3PO is a novel small-molecule inhibitor of the PFKFB3 isozyme, attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines with IC50 of 1.4-24 μM. 3PO reduces glycolytic flux and suppresses glucose uptake. 3PO inhibits endothelial cell proliferation and causes G2/M cell cycle arrest in vitro. 3PO attenuates vessel sprouting and tumor growth in vivo. 3PO amplifies the antiangiogenic effect of VEGFR blockade.
| Molecular Weight | 210.23 |
| Formula | C13H10N2O |
| CAS Number | 18550-98-6 |
| Solubility (25°C) | DMSO 21.02 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 PFKFB3 Products |
|---|
| AZ-67
AZ-67 is an inhibitor of PFKFB3 as well as glycolysis and can be used in studies related to neurodegenerative diseases. |
| AZ-PFKFB3-67 quarterhydrate
AZ-PFKFB3-67 quarterhydrate is potent and selective metabolic kinase PFKFB3 inhibitor, with IC50s of 11, 159 and 1130 nM for PFKFB3, PFKFB2 and PFKFB1 respectively. |
| AZ-PFKFB3-67
AZ-PFKFB3-67 is potent and selective metabolic kinase PFKFB3 inhibitor, with IC50s of 11, 159 and 1130 nM for PFKFB3, PFKFB2 and PFKFB1 respectively. |
| PFK-158
PFK-158, also known as ACT-PFK-158, is a potent and selective inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatases (PFK-2/FBPase) isoform 3 (PFKFB3) with potential antineoplastic activity. |
| AZ PFKFB3 26
AZ PFKFB3 26 is a potent and selective PFKFB3 inhibitor. |
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