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PGMI-004A 

Cat. No. M28163
PGMI-004A  Structure
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Biological Activity

PGMI-004A is a potent phosphoglycerate mutase 1 (PGAM1) inhibitor with an IC50 of 13.1 μM.

Chemical Information
Molecular Weight 463.38
Formula C21H12F3NO6S
CAS Number 1313738-90-7
Form Solid
Solubility (25°C) DMSO ≥ 125 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Nazia Kanwal, et al. Pak J Pharm Sci. In silico-based identification of phytochemicals as novel human phosphoglycerate mutase 1 (PGAM1) inhibitors for cancer therapy

[2] Ke Huang, et al. Eur J Med Chem. Synthesis and biological evaluation of anthraquinone derivatives as allosteric phosphoglycerate mutase 1 inhibitors for cancer treatment

[3] Penghui Wang, et al. Molecules. The Design and Synthesis of N-Xanthone Benzenesulfonamides as Novel Phosphoglycerate Mutase 1 (PGAM1) Inhibitors

[4] Penghui Wang, et al. Bioorg Med Chem. Xanthone derivatives as phosphoglycerate mutase 1 inhibitors: Design, synthesis, and biological evaluation

[5] Taro Hitosugi, et al. Cancer Cell. Phosphoglycerate mutase 1 coordinates glycolysis and biosynthesis to promote tumor growth

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Keywords: PGMI-004A  supplier, Phosphatase, inhibitors, activators


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