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Reagentes e instrumentos para imunologia, biologia celular e biologia molecular.

Pomalidomide [19171-19-8]

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Referência HY-10984-50mg

Tamanho : 50mg

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Telefone : +1 850 650 7790

Marca : MedChemExpress

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Description

Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.

IC₅₀ & Target^[5]

Cereblon

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	> 10 μM Compound: POM	Cytotoxicity against human A375 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A375 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33256948]
A549	IC₅₀	> 33.3 μM Compound: Poma	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay	[PMID: 39089850]
B16-F10	IC₅₀	> 10 μM Compound: POM	Cytotoxicity against mouse B16F10 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against mouse B16F10 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33256948]
BXPC-3	IC₅₀	<= 30 μM Compound: POM	Antiproliferative activity against human BxPC-3 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against human BxPC-3 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 33506674]
HCT-116	IC₅₀	> 33.3 μM Compound: Poma	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay	[PMID: 39089850]
HCT-116	IC₅₀	> 50 μM Compound: Pomalidomide	Antiproliferative activity against human HCT-116 cells expressing wildtype ATM incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HCT-116 cells expressing wildtype ATM incubated for 72 hrs by CCK8 assay	[PMID: 38325007]
HeLa	IC₅₀	1.27 μM Compound: actimid	Inhibition of IL-1-alpha-induced NF-kappaB activation in HeLa cells assessed as blocking of p50/p65 nuclear translocation Inhibition of IL-1-alpha-induced NF-kappaB activation in HeLa cells assessed as blocking of p50/p65 nuclear translocation	[PMID: 17845850]
JeKo-1	IC₅₀	2617.33 nM Compound: Pomalidomide	Antiproliferative activity against human Jeko-1 cells assessed as cell viability measured after 7 days by CCK-8 assay Antiproliferative activity against human Jeko-1 cells assessed as cell viability measured after 7 days by CCK-8 assay	[PMID: 35635954]
JeKo-1	IC₅₀	> 20000 nM Compound: Pomalidomide	Antiproliferative activity against human Jeko-1 cells expressing CRBN-knockout assessed as cell viability measured after 7 days by CCK-8 assay Antiproliferative activity against human Jeko-1 cells expressing CRBN-knockout assessed as cell viability measured after 7 days by CCK-8 assay	[PMID: 35635954]
Jurkat	IC₅₀	> 33.3 μM Compound: Poma	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay	[PMID: 39089850]
K562	IC₅₀	> 10 μM Compound: Pomalidomide	Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 34217059]
K562	IC₅₀	> 10 μM Compound: Pomalidomide	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 2 days by CCK8 assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 2 days by CCK8 assay	[PMID: 36306539]
KARPAS-299	IC₅₀	> 10 μM Compound: pomalidomide	Antiproliferative activity against human KARPAS-299 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human KARPAS-299 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34176264]
LP-1	GI₅₀	> 10 μM Compound: pom	Antiproliferative activity against human LP-1 cells assessed as growth inhibition incubated for 3 days by fluorescence based assay Antiproliferative activity against human LP-1 cells assessed as growth inhibition incubated for 3 days by fluorescence based assay	[PMID: 38505842]
LoVo	IC₅₀	> 50 μM Compound: Pomalidomide	Antiproliferative activity against ATM deficient human LoVo cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against ATM deficient human LoVo cells incubated for 72 hrs by CCK8 assay	[PMID: 38325007]
MCF7	IC₅₀	17 μM Compound: Pomalidomide	Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 37229829]
MCF7	IC₅₀	> 100 μM Compound: Poma	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 37619298]
MCF7	IC₅₀	> 100 μM Compound: Pomalidomide	Antiproliferative activity against human MCF-7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF-7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 34864330]
MDA-MB-231	IC₅₀	> 100 μM Compound: Poma	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 37619298]
MDA-MB-231	IC₅₀	> 100 μM Compound: Pomalidomide	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 34864330]
MDA-MB-468	IC₅₀	> 100 μM Compound: Poma	Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 37619298]
MIA PaCa-2	IC₅₀	<= 30 μM Compound: POM	Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 33506674]
MM1.S	IC₅₀	21.93 nM Compound: Pomalidomide	Antiproliferative activity against human MM1.S cells assessed as cell viability measured after 7 days by CCK-8 assay Antiproliferative activity against human MM1.S cells assessed as cell viability measured after 7 days by CCK-8 assay	[PMID: 35635954]
MM1.S	IC₅₀	837.8 nM Compound: Pomalidomide	Antiproliferative activity against human MM1.S cells assessed as cell viability measured after 3 days by CCK-8 assay Antiproliferative activity against human MM1.S cells assessed as cell viability measured after 3 days by CCK-8 assay	[PMID: 35635954]
MX1	IC₅₀	> 100 μM Compound: Poma	Antiproliferative activity against human MX1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MX1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 37619298]
NAMALVA	IC₅₀	0.03 μM Compound: 2	Antiproliferative activity against human NAMALWA cells assessed as inhibition of [3H]thymidine incorporation after 72 hrs by scintillation counting Antiproliferative activity against human NAMALWA cells assessed as inhibition of [3H]thymidine incorporation after 72 hrs by scintillation counting	[PMID: 23168019]
NCI-H929	CC₅₀	0.035 μM Compound: Pomalidomide	Antiproliferative activity against human NCI-H929 cells after 72 hrs by WST-1 assay Antiproliferative activity against human NCI-H929 cells after 72 hrs by WST-1 assay	[PMID: 30684871]
OCI-Ly10	IC₅₀	1.4 μM Compound: 2	Antiproliferative activity against human OCI-Ly10 cells measured after 4 days by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human OCI-Ly10 cells measured after 4 days by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 38920289]
PBMC	IC₅₀	0.013 μM Compound: 2	Inhibition of TNF-alpha production in LPS-stimulated human PBMC preincubated for 1 hr before LPS challenge measured after 28 to 20 hrs by ELISA Inhibition of TNF-alpha production in LPS-stimulated human PBMC preincubated for 1 hr before LPS challenge measured after 28 to 20 hrs by ELISA	[PMID: 23168019]
PBMC	IC₅₀	13 nM Compound: 5a	Inhibition of lipopolysaccharide stimulated TNF-alpha release in human PBMC Inhibition of lipopolysaccharide stimulated TNF-alpha release in human PBMC	[PMID: 10386948]
T-cell	EC₅₀	0.008 μM Compound: 2	Inhibition of IL-2 production in human T cells measured after 2 to 3 days by ELISA Inhibition of IL-2 production in human T cells measured after 2 to 3 days by ELISA	[PMID: 23168019]
THP-1	IC₅₀	> 33.3 μM Compound: Poma	Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay	[PMID: 39089850]
TMD8	IC₅₀	187 nM Compound: Pomalidomide	Cytotoxicity against human TMD8 cells incubated for 48 hrs by celltitre glo 2.0 assay Cytotoxicity against human TMD8 cells incubated for 48 hrs by celltitre glo 2.0 assay	[PMID: 37195170]

In Vitro

Pomalidomide also inhibits Whole Blood TNF-α with IC₅₀ of 25 nM^[1]. Exposure of lymphoma cells to Pomalidomide (CC-4047) leads to 40% decrease in cell proliferation when compared with vehicle-treated controls. Pomalidomide inhibits by 40% the DNA synthesis of Raji cells (P=0.036)^[2]. In both CD4⁺ and CD8⁺ cells, Pomalidomide (CC-4047) is the most potent IL-2-elevator, followed by CC-6032 and CC-5013. Pomalidomide is significantly more potent than CC-5013 at elevating IL-2, IL-5, and IL-10, and slightly more potent than CC-5013 at elevating IFN-γ^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (182.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.6598 mL	18.2989 mL	36.5979 mL
5 mM	0.7320 mL	3.6598 mL	7.3196 mL
10 mM	0.3660 mL	1.8299 mL	3.6598 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/0.5% Tween-80 in Saline water
Solubility: 10 mg/mL (36.60 mM); Suspended solution; Need ultrasonic

Pureté et documentation

Purity: 99.96%

Fiche technique (285 KB) SDS (418 KB)

COA (252 KB) HNMR (119 KB) RP-HPLC (144 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Zhu YX, et al. Molecular mechanism of action of the immune-modulatory drugs, thalidomide, lenalidomide and pomalidomide in multiple myeloma. Leuk Lymphoma. 2013 Apr;54(4):683-7. [Content Brief]

[2]. Hernandez-Ilizaliturri FJ1, et al. Immunomodulatory drug CC-5013 or CC-4047 and rituximab enhance antitumor activity in a severe combined immunodeficient mouse lymphoma model. Clin Cancer Res. 2005 Aug 15;11(16):5984-92. [Content Brief]

[3]. Schafer PH, et al. Enhancement of cytokine production and AP-1 transcriptional activity in T cells by thalidomide-related immunomodulatory drugs. J Pharmacol Exp Ther. 2003 Jun;305(3):1222-32. [Content Brief]

[4]. Li Z, et al. Pomalidomide shows significant therapeutic activity against CNS lymphoma with a major impact on the tumor microenvironment in murine models. PLoS One. 2013 Aug 5;8(8):e71754. [Content Brief]

[5]. Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63. [Content Brief]

[6]. Liu D, et al. Tumour necrosis factor-α inhibits hepatic lipid deposition through GSK-3β/β-catenin signaling in juvenile turbot (Scophthalmus maximus L.). Gen Comp Endocrinol. 2016 Mar 1;228:1-8. [Content Brief]

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Referência HY-10984-50mg

Contactar o distribuidor local :

Marca : MedChemExpress

Contactar o distribuidor local :

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