LB-100 is a water soluble protein phosphatase 2A (PP2A) inhibitor, with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells. LB-100 increases concentration of doxorubicin within cells (2.5 fold to control) and sensitizes tumor cells to the cytotoxicity of doxorubicin. LB-100 increaseds VEGF secretion, and thus enhances HIF-1α-VEGF mediated angiogenesis.
In vivo, LB-100 (2 mg/kg, i.p.) decreases in a time-dependent manner the activity of PP2A in xenografts and livers in nude mice. The combination of doxorubicin (1.5 kg/mL, every other day) and LB-100 (2 mg/kg, every other day) significantly slows the growth of tumors with reduction of tumor volume in two animals with no effects on tumor growth in animals treated with single agents.
Another CAS# 1632032-53-1
Molecular Weight | 268.31 |
Formula | C13H20N2O4 |
CAS Number | 1026680-07-8 |
Solubility (25°C) | Water ≥ 40 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.
Related PPAR Products |
---|
DSO-5a
DSO-5a is a potent, selective, orally active BB3 agonist. |
Carfloglitazar sodium
Carfloglitazar sodium is a dual agonist of the pan peroxisome proliferator-activated receptor (PPARα/γ) with EC50 values of 1.2, 0.08, and 1.7 μM for PPARα, PPARγ, and PPARδ, respectively.It can be used in studies related to nonalcoholic steatohepatitis (NASH). |
Seladelpar
Seladelpar is a potent, orally active, specific PPAR-δ agonist with an EC50 of 2 nM. |
4'-O-Methylhonokiol
4-O-Methyl honokiol is a natural neolignan isolated from Magnolia officinalis, acts as a PPARγ agonist, and inhibtis NF-κB activity, used for cancer and inflammation research. |
3-Phenyl-2-propen-1-ol
trans-Cinnamyl alcohol is a trans-isomer of Cinnamyl alcohol. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.