An inhibitor of cereblon (IC50 = ~3 µM for the human recombinant CRBN-DDB1 complex); inhibits autoubiquitination of CRBN in HEK293T cells expressing CRBN; inhibits proliferation of U266 myeloma cells at 0.1-10 µM; reduces tumor growth in a H929 R10-1 lenalidomide-resistant mouse xenograft model at 3 mg/kg per day when used in combination with dexamethasone

Pomalidomide – 25 mg

Brand:
Cayman
CAS:
19171-19-8
Storage:
-20
UN-No:
Non-Hazardous - /

Pomalidomide is an analog of thalidomide (Item No. 14610) that inhibits the E3 ligase protein cereblon (CRBN) with an IC50 value of approximately 3 µM for the human recombinant CRBN-DNA damage binding protein-1 (CRBN-DDB1) complex.{23504} It inhibits autoubiquitination of CRBN in HEK293T cells expressing CRBN but not those expressing a thalidomide-binding defective CRBN mutation. It inhibits proliferation of U266 myeloma cells when used at concentrations ranging from 0.1 to 10 µM. Pomalidomide also has antiangiogenic and immunomodulatory effects against myeloma cells, modulating cell adhesion, decreasing production of key pro-survival cytokines, including TNF-α, and triggering the activation of caspase-8.{23505,23398} Pomalidomide (3 mg/kg per day), in combination with dexamethasone, reduces tumor growth in a H929 R10-1 lenalidomide-resistant mouse xenograft model.{42256} Formulations containing pomalidomide have been used in the treatment of multiple myeloma.  

 

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Description

An inhibitor of cereblon (IC50 = ~3 µM for the human recombinant CRBN-DDB1 complex); inhibits autoubiquitination of CRBN in HEK293T cells expressing CRBN; inhibits proliferation of U266 myeloma cells at 0.1-10 µM; reduces tumor growth in a H929 R10-1 lenalidomide-resistant mouse xenograft model at 3 mg/kg per day when used in combination with dexamethasone

Formal name: 4-amino-2-(2,6-dioxo-3-piperidinyl)-1H-isoindole-1,3(2H)-dione

Synonyms:  3-amino Thalidomide|CC-4047

Molecular weight: 273.2

CAS: 19171-19-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Ubiquitin Ligase System||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Tumor Microenvironment||Research Area|Cell Biology|ECM & Adhesion Molecules||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System||Research Area|Immunology & Inflammation

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