| Bioactivity | Emavusertib (CA-4948) is a potent IRAK4/FLT3 inhibtor with anti-tumor activity[1]. | ||||||||||||
| Invitro | Emavusertib (CA-4948) is over 500-fold more selective for IRAK-4 compared to IRAK-1. Emavusertib reduces TNF-α, IL-1β, IL-6 and IL-8 release from TLR-Stimulated THP-1 Cells with an IC50 <250 nM. Emavusertib also has antiproliferative activity due to inhibition of receptor-type tyrosine-protein kinase FLT3[1]. | ||||||||||||
| In Vivo | Emavusertib (CA-4948) shows anti-tumor activity in animal models including tumors containing MyD88 gene mutations. Emavusertib shows antileukemic activity in mouse models of FLT3 wild-type and FLT3 mutated acute myeloid leukemia (AML)[1]. | ||||||||||||
| Name | Emavusertib | ||||||||||||
| CAS | 1801344-14-8 | ||||||||||||
| Formula | C24H25N7O5 | ||||||||||||
| Molar Mass | 491.50 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. Wiese MD, et al. Investigational IRAK-4 inhibitors for the treatment of rheumatoid arthritis. Expert Opin Investig Drugs. 2020 Apr 17:1-8. |