All AbMole products are for research use only, cannot be used for human consumption.
Pomalidomide (CC-4047 or Actimid), is a derivative of thalidomide that is anti-angiogenic and also acts as an immunomodulator. Pomalidomide was able to directly inhibit both the tumor cell and vascular compartments of myeloma cancers. This dual activity of pomalidomide makes it more efficacious than thalidomide in vitro and in vivo. Pomalidomide inhibits the growth of T regulatory cells which is stimulated by IL-2 with an IC50 of ~1 μM. In vivo, Pomalidomide treatment of compound resistant myeloma cell tumors in mice was able to produce complete and sustained regressions without any observed toxicity. Additionally, Pomalidomide (CC-4047) induced complete regressions of Burkitt's lymphoma cell tumors. Pomalidomide enhances the antitumor effect of rituximab against B-cell lymphomas in severe combined immunodeficient mice. Phase III results showed significant extension of progression-free survival (median 3.6 months vs. 1.8 months; P < 0.001), and overall survival in patients taking pomalidomide and dexamethasone.
| Molecular Weight | 273.24 |
| Formula | C13H11N3O4 |
| CAS Number | 19171-19-8 |
| Form | Solid |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage | 2-8°C |
| Related Ligand for E3 Ligase Products |
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| Thalidomide
Thalidomide is a sedative and immunomodulator used to study the symptoms of many cancers, it has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM. |
| VH-298
VH-298 is a potent VHL inhibitor that stabilizes HIF-α and elicits a hypoxic response via a different mechanism, with a Kd value of 80 to 90 nM. |
| VHL Ligand 1 hydrochloride
VHL Ligand 1 hydrochloride is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. |
| E3 ligase Ligand 1
E3 ligase Ligand 1 (VHL ligand 2 hydrochloride; (S,R,S)-AHPC-Me hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. |
| E3 ligase Ligand 2
E3 ligase Ligand 2 (Thalidomide-4-OH) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein, it can be connected to the ligand for protein by a linker to form PROTACs. |
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