ホームページ Ubiquitin E3 ligase Ligand chemical - TNF-alpha inhibitor - E3 Ligase inhibitor - Apoptosis related activator Pomalidomide For research use only.

Pomalidomide

別名：CC-4047

Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs. Pomalidomide can be utilized in PROTAC as a ligand for targeting E3 ligase and inhibiting the E3 ligase protein cereblon (CRBN). Pomalidomide promotes apoptosis and cell cycle arrest.

Pomalidomide化学構造

CAS No. 19171-19-8

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 40500 国内在庫あり
JPY 28500 国内在庫あり
JPY 55500 国内在庫あり
JPY 145500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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製品安全説明書

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Pomalidomide関連製品

E3 ligase Ligand阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 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

製品説明 Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs. Pomalidomide can be utilized in PROTAC as a ligand for targeting E3 ligase and inhibiting the E3 ligase protein cereblon (CRBN). Pomalidomide promotes apoptosis and cell cycle arrest.
特性 A derivative of thalidomide and up to 10,000 times more potent than thalidomide.
Targets
CRBN [5] TNF-α [1]
(PBMCs)
13 nM
In Vitro
In vitro

Pomalidomide inhibits lipopolysaccharide (LPS) stimulated TNF-alpha release in human PBMC and in human whole blood with IC50 values of 13 nM and 25 nM, respectively. [1] Pomalidomide inhibits the growth of T regulatory cells which is stimulated by IL-2 with an IC50 of ~1 μM. [2] Treatment with Pomalidomide (6.4 nM-10 μM) increases the production of IL-2 in human peripheral blood T cells, and is slightly more potent in the CD4+ subset than in the CD8+ subset. Pomalidomide is significantly more potent than CC-5013 at elevating IL-2, IL-5, and IL-10 levels, but only slightly more potent than CC-5013 at elevating IFN-γ levels. Pomalidomide enhances SEE and Raji cells induced AP-1 transcriptional activity in Jurkat cells in a dose-dependent manner, with a maximal enhancement of 4-fold at 1 μM. [3] Exposure of Raji cells to various concentrations of Pomalidomide (2.5-40 μg/mL) for 48 hours leads to a significant decrease in cell proliferation and DNA synthesis. There is a reduction of ~40% compared to vehicle-treated controls. [4]
Kinase Assay Inhibition of TNF-α synthesis
TNF-α inhibitory activity is measured in lipopolysacharide (LPS) stimulated PBMC. Pomalidomide is added to human PBMCs 1 hour prior to the addition of LPS (1 μg/mL) and incubation continued for an additional 18-20 hours. Supernatants are then harvested, and the concentration of TNF-α in the supernatants is determined by ELISA. The concentration of Pomalidomide that inhibits TNF- production by 50% (IC50) is calculated by nonlinear regression analysis. The human whole blood TNF- inhibition assay is run in a similar fashion to the PBMC assay except that heparinized fresh human whole blood is plated directly into microtiter plates.
細胞実験 細胞株 Raji, SU-DHL-4 and SU-DHL-10 cell lines
濃度 Dissolved in DMSO, final concentrations 2.5-40 μg/mL
反応時間 24 or 48 hours
実験の流れ

For assessment of cell apoptosis, Lymphoma cell lines are exposed to Pomalidomide (5 μg/mL) for 24 hours or 48 hours. The cells are stained with FITC-labeled Annexin V and propidium iodine. Cell apoptosis is analyzed by multicolor flow cytometric analysis using a fluorescence-activated cell sorter/FACStar Plus flow cytometer. Cells are scored as apoptotic if they are Annexin V–positive and propidium iodine–negative/positive (early and late apoptosis, respectively). For determination of cell proliferation, the Lymphoma cell lines are exposed to Pomalidomide (2.5, 5, 10, 20, and 40 μg/mL) for 24 hours or 48 hours. 1 μCi per well (96-well plate) of [3H]-thymidine is added and cells are incubated for another 18 hours. Cells are then harvested using the Harvest system into the 96-well glass filters and [3H]-thymidine uptake is measured using an automated scintillation counter.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot CEBPβ IKZF1 / IKZF3 / UBE2G1 / CRBN 21389327
Immunofluorescence IKZF1 29496670
In Vivo
In Vivo

Pomalidomide enhances the antitumor effect of rituximab against B-cell lymphomas in severe combined immunodeficient mice. Administration of Pomalidomide in combination with rituximab, gives the mice a median survival period of 74 days compared with 58 days of CC5013/rituximab treatment and 45 days of rituximab nonotherapy. The synergistic effect of Pomalidomide and rituximab can be completely abrogated by depletion of NK cells, supporting the proposal that NK cell expansion is one mechanism by which Pomalidomide may augment rituximab antitumor activity. [4]
動物実験 動物モデル Disseminated lymphoma-bearing SCID mice
投与量 0.5 mg/kg
投与経路 Injection i.p.
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

化学情報

分子量 273.24 化学式

C13H11N3O4
CAS No. 19171-19-8 SDF Download Pomalidomide SDFをダウンロードする
Smiles C1CC(=O)NC(=O)C1N2C(=O)C3=C(C2=O)C(=CC=C3)N
保管

In vitro
Batch:

DMSO : 55 mg/mL ( (201.28 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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よくある質問（FAQ）

質問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.

質問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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