Lck Inhibitor is a potent, orally activeLck (lymphocyte specific kinase)inhibitor withIC₅₀s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn,SrcandSykkinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK,CDKand RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis^[1].

Lck Inhibitor (compound 25) exhibits good potency in the T-cell receptor-induced IL-2 secretion assay (IL-2, IC₅₀=0.46 μM) and also inhibits subsequent T-cell proliferation (T-cell prolif, IC₅₀=0.53 μM) in the same human T-cells. Lck Inhibitor also inhibits a human mixed lymphocyte reaction (huMLR) with a 10-fold increase in potency as compared to the other invitro cell assays utilizing purified human cells. Lck Inhibitor also displays inhibition of a mechanism-based biochemical cell assay probing Lck-dependent TCR-chain phosphorylation (TCR-chain). Lck Inhibitor shows a 10-fold reduction in potency when IL-2 is induced in a receptor-independent fashion by stimulating with phorbo lester and calcium ionophore (PMA/iono). Lck Inhibitor exhibits a similar level of potency when tested in a general proliferation assay using the human T-cell line, Jurkat (JKT)^[1].

Lck Inhibitor (0-60 mg/kg; p.o.; once daily; from day 9 today 17) shows a dose-dependent inhibition of arthritis^[1].
Lck Inhibitor (p.o.; 5 mg/kg) treatment shows the C_max, AUC_0-∞, t_maxand F% are 82 ng/mL, 862 ng h/mL, and 17%, respectively^[1].

530.62

Solid

C₃₁H₃₀N₈O

847950-09-8

Room temperature in continental US; may vary elsewhere.

DMSO : 100 mg/mL(188.46 mM;Need ultrasonic)

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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

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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• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (4.71 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (4.71 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。