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PF-06843195

Cat. No. M21296
PF-06843195 Structure
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Biological Activity

PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts.The Ki of PF-06843195 acting on PI3Kα and PI3Kδ is less than 0.018 nM and 0.28 nM, respectively.PF-06843195 has a significant inhibitory effect on PI3K/mTOR signaling pathway and had a long-lasting anti-tumor effect.

Chemical Information
Molecular Weight 498.46
Formula C20H25F3N8O4
CAS Number 2067281-51-8
Solubility (25°C) DMSO : 62.5 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] Hengmiao Cheng, et al. J Med Chem. Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195)

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