Pomalidomide

SKU: orb1305562

Description

Pomalidomide is a cereblon (CRBN)-binding immunomodulatory and anti-angiogenic agent. It is widely utilized in research for the development of PROTAC degraders and has been investigated in both in vitro and in vivo models for oncology and immunology applications.

Research Area

Cardiovascular Research, Immunology & Inflammation, Protein Biochemistry

Key Properties

• CAS Number: 19171-19-8
• MW: 273.2
• Purity: >98%
• Formula: C₁₃H₁₁N₃O₄
• SMILES: Nc1cccc2C(=O)N(C3CCC(=O)NC3=O)C(=O)c12
• Target: Ubiquitin ligase
• Solubility: Soluble in DMSO (up to 50 mg/ml)

Bioactivity

• Target IC50:
  TNF-α:13 nM (PBMCs)
• In Vivo:
  METHODS: To assess the potential value in cerebral ischemia, Pomalidomide (50 mg/kg, 1% carboxy methyl cellulose) was administered intraperitoneally once daily for 21 days to transgenic mice chronically overexpressing the TNF-α surface-active protein (SP)-C promoter (SP-C/TNF-α mice). RESULTS: Pomalidomide significantly reduced serum TNF-α and IL-5 levels.
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• In Vitro:
  METHODS: Multiple myeloma cells RPMI8226 and OPM2 were treated with Pomalidomide (0.01-50 µM) for 48 h. Cell viability was measured by MTT assay. RESULTS: Pomalidomide significantly decreased the cell viability of RPMI8226 and OPM2 cells at 48 h with IC50 values of 8 µM and 10 µM, respectively. METHODS: Multiple myeloma cells H929, U266 and MM.1s were treated with Pomalidomide (0.05-1 µM) and ACY-241 (3 µM) for 4 days and apoptosis was detected by Flow cytometry. RESULTS: Apoptosis was significantly increased when the two drugs were combined relative to either single drug.
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• Cell Research:
  In vitro effects of either CC-5013 or CC-4047 as single agent or in combination with rituximab were evaluated by flow cytometric analysis. Lymphoma cell lines (1 × 10^6 cells) were exposed to either CC-5013 (5 μg/mL), CC-4047 (5 μg/mL), or vehicle control (DMRIE-C, 0.01%) alone or in combination with rituximab at a final concentration of 10 μg/mL. Following a period of incubation of 24 or 48 hours, apoptosis was assessed by staining-treated cells with FITC-labeled Annexin V and propidium iodine. All samples were analyzed by multicolor flow cytometric analysis using a fluorescence-activated cell sorter/FACStar Plus flow cytometer. Cells were scored as apoptotic if they were Annexin V–positive and propidium iodine–negative/positive (early and late apoptosis, respectively) .
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• Animal Research:
  These studies were carried out using a disseminated lymphoma-bearing SCID mouse xenograft model. Raji cells were harvested from confluent cultures and only suspensions with >90% viable cells were used for animal inoculation. Subsequently, on day 0, SCID mice received 1 ×10^6 Raji cells via i.v. Untreated SCID mice inoculated by i.v. injection develop symptomatic central nervous system, pulmonary, and liver metastasis that result in death from massive tumor burden and central nervous system involvement after 17 to 21 days after inoculation. A second lymphoma mouse model was used to address the significance of NK cell expansion in the biological interactions observed between rituximab and IMiDs. The second mouse lymphoma xenograft consisted of SCID mice depleted of NK cells bearing Raji cells implanted via tail vein injection as described above .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CC-4047

Compound Identifiers

PubChem CID

134780