Lck Inhibitor|cas:847950-09-8|西域试剂

Lck Inhibitor,99.45%

产品编号：Bellancom-12072| CAS NO：847950-09-8| 分子式：C₃₁H₃₀N₈O| 分子量：530.62

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货号	价格	库存与货期
Bellancom-12072	￥1162.00	杭州北京（现货）
Bellancom-12072	￥1851.00	杭州北京（现货）
Bellancom-12072	￥7403.00	杭州北京（现货）
Bellancom-12072	￥13299.00	杭州北京（现货）

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Lck Inhibitor

产品介绍

Lck Inhibitor 是一种有效的口服活性淋巴细胞特异性激酶 (Lck) 抑制剂，对 Lck，Lyn，Src 和 Syk 激酶的 IC₅₀ 分别为 7、2.1、4.2 和 200 nM。与 MAPK，CDK 和 RSK 家族代表相比，Lck Inhibitor 对 Lck 的选择性高出 1000 倍以上。Lck Inhibitor 抑制 T 细胞增殖和关节炎模型。

生物活性

Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC₅₀s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.

体外研究

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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Lewis rat (adjuvant-inducedarthritis model)
Dosage:	0, 30, and 60 mg/kg
Administration:	P.o.; once daily; from day 9 today 17
Result:	Showed a dose-dependent inhibition of arthritis, with an ED₅₀ estimated at 24 mg/kg.

Animal Model:	Sprague-Dawley Rats
Dosage:	P.o. (Pharmacokinetic Analysis)
Administration:	5 mg/kg
Result:	The C_max, AUC_0-∞, t_max and F% were 82 ng/mL, 862 ng h/mL, and 17%, respectively.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Lewis rat (adjuvant-inducedarthritis model)
Dosage:	0, 30, and 60 mg/kg
Administration:	P.o.; once daily; from day 9 today 17
Result:	Showed a dose-dependent inhibition of arthritis, with an ED₅₀ estimated at 24 mg/kg.

Animal Model:	Sprague-Dawley Rats
Dosage:	P.o. (Pharmacokinetic Analysis)
Administration:	5 mg/kg
Result:	The C_max, AUC_0-∞, t_max and F% were 82 ng/mL, 862 ng h/mL, and 17%, respectively.

性状

Solid

溶解性数据

In Vitro:

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

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8846 mL	9.4229 mL	18.8459 mL
5 mM	0.3769 mL	1.8846 mL	3.7692 mL
10 mM	0.1885 mL	0.9423 mL	1.8846 mL

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

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
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

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。