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
CAS: 19171-19-8
产品质控
批次：
纯度：
99.98%
99.98
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 |
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| 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] |
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|---|---|---|---|---|
| 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。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | CEBPβ IKZF1 / IKZF3 / UBE2G1 / CRBN |
|
21389327 | |
| 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] |
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|---|---|---|
| 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) | |||
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体外溶解度 |
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 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
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
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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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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