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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Ligand for E3 Ligase Products |
|---|
| 2,6-bis(benzyloxy)-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine
2,6-bis(benzyloxy)-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine |
| 2,6-Bis(benzyloxy)pyridine-3-boronic acid
2,6-Bis(benzyloxy)pyridine-3-boronic acid |
| 2,6-Bis(benzyloxy)-3-bromopyridine
2,6-Bis(benzyloxy)-3-bromopyridine |
| 2,6-bis(benzyloxy)pyridin-3-amine
2,6-bis(benzyloxy)pyridin-3-amine |
| 3-[2,5-Difluoro-4-(4-piperidinyl)phenyl]-2,6-piperidinedione
3-[2,5-Difluoro-4-(4-piperidinyl)phenyl]-2,6-piperidinedione |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
