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Pomalidomide

別名: CC-4047 中文名稱(chēng)：泊馬度胺

Pomalidomide抑制LPS誘導(dǎo)的TNF-α釋放，在PBMCs中IC50為13 nM。Pomalidomide 可以在PROTAC中用作靶向 E3 ligase 和抑制 E3 ligase protein cereblon (CRBN)。Pomalidomide可促進(jìn)凋亡和細(xì)胞周期阻滯。

Pomalidomide Chemical Structure

Pomalidomide Chemical Structure

CAS: 19171-19-8

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買(mǎi)數(shù)量
10mM (1mL in DMSO) 748.13 現(xiàn)貨
50mg 1556.1 現(xiàn)貨
200mg 3030.3 現(xiàn)貨
1g 7944.3 現(xiàn)貨
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Pomalidomide相關(guān)產(chǎn)品

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類(lèi)型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)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
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生物活性

產(chǎn)品描述 Pomalidomide抑制LPS誘導(dǎo)的TNF-α釋放，在PBMCs中IC50為13 nM。Pomalidomide 可以在PROTAC中用作靶向 E3 ligase 和抑制 E3 ligase protein cereblon (CRBN)。Pomalidomide可促進(jìn)凋亡和細(xì)胞周期阻滯。
特性 Pomalidomide是Thalidomide 衍生物，效果比Thalidomide強(qiáng)10,000倍。
靶點(diǎn)
CRBN [5] TNF-α [1]
(PBMCs)
13 nM
體外研究(In Vitro)
體外研究活性

Pomalidomide 抑制脂多糖(LPS)刺激的TNF-alpha釋放，作用于人類(lèi) PBMC 和人類(lèi)全部血液時(shí)，IC50分別為13 nM 和25 nM。[1] Pomalidomide抑制 IL-2刺激的T 調(diào)節(jié)細(xì)胞，IC50為~1 μM。[2]6.4 nM-10 μM Pomalidomide 處理人類(lèi)外周血T細(xì)胞 ，提高 IL-2 產(chǎn)量，作用于CD4+子集比作用于CD8+子集有效。 Pomalidomide 比CC-5013顯著促進(jìn)IL-2, IL-5,和 IL-10, 比CC-5013稍微促進(jìn) IFN-γ。Pomalidomide 作用于Jurkat細(xì)胞，增強(qiáng) SEE和 Raji細(xì)胞誘導(dǎo)的 AP-1 轉(zhuǎn)錄活性，1 μM時(shí)最高增強(qiáng)4倍，這種作用存在劑量依賴(lài)性。[3] 用不同濃度Pomalidomide(2.5-40 μg/mL) 處理Raji細(xì)胞48小時(shí)，導(dǎo)致細(xì)胞增殖和DNA合成明顯降低，與對(duì)照組相比降低~40% 。[4]
激酶實(shí)驗(yàn) 抑制TNF-α合成實(shí)驗(yàn)
在內(nèi)毒素(LPS)刺激的PBMC中測(cè)定TNF-α抑制活性。Pomalidomide 加到PBMCs中1小時(shí)，然后加入LPS (1 μg/mL)，再處理18-20小時(shí)。收集懸浮液，通過(guò)ELISA測(cè)定懸浮液中的TNF-α濃度。通過(guò)回歸曲線分析計(jì)算IC50值。人類(lèi)全部血液TNF抑制實(shí)驗(yàn)和PBMC實(shí)驗(yàn)差不多，除了肝素化的新鮮血液直接加到微量滴定法板上。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 Raji,SU-DHL-4和SU-DHL-10 細(xì)胞系
濃度 溶于DMSO, 終濃度為2.5-40 μg/mL
孵育時(shí)間 24或48小時(shí)
方法

為了測(cè)定細(xì)胞凋亡,用Pomalidomide(5 μg/mL)處理淋巴瘤細(xì)胞系24小時(shí)或48小時(shí)。用FITC標(biāo)記的膜聯(lián)蛋白V和碘化丙啶進(jìn)行細(xì)胞染色。使用熒光激活細(xì)胞分選儀/FACStar 和流式細(xì)胞儀，通過(guò)多色流式細(xì)胞儀分析細(xì)胞凋亡。如果膜聯(lián)蛋白V陽(yáng)性及碘化丙啶陰性/陽(yáng)性，則判斷為細(xì)胞凋亡(分布為凋亡早期和晚期)。為了測(cè)定細(xì)胞增殖，用Pomalidomide(2.5, 5, 10, 20,和40 μg/mL)處理淋巴瘤細(xì)胞系24小時(shí)或48小時(shí)。在96孔板上，每孔加入1 μCi[3H]-胸甘，細(xì)胞再溫育18小時(shí)。收集細(xì)胞，加到96孔玻璃過(guò)濾器中，然后使用自動(dòng)閃爍計(jì)數(shù)器測(cè)定攝取的[3H]-胸甘。
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot

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