PF06650833 is an inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4). IRAK4 kinase is important in innate immunity, involved in initiating signaling from Toll-like receptors and members of th einterleukin-1 receptor family. IRAK4 kinase is an attractive target for the treatment of various diseases associated with deregulated inflammation, such as rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, and systemic lupus erythematosus. PF06650833 has been investigated for treatment of lupus.
| Molecular Weight | 361.37 |
| Formula | C18H20FN3O4 |
| CAS Number | 1817626-54-2 |
| Solubility (25°C) | DMSO ≥ 20 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.
| Related IRAK Products |
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| BIO-7488
BIO-7488 is a potent, selective, oral active and CNS-penetrant IRAK4 inhibitor, with IC50 values of 0.6 nM and >30 μM for IRAK4 and hERG, respectively. |
| IRAK4-IN-22
IRAK4-IN-22 is an orally potent and selective potent IRAK4 inhibitor with IC50 values of 3 and 17 nM for IRAK4 and TAK1, respectively.In addition, IRAK4-IN-21 potently inhibits the production of IL-23 (IC50=0.10 µM), which may be useful in studies related to autoimmune diseases such as plaque psoriasis and psoriasis vulgaris. arthritis). |
| HS271
HS271 is an orally potent and selective IRAK4 inhibitor with an IC50 value of 7.2 μM. In addition, HS271 has superior in vitro enzymatic and cellular activities. |
| PROTAC IRAK4 degrader-3
PROTAC IRAK4 degrader-3 is a von Hippel-Lindau based IRAK4 degrader PROTAC. |
| IRAK inhibitor 4 (trans)
IRAK inhibitor 4 (trans) is the trans form of IRAK inhibitor 4 and a potent inhibitor of IRAK4. |
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