Pomalidomide (CC-4047)

別名: CC-4047

目錄號(hào)：S1567 Purity: 99.98%

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 (CC-4047) Chemical Structure

CAS: 19171-19-8

規(guī)格	價(jià)格	庫(kù)存
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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產(chǎn)品質(zhì)控

批次：純度： 99.98%

99.98

Pomalidomide (CC-4047)相關(guān)產(chǎn)品

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細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息(PMID)
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

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 PBMC 和人類全部血液時(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)
激酶實(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ELISA測(cè)定懸浮液中的TNF-α濃度。通過回歸曲線分析計(jì)算IC50值。人類全部血液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