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CAY10505

Cat. No. M3367
CAY10505 Structure
Size Price Availability
25mg USD 80  USD80 Out of stock
50mg USD 140  USD140 Out of stock
200mg USD 380  USD380 Out of stock
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Quality Control & Documentation
Biological Activity

CAY10505 is a potent PI3Kγ inhibitor with an IC50 of 30 nM. Phosphoinositide 3-kinase γ (PI3Kγ) is expressed primarily in hematopoietic cells and plays several important roles in immunity. CAY10505  also prevents other α, β, and δ isoforms with IC50 of 0.94, 20, and 20 μM, respectively. CAY10505  significantly inhibits only the unrelated casein kinase 2 (CK2, IC50 = 20 nM). CAY10505  also suppress the phosphorylation of the PI3K substrate PKB/Akt in murine macrophages (IC50 = 228 nM). Oral administration of CAY10505  decreases neutrophil recruitment in mice to an extent that is comparable to that observed in PI3Kγ-deficient mice.

Chemical Information
Molecular Weight 289.28
Formula C14H8FNO3S
CAS Number 1218777-13-9
Solubility (25°C) DMSO 48 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] Claudia Hofmann, et al. PI3K-dependent multiple myeloma cell survival is mediated by the PIK3CA isoform

[2] Sandeep Tyagi, et al. Effect of phosphatidylinositol 3-kinase-γ inhibitor CAY10505 in hypertension, and its associated vascular endothelium dysfunction in rats

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  Catalog
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Keywords: CAY10505 supplier, PI3K, inhibitors, activators


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