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 | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| 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.
| Related IRAK Products |
|---|
| 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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