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Lck Inhibitor

Lck抑制剂，Lck Inhibitor是新型的Lck抑制剂，IC50为7 nM。

目录号: PC16038 纯度: ≥98%

CAS No. :847950-09-8

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中文名称

Lck Inhibitor

中文别名

6-(2,6-二甲基苯基)-2-[[4-(4-甲基-1-哌嗪基)苯基]氨基]-嘧啶并[5',4':5,6]嘧啶并[1,2-A]苯并咪唑-5(6H)-酮

英文名称

Lck Inhibitor

英文别名

Pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-one, 6-(2,6-dimethylphenyl)-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-;6-(2,6-Dimethylphenyl)-2-{[4-(4-methyl-1-piperazinyl)phenyl]amino }pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-one;PYRIMIDO[5',4':5,6]PYRIMIDO[1,2-A]BENZIMIDAZOL-5(6H)-ONE, 6-(2,6-DIMETHYLPHENYL)-2-[[4-(4-METHYL-1-PIPERAZINYL)PHENYL]A...;TC-S 7003

Cas No.

847950-09-8

分子式

C₃₁N₈OH₃₀

分子量

530.62

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

性状

Solid

体外研究(In Vitro)

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).

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

体内研究(In Vivo)

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.

Medlife 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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Martin, Matthew W.; Newcomb, John; Nunes, Joseph J.; et al. Structure-Based Design of Novel 2-Amino-6-phenyl-pyrimido[5,4:5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as Potent and Orally Active Inhibitors of Lymphocyte Specific Kinase (Lck): Synthesis, S [Information]

[2]. Liew, Chin Y.; Ma, Xiao H.; Liu, Xianghui; Yap, Chun W. SVM Model for Virtual Screening of Lck Inhibitors. Journal of Chemical Information and Modeling (2009), 49(4), 877-885. [Information]

溶解度数据

体外研究:

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

配制储备溶液

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 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 ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 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。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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