Bioactivity | Emavusertib (CA-4948) hydrochloride is a selective, potent and orally active IRAK4/FLT3 inhibitor. Emavusertib hydrochloride has an IC50 of 57 nM for IRAK4 in a FRET kinase assay. Emavusertib hydrochloride shows anti-tumor activity[1][2][3]. |
Invitro | Emavusertib 对 IRAK-4 的结合亲和力比对 IRAK 1、2 和 3 的结合亲和力高出 350 倍以上[3]。Emavusertib (10 μM, 72 h) 可降低边缘区淋巴瘤 (MZL) 细胞系中增殖细胞的百分比并诱导亚 G0 分数适度增加[3]。Emavusertib (10 μM, 72 h) 可诱导 MZL 细胞凋亡细胞群显著增加,尤其是与 Ibrutinib (HY-10997) 联合使用时[3]。 0 --> Emavusertib hydrochloride 相关抗体: |
In Vivo | Emavusertib (25-150 mg/kg,口服,每日一次,连续 14 天)可诱导小鼠肿瘤生长抑制[3]。 Animal Model: |
Name | Emavusertib hydrochloride |
CAS | 2376399-42-5 |
Formula | C24H26ClN7O5 |
Molar Mass | 527.96 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
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. [2]. Guidetti F, et al. Targeting IRAK4 with Emavusertib in Lymphoma Models with Secondary Resistance to PI3K and BTK Inhibitors. J Clin Med. 2023 Jan 4;12(2):399. [3]. Parrondo RD, et al. IRAK-4 inhibition: emavusertib for the treatment of lymphoid and myeloid malignancies. Front Immunol. 2023 Oct 26;14:1239082. |