凋亡,DNA片段化增多、caspase-3激活、PARP分裂、Bax和Noxa上调、Bcl-2下调[2]
细胞实验 细胞系 OVCAR-3细胞
浓度 40 μM
孵育时间 20 h
方法

将OVCAR-3细胞以75000细胞每孔的密度接种于12孔板,每孔3 ml培养基。第二天,移除其中2.5 ml培养基,用cisplatin或APR-246或两者结合处理细胞20小时。24小时后,收集细胞,胰蛋白酶化后洗涤两次,用Annexin V and propidium iodine (PI)染色,进行流式分析。

实验图片 检测方法 检测指标 实验图片 PMID
Western blot FL-PARP / Cleaved PARP p-p53 26452133
Growth inhibition assay Cell viability 26452133
体内研究(In Vivo)
体内研究活性 APR-246在临床治疗恶性血液病和前列腺癌的1期和2期的剂量探索研究中,展示了其良好的安全性。在动物实验中,APR-246同样也具有良好耐受性,在携带A2780-CP20移植瘤的小鼠中,APR-246的单次给药能够抑制肿瘤生长,生长率下降了21%[1]
动物实验 Animal Models CD-1 Nu/Nu小鼠
Dosages 400 mg/kg/天
Administration 静脉注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04383938 Completed
Bladder Cancer|Gastric Cancer|Non Small Cell Lung Cancer|NSCLC|Urothelial Carcinoma|Advanced Solid Tumor
Aprea Therapeutics
June 25 2020 Phase 1|Phase 2
NCT04214860 Completed
Myeloid Malignancy
Aprea Therapeutics
December 13 2019 Phase 1
NCT03391050 Terminated
Melanoma
Aprea Therapeutics|Jules Bordet Institute
January 18 2018 Phase 1|Phase 2
NCT02999893 Terminated
Oesophageal Carcinoma
Peter MacCallum Cancer Centre Australia
April 11 2017 Phase 1|Phase 2

化学信息&溶解度

分子量 199.25 分子式

C10H17NO3

CAS号 5291-32-7 SDF Download Eprenetapopt (APR-246) SDF
Smiles COCC1(C(=O)C2CCN1CC2)CO
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 40 mg/mL ( 200.75 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : 40 mg/mL

Ethanol : 40 mg/mL

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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