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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.
| 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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
| Molecular Weight | 289.28 |
| Formula | C14H8FNO3S |
| CAS Number | 1218777-13-9 |
| Purity | >99% |
| Solubility | DMSO 50 mg/mL |
| Storage | at -20°C |
| Related PI3K Products |
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| IPI3063
IPI-3063 is a potent and selective p110δ inhibitor with biochemical IC50 of 2.5 ± 1.2 nM and IC50 values for the other class I PI3K isoforms (p110α, p110β, p110γ) are at least 400-fold higher. |
| GDC-0084
GDC-0084 is a brain penetrant inhibitor of PI3K and mTOR. |
| GNE-317
GNE-317 is a potent, brain-penetrant PI3K inhibitor. |
| Serabelisib
Serabelisib (INK-1117,MLN-1117,TAK-117) is a potent and selective oral PI3Kα isoform inhibitor (IC50 of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinase. |
| SF2523
SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively. |
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