Pomalidomide

别名: CC-4047 中文名称:泊马度胺

Pomalidomide抑制LPS诱导的TNF-α释放,在PBMCs中IC50为13 nM。Pomalidomide 可以在PROTAC中用作靶向 E3 ligase 和抑制 E3 ligase protein cereblon (CRBN)。Pomalidomide可促进凋亡和细胞周期阻滞。

Pomalidomide Chemical Structure

Pomalidomide Chemical Structure

CAS: 19171-19-8

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 748.13 现货
50mg RMB 1556.1 现货
200mg RMB 3030.3 现货
1g RMB 7944.3 现货
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客户使用Selleck的Pomalidomide发表文献101

产品质控

批次: 纯度: 99.98%
99.85

Pomalidomide相关产品

E3 ligase Ligand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
SH-SY5Y  Apoptosis Assay 25 μg/mL 1 h causes statistically significant reduction in both CPF- and CPF+CM-induced apoptosis  24975276
RPMI8226 Function Assay 0.1-10 μM 4 h increases VEGF mRNA expression 25053990
OPM2  Function Assay 10 μM 48 h strengthens cytoplasmic-nuclear shuttling of mTOR and p-mTOR protein 26097872
RPMI8226  Function Assay 10 μM 48 h strengthens cytoplasmic-nuclear shuttling of mTOR and p-mTOR protein 26097872
OPM2  Growth Inhibition Assay 0.01-50 μM 48 h IC50=10 μM 26097872
RPMI8226  Growth Inhibition Assay 0.01-50 μM 48 h IC50=8 μM 26097872
APK-1 Growth Inhibition Assay 39-1250 nM 5 d IC50=226 nM, inhibits cell viability dose dependently 26119939
BCP-1 Growth Inhibition Assay 39-1250 nM 5 d IC50=396 nM, inhibits cell viability dose dependently 26119939
BC-1 Growth Inhibition Assay 39-1250 nM 5 d IC50=744 nM, inhibits cell viability dose dependently 26119939
UMPEL-3 Growth Inhibition Assay 39-1250 nM 5 d IC50=111 nM, inhibits cell viability dose dependently 26119939
UMPEL-1 Growth Inhibition Assay 39-1250 nM 5 d IC50=32 nM, inhibits cell viability dose dependently 26119939
VG-1 Growth Inhibition Assay 39-1250 nM 5 d IC50=101 nM, inhibits cell viability dose dependently 26119939
JSC-1 Growth Inhibition Assay 39-1250 nM 5 d IC50=34 nM, inhibits cell viability dose dependently 26119939
BCBL-1 Growth Inhibition Assay 39-1250 nM 5 d IC50=74 nM, inhibits cell viability dose dependently 26119939
BC-3 Growth Inhibition Assay 39-1250 nM 5 d IC50=107 nM, inhibits cell IC50=107 nM, viability dose dependently 26119939
R-CD38 Cytotoxicity Assay 10 μM 24 h potently augments direct and indirect MM cell killing by SAR 26338273
J-CD38 Cytotoxicity Assay 10 μM 24 h potently augments direct and indirect MM cell killing by SAR 26338273
MOLP-8 Cytotoxicity Assay 10 μM 24 h potently augments direct and indirect MM cell killing by SAR 26338273
JJN3 Growth Inhibition Assay 0.1-100 μM 72 h inhibits cell growth slightly 23178378
XG-1 Growth Inhibition Assay 0.1-100 μM 72 h inhibits cell growth 23178378
CD138+  Growth Inhibition Assay 0.1-100 μM 72 h inhibits cell growth 23178378
XG-1 Function Assay 2/100 μM 24 h inhibits CCL3/MIP-1α mRNA expression 23178378
U266 Growth Inhibition Assay 0.01-10 μM 48 h inhibits cell growth dose dependently 22552008
CRBN60 Growth Inhibition Assay 0.01-10 μM 48 h inhibits cell growth dose dependently 22552008
CRNB75 Growth Inhibition Assay 0.01-10 μM 48 h inhibits cell growth dose dependently 22552008
MM.1S Growth Inhibition Assay 0.01-10 μM 48 h significantly inhibits proliferation at concentrations as low as 0.01μM 21389327
OPM2 Growth Inhibition Assay 0.01-10 μM 48 h significantly inhibits proliferation at concentrations as low as 0.01μM 21389327
MM.1S Function Assay 10 μM 72 h significantly decreases the protein level of C/EBPβ isoforms  21389327
H929 Function Assay 10 μM 72 h significantly decreases the protein level of C/EBPβ isoforms  21389327
OPM2 Function Assay 10 μM 72 h significantly decreases the protein level of C/EBPβ isoforms  21389327
CT26 Function Assay 1/10 μM 24 h reduces the numbers of live colonies  19638977
DF15 Function assay 0.01 to 1 uM 5 hrs Induction of cereblon-mediated aiolos degradation in human DF15 cells at 0.01 to 1 uM after 5 hrs by immunoblot analysis 28425720
OPM2 Function assay 0.01 to 1 uM 5 hrs Induction of cereblon-mediated ikaros degradation in human OPM2 cells at 0.01 to 1 uM after 5 hrs by immunoblot analysis 28425720
DF15 Function assay 0.01 to 1 uM 5 hrs Induction of cereblon-mediated ikaros degradation in human DF15 cells at 0.01 to 1 uM after 5 hrs by immunoblot analysis 28425720
OPM2 Function assay 0.01 to 1 uM 5 hrs Induction of cereblon-mediated aiolos degradation in human OPM2 cells at 0.01 to 1 uM after 5 hrs by immunoblot analysis 28425720
T-cells Function assay 2 to 3 days Inhibition of IL-2 production in human T cells measured after 2 to 3 days by ELISA, EC50 = 0.008 μM. 23168019
DF15 Function assay 4 hrs Induction of cereblon-mediated aiolos degradation in human DF15 cells expressing ePL-tagged aiolos after 4 hrs by luminometric analysis, EC50 = 0.022 μM. 28425720
DF15 Function assay 4 hrs Induction of cereblon-mediated ikaros degradation in human DF15 cells expressing ePL-tagged ikaros after 4 hrs by luminometric analysis, EC50 = 0.024 μM. 28425720
DF15 Function assay 4 hrs Induction of CRL4/CRBN ubiquitin ligase-mediated aiolos degradation in human DF15 cells expressing pLOC-ePL-tagged aiolos after 4 hrs by luminescence based beta-galactosidase enzyme fragmentation complementation assay, EC50 = 0.027 μM. 28358507
NAMALWA Antiproliferative assay 72 hrs Antiproliferative activity against human NAMALWA cells assessed as inhibition of [3H]thymidine incorporation after 72 hrs by scintillation counting, IC50 = 0.03 μM. 23168019
HeLa Function assay Inhibition of IL-1-alpha-induced NF-kappaB activation in HeLa cells assessed as blocking of p50/p65 nuclear translocation, IC50 = 1.27 μM. 17845850
点击查看更多细胞系数据

生物活性

产品描述 Pomalidomide抑制LPS诱导的TNF-α释放,在PBMCs中IC50为13 nM。Pomalidomide 可以在PROTAC中用作靶向 E3 ligase 和抑制 E3 ligase protein cereblon (CRBN)。Pomalidomide可促进凋亡和细胞周期阻滞。
特性 Pomalidomide是Thalidomide 衍生物,效果比Thalidomide强10,000倍。
靶点
CRBN [5] TNF-α [1]
(PBMCs)
13 nM
体外研究(In Vitro)
体外研究活性

Pomalidomide 抑制脂多糖(LPS)刺激的TNF-alpha释放,作用于人类 PBMC 和人类全部血液时,IC50分别为13 nM 和25 nM。[1] Pomalidomide抑制 IL-2刺激的T 调节细胞,IC50为~1 μM。[2]6.4 nM-10 μM Pomalidomide 处理人类外周血T细胞 ,提高 IL-2 产量,作用于CD4+子集比作用于CD8+子集有效。 Pomalidomide 比CC-5013显著促进IL-2, IL-5,和 IL-10, 比CC-5013稍微促进 IFN-γ。Pomalidomide 作用于Jurkat细胞,增强 SEE和 Raji细胞诱导的 AP-1 转录活性,1 μM时最高增强4倍,这种作用存在剂量依赖性。[3] 用不同浓度Pomalidomide(2.5-40 μg/mL) 处理Raji细胞48小时,导致细胞增殖和DNA合成明显降低,与对照组相比降低~40% 。[4]

激酶实验 抑制TNF-α合成实验
在内毒素(LPS)刺激的PBMC中测定TNF-α抑制活性。Pomalidomide 加到PBMCs中1小时,然后加入LPS (1 μg/mL),再处理18-20小时。收集悬浮液,通过ELISA测定悬浮液中的TNF-α浓度。通过回归曲线分析计算IC50值。人类全部血液TNF抑制实验和PBMC实验差不多,除了肝素化的新鲜血液直接加到微量滴定法板上。
细胞实验 细胞系 Raji,SU-DHL-4和SU-DHL-10 细胞系
浓度 溶于DMSO, 终浓度为2.5-40 μg/mL
孵育时间 24或48小时
方法

为了测定细胞凋亡,用Pomalidomide(5 μg/mL)处理淋巴瘤细胞系24小时或48小时。用FITC标记的膜联蛋白V和碘化丙啶进行细胞染色。使用荧光激活细胞分选仪/FACStar 和流式细胞仪,通过多色流式细胞仪分析细胞凋亡。如果膜联蛋白V阳性及碘化丙啶阴性/阳性,则判断为细胞凋亡(分布为凋亡早期和晚期)。为了测定细胞增殖,用Pomalidomide(2.5, 5, 10, 20,和40 μg/mL)处理淋巴瘤细胞系24小时或48小时。在96孔板上,每孔加入1 μCi[3H]-胸甘,细胞再温育18小时。收集细胞,加到96孔玻璃过滤器中,然后使用自动闪烁计数器测定摄取的[3H]-胸甘。

实验图片 检测方法 检测指标 实验图片 PMID
Western blot IKZF1 / IKZF3 / UBE2G1 / CRBN CEBPβ 30234487
Immunofluorescence IKZF1 29496670
体内研究(In Vivo)
体内研究活性

Pomalidomide 作用于SCID小鼠,增强 Rituximab作用于B细胞淋巴瘤的抗癌效果。Pomalidomide和Rituximab联用使鼠平均寿命为74天,与 CC5013/Rituximab 处理的鼠平均寿命为58天。NK细胞耗尽则Pomalidomide和Rituximab协同作用完全被废除, 说明NK细胞增多是Pomalidomide增强 Rituximab抗癌的一个机制。[4]

动物实验 Animal Models 携带扩散性淋巴瘤的SCID小鼠
Dosages 0.5 mg/kg
Administration 腹腔注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04902443 Recruiting
Viral Associated Malignancies|Kaposi Sarcoma|EBV/KSHV-associated Lymphomas
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
December 10 2021 Phase 1

化学信息&溶解度

分子量 273.24 分子式

C13H11N3O4

CAS号 19171-19-8 SDF Download Pomalidomide SDF
Smiles C1CC(=O)NC(=O)C1N2C(=O)C3=C(C2=O)C(=CC=C3)N
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 55 mg/mL ( 201.28 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : 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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常见问题及建议解决方法

问题 1:
Is S1567 in the 1% DMSO+30% polyethylene glycol+1% Tween 80 suitable for oral administration?

回答:
S1567 in 1% DMSO+30% polyethylene glycol+1% Tween 80 is a suspension. This formulation is for oral gavege.

问题 2:
I would like to know if the pomalidomide is racemic or optically active?

回答:
Our S1567 Pomalidomide is racemic.

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