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THZ-P1-2

Cat. No. M21521
THZ-P1-2  Structure
Size Price Availability
10mg USD 780  USD780 1-2 Weeks
50mg USD 2200  USD2200 1-2 Weeks
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Quality Control & Documentation
Biological Activity

THZ-P1-2 is a first-in-class, selective PI5P4K inhibitor with an IC50 of 190 nM for Pi5P4α.

Chemical Information
Molecular Weight 531.61
Formula C31H29N7O2
CAS Number 2058075-45-7
Solubility (25°C) DMSO ≥ 200 mg/mL
Storage 2-8℃, protect from light, dry, sealed
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] Keli Lima, et al. Blood Cancer J. The PIP4K2 inhibitor THZ-P1-2 exhibits antileukemia activity by disruption of mitochondrial homeostasis and autophagy

[2] Theresa D Manz, et al. ACS Med Chem Lett. Structure-Activity Relationship Study of Covalent Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors

[3] Sindhu Carmen Sivakumaren, et al. Cell Chem Biol. Targeting the PI5P4K Lipid Kinase Family in Cancer Using Covalent Inhibitors

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  Catalog
Abmole Inhibitor Catalog




Keywords: THZ-P1-2 supplier, PI5P4K, inhibitors, activators


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