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Linperlisib, also known as YY-20394 and PI3Kδ-IN-2, is a potent and selective PI3Kδ inhibitor. Linperlisib significantly inhibited T cell differentiation into Treg both in mouse splenocyte and in human primary CD4+ T cells, and was especially potent inhibiting their IL-10 secretion in vitro. YY-20394 significantly inhibited primary tumor growth in immune-competent mice with 4T1 and CT26 tumors, as well as 4T1 lung metastasis with dose dependency.
| 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.
| Molecular Weight | 588.69 |
| Formula | C28H37FN6O5S |
| CAS Number | 1702816-75-8 |
| Purity | >99% |
| Solubility | DMSO 50 mg/mL |
| Storage | at -20°C |
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