货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T96915-1ml	10mM in DMSO	￥720.00 T96915-1ml ￥720.00 现货	6 6	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T96915-1ml

10mM in DMSO

￥720.00

产品描述：

BTK抑制剂;BTK Inhibitors;;InformationARQ 531 ARQ 531 is an ATP-competitive tyrosine kinase inhibitor designed to target BTK with an IC50 of 0.85 nM. It also has a distinct kinase selectivity profile with strong inhibitory activity against several key oncogenic drivers from TEC, Trk and Src family kinases.TargetsBTK (Cell-free assay); BRK (Cell-dree); BRK (Cell-free assay); LCK (Cell-free); LCK (Cell-free assay) 29927,0.85 nM; 2.45 nM; 2.45 nM; 3.86 nM; 3.86 nMIn vitroARQ 531 potently inhibited BTK (IC50 = 0.85 nM), the binding potency was accompanied by long residence time (51 min). ARQ 531 selectively inhibits BCR signaling dependent PI3K/AKT/mTOR, Ras/Raf/Erk and Rap-GTPase-Cofilin pathways in TMD8 cells. It potently inhibits proliferation of hematological malignant cell lines both sensitive and resistant to ibrutinib addicted to BCR signaling. Unlike ibrutinib, ARQ 531 suppressed both the upstream activating signals (via inhibition of a select member of Src kinase family) and the downstream signaling pathways (via pAKT and pERK kinases). In GCB-DLBCL cell lines (SUDHL-4 and DOHH-2), ARQ 531 potently suppressed expression of anti-apoptotic c-Myc and BCL6 oncoproteins in a dose dependent fashion, and concomitantly induced apoptotic cleavage of PARP protein.In vivoARQ 531 has potent anti-tumor activity was observed in both ABC-DLBCL and GCB-DLBCL mouse xenograft models. ARQ 531 crosses the blood, brain-barrier. In a single oral dose study of 10mg/kg in monkeys, the bioavailability of ARQ 531 is 72.4% with a Cmax of 9 μM and a half-life greater than 24 hours.Cell Research(from reference)Cell lines：CLL cells Concentrations：0.1 μM, 1.0 μM, or 10.0 μM Incubation Time：72 h

靶点：

IC50: 0.85 nM (WT-BTK), 0.39 nM (C481S-BTK).

体内研究：

Nemtabrutinib 在 TMD-8 肿瘤异种移植模型中有效。Nemtabrutinib 在治疗 14 天后可使肿瘤完全消退。Nemtabrutinib 在胶原诱导的关节炎模型中也有效。Nemtabrutinib 在小鼠模型中显示出强大的抗关节炎功效。在 BTK 驱动的 TMD8 异种移植小鼠模型中，Nemtabrutinib 表现出优异的抗肿瘤活性和持久的疗效。Nemtabrutinib 在小鼠胶原诱导性关节炎 (CIA) 模型中表现出体内疗效。

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.088 ml	10.44 ml	20.88 ml
5 mM	0.418 ml	2.088 ml	4.176 ml
10 mM	0.209 ml	1.044 ml	2.088 ml
50 mM	0.042 ml	0.209 ml	0.418 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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