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ARQ 531

CAS No. : 2095393-15-8

MCE 站：ARQ 531

产品活性：ARQ 531 (MK-1026) 是 BTK 可逆的、非共价的、具有口服活性的抑制剂，其对 WT-BTK 和 C481S-BTK 的 IC₅₀ 值分别为 0.85 nM 和 0.39 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Btk

In Vitro: ARQ 531 shows strong target inhibition in TMD8 cell line. The IC₅₀ values are 0.85 nM ａnd 0.39 nM for WT-BTK ａnd C481S-BTK, respectively, in biochemical assay. Additionally, ARQ 531 also shows strong inhibition of TEK kinases with IC₅₀s of 5.23 nM (BMX), 5.80 nM (TEC), 36.4 nM (TXK). The IC₅₀s of ARQ 531 for SRC kinases are 3.86 nM (LCK), 4.22 nM (YES), 9.71 nM (BLK), 18.3 nM (HCK), 18.8 nM (LYNa), 25.9 nM (FGR), 32.2 nM (FYN), 48.0 nM (FRK) ａnd for TRK kinases are 11.7 nM (TrkB), 13.1 nM (TrkA), 19.1 nM (TrkC). ARQ 531 inhibits proliferation of diverse types of cell lines (TMD8: GI₅₀=0.13 μM, REC1: GI₅₀=0.18 nM) ａnd shows potency in cell lines that are addict to BCR, Src-family kinase ａnd PI3K/AKT pathways.

In Vivo: ARQ 531 is efficacious in TMD-8 tumor xenograft model. ARQ 531 causes complete tumor regression after 14 days of treatment. ARQ 531 is also efficacious in collagen induced arthritis model. ARQ 531 demonstrates potent efficacy against arthritis in mouse model. In the BTK driven TMD8 xenograft mouse model, ARQ 531 demonstrates excellent anti-tumor activity with durable response. ARQ 531 demonstrates in vivo efficacy in a mouse collagen-induced arthritis (CIA) model.

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