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.
Thalidomide (50 μg/mL) potentiates the anti-tumor activity of icotinib against the proliferation of both PC9 and A549 cells, and this effect is correlated with apoptosis and cell migration. In addition, Thalidomide and icotinib inhibits the EGFR and VEGF-R2 pathways in PC9 cells.
In vivo, Thalidomide (100 mg/kg, p.o.) inhibits the collagen deposition, down-regulates the mRNA expression level of α-SMA and collagen I, and significantly reduces the pro-inflammatory cytokines in RILF mice. Thalidomide alleviates RILF via suppression of ROS and down-regulation of TGF-β/Smad pathway dependent on Nrf2 status.
Brain Behav Immun. 2022 Feb 7;102:23-39.
Spinal microglia-derived TNF promotes the astrocytic JNK/CXCL1 pathway activation in a mouse model of burn pain
Thalidomide purchased from AbMole
Biomed Pharmacother. 2021 Sep;141:111876.
Cudraxanthone L inhibits gastric cancer by regulating the MAPK signalling and promoting FAS-mediated pathway
Thalidomide purchased from AbMole
| Molecular Weight | 258.23 |
| Formula | C13H10N2O4 |
| CAS Number | 50-35-1 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
[1] Takumi Ito, et al. Molecular mechanisms of thalidomide and its derivatives
[2] James E Ridings. The thalidomide disaster, lessons from the past
[3] Michael E Franks, et al. Thalidomide
[4] E Laffitte, et al. Thalidomide
[5] R J D'Amato, et al. Thalidomide is an inhibitor of angiogenesis
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