CAS NO: | 1704801-24-0 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | AX-024 hydrochloride is an orally available, first-in-class inhibitor of theTCR-Nckinteraction that selectively inhibits TCR-triggered T cell activation with anIC50~1 nM. AX-024 hydrochloride modulates cell signaling by targetingSH3domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production ofIL-6,TNF-α,IFN-γ,IL-10andIL-17A. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | AX-024 hydrochloride is >10,000-fold more potent than the AX-000 hit in terms of inhibition of TCR-triggered T cell proliferation. The IC50of AX-024 hydrochloride in this assay is 1 nM, although it shows inhibitory effects at a concentration of 1 pM or less. AX-024 hydrochloride is also a much more potent inhibitor of cytokine release by human peripheral blood mononuclear cells stimulated with anti-CD3 than AX-000, strongly hindering interleukin-6 (IL-6), tumor necrosis factor-α (TNFα), interferon-γ (IFN-γ), IL-10, and IL-17A production at a concentration of 10 nM. In CD8+T cells of OT1 TCR transgenic (OT1Tg) mice bearing wild-type (WT) AX-024 hydrochloride strongly inhibits T cell proliferation at a concentration of 0.1 nM when OT1TgT cells are WT for the PRS mutation. Coimmunoprecipitation experiments in these cells show that Nck recruitment to the TCR is induced upon stimulation in the absence of drug but is inhibited in the presence of AX-024 hydrochloride in a dose-dependent manner at concentrations starting from 1 nM[1]. | ||||||||||||||||
体内研究 (In Vivo) | The AX-024 hydrochloride-treated group presents less scales and reduces skin thickening compare to the vehicle group. AX-024 hydrochloride significantly reduces thickening of both skin layers, but more effectively of the dermis, which rather resembles that of mice treated with a control cream lacking imiquimod (IMQ). AX-024 hydrochloride significantly diminishes the number of airway inflammatory cells in both assays. Mice receiving AX-024 hydrochloride rapidly recovers from neurological impairment and weight loss, becoming symptom-free by day 30, unlike mice that receives the vehicle, in which ataxia and loss of the righting reflex persist[1]. | ||||||||||||||||
分子量 | 375.86 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C21H23ClFNO2 | ||||||||||||||||
CAS 号 | 1704801-24-0 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 33 mg/mL(87.80 mM;Need ultrasonic and warming) H2O : 16.67 mg/mL(44.35 mM;Need ultrasonic) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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