PROTAC IRAK4 degrader-7 是一种具有口服活性的 PROTAC IRAK4 降解剂 | MedChemExpress (MCE)

KT-474

CAS：2432994-31-3

品牌：MedChemExpress (MCE)

存储条件：Please store the product under the recommended conditions in the Certificate of Analysis.

生物活性： PROTAC IRAK4 degrader-7 (Compound I-417) 是一种具有口服活性的 PROTAC IRAK4 降解剂，具有抗肿瘤活性[1]。

体外：KT-474 (1-100 nM) 抑制 Resiquimod (HY-13740) 诱导和脂多糖 (HY-D1056) 诱导的 PBMC 产生 IL-6 和 IL-8[2] 。 KT-474 (10-100 nM) 抑制 CpG-B 刺激的 B 细胞中 NF-kB 激活 (磷酸化 p65)[2]。 KYM-001 (48-72 h) 在 ABC DLBCL 中抑制细胞周期并诱导细胞凋亡，与 MYD88-WT 细胞系相比，在 MYD88 突变体细胞系中具有优先活性[3]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内：KT-474 (口服) 可在 MYD88 突变 ABC DLBCL 异种移植模型中诱导肿瘤消退[3]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

详情：www.medchemexpress.cn/protac-irak4-degrader-7.html

参考文献：

[1]. Nello Mainolfi, et al. Irak degraders and uses thereof. Patent WO2020113233A1.
[2]. Ackerman L, et al. IRAK4 degrader in hidradenitis suppurativa and atopic dermatitis: a phase 1 trial. Nat Med. 2023 Dec;29(12):3127-3136.
[3]. Joseph F. Kelleher, et al. Abstract LB-272: KYM-001, a first-in-class oral IRAK4 protein degrader, induces tumor regression in xenograft models of MYD88-mutant ABC DLBCL alone and in combination with BTK inhibition. Cancer Res (2019) 79 (13_Supplement): LB-272.