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產(chǎn)品簡介 品牌 MedChemExpress (MCE) 貨號 HY-112215 規(guī)格 10 mM * 1 mL；5 mg；10 mg 供貨周期 現(xiàn)貨 應(yīng)用領(lǐng)域 生物產(chǎn)業(yè)     ARQ 531 是 BTK 可逆的非共價抑制劑，其對 WT-BTK 和 C481S-BTK 的 IC50 值分別為 0.85 nM 和 0.39 nM。
詳細介紹 ARQ 531

產(chǎn)品活性：ARQ 531 是 BTK 可逆的非共價抑制劑，其對 WT-BTK 和 C481S-BTK 的 IC50 值分別為 0.85 nM 和 0.39 nM。

研究領(lǐng)域：Protein Tyrosine Kinase/RTK

作用靶點：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=1.7 nM, REC1: GI50=0.55 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.

相關(guān)產(chǎn)品：Kinase Inhibitor Library | Covalent Screening Library | Clinical Compound Library | Clinical Compound Library Plus | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Bioactive Compound Library Plus | Ibrutinib | Acalabrutinib | Fenebrutinib | Evobrutinib | Ibrutinib-biotin | Tirabrutinib | ( )-Zanubrutinib | Spebrutinib | GDC-0834 | Vecabrutinib | BMX-IN-1 | BTK IN-1 | CGI-1746 | RN486 | PRN1008 | BMS-986195 | CNX-774 | PCI-33380 | QL47 | BMS-986142 | BMS-935177 | LFM-A13 | CG-806 | Btk inhibitor 2 | PCI 29732

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