IRAK4-IN-7 (CA-4948) is a selective, potent and orally active inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4) that regulates IRAK4 function in the TLR and IL-1R signaling cascades.
In vitro, IRAK4-IN-7 (CA-4948) blocked downstream NF-κB pathway signaling, including secretion of proinflammatory cytokines, in Toll-like receptor stimulated THP1 leukemic cells.
In vivo: IRAK4-IN-7 (CA-4948) exhibits favorable DMPK properties, oral bioavailability, and is well tolerated in mice. Furthermore, IRAK4-IN-7 was previously shown to exhibit dose-dependent efficacy in ABC-DLBCL MYD88-L265P xenograft tumor models using cell lines OCI-LY3 and OCI-Ly10 and patient-derived tumors. Drug treatment led to decreased viability of MDS/AML stem cells (CD34+/CD38-/Lin-ve) in vivo studies using a THP1 leukemia xenograft model in NSG mice.
Cell Experiment | |
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Cell lines | |
Preparation method | |
Concentrations | |
Incubation time |
Animal Experiment | |
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Animal models | SCID Beige mice |
Formulation | |
Dosages | 50 mg/kg |
Administration | p.o. |
Molecular Weight | 417.42 |
Formula | C21H19N7O3 |
CAS Number | 1801343-74-7 |
Solubility (25°C) | DMSO ≥ 10 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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.
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