Pomalidomide

Pomalidomide is an analog of thalidomide (Cay-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. 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-alpha, and triggering the activation of caspase-8. Pomalidomide (3 mg/kg per day), in combination with dexamethasone, reduces tumor growth in a H929 R10-1 lenalidomide-resistant mouse xenograft model. Formulations containing pomalidomide have been used in the treatment of multiple myeloma.Formal Name: 4-amino-2-(2,6-dioxo-3-piperidinyl)-1H-isoindole-1,3(2H)-dione. CAS Number: 19171-19-8. Synonyms: CC-4047, 3-amino Thalidomide. Molecular Formula: C13H11N3O4. Formula Weight: 273.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/mL, DMSO: 15 mg/mL, DMSO:PBS (pH 7.2) (1:6): 0.14 mg/mL. lambdamax: 226, 238, 323, 390 nm. SMILES: NC1=C2C(C(N(C3C(NC(CC3)=O)=O)C2=O)=O)=CC=C1. InChi Code: InChI=1S/C13H11N3O4/c14-7-3-1-2-6-10(7)13(20)16(12(6)19)8-4-5-9(17)15-11(8)18/h1-3,8H,4-5,14H2,(H,15,17,18). InChi Key: UVSMNLNDYGZFPF-UHFFFAOYSA-N.