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PI3Kγ inhibitor 7

Cat. No. M43388
PI3Kγ inhibitor 7 Structure
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Biological Activity

PI3Kγ inhibitor 7 is a potent and orally active PI3Kγ inhibitor with IC50 values of 4768, 878.1, 3.42, 355.2 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively.

Chemical Information
Molecular Weight 555.59
Formula C31H25N9O2
CAS Number 2575863-25-9
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] Dongyan Song et al. JCI Insight. PTP1B inhibitors protect against acute lung injury and regulate CXCR4 signaling in neutrophils

[2] Kevin H Lin et al. Nat Cancer. P2RY2-AKT activation is a therapeutically actionable consequence of XPO1 inhibition in acute myeloid leukemia

[3] Kouji Matsushima et al. Cytokine. Interleukin-8: An evolving chemokine

[4] Christopher Ronald Funk et al. Blood. PI3Kδ/γ inhibition promotes human CART cell epigenetic and metabolic reprogramming to enhance antitumor cytotoxicity

[5] Mingchuan Li et al. Circulation. Phosphoinositide 3-Kinase Gamma Inhibition Protects From Anthracycline Cardiotoxicity and Reduces Tumor Growth

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