货号	规格	价格	上海	北京	珠海	重庆	武汉
S84422-1mg买3赠1	97.40%	￥348.00 S84422-1mg ￥348.00 现货（买3赠1）	9 9	-	-	-	-
S84422-5mg促销	97.40%	￥1120.00 ￥896.00 S84422-5mg ￥896.00 现货	8 8	-	-	-	-
S84422-25mg促销	97.40%	￥3180.00 ￥2540.00 S84422-25mg ￥2540.00 现货	7 7	-	-	-	-

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产品描述：

RK-24466 (KIN 001-51) is a potent and selective Lck inhibitor; inhibits Lck (64-509) and LckCD isoforms with IC50s of less than 1 and 2 nM, respectively.

靶点：

IC50: <1 nM (Lck (64-509)), 2 nM (LckCD);Src

体内研究：

RK-24466 inhibits T-cell receptor stimulated (a-CD3 mAb) IL-2 production in mice at low doses (ED50=4 mg/kg) after ip administration. However, efficacy is greatly reduced after oral administration (ED50=25 mg/kg) which is presumed to reflect poor intestinal absorption in the latter regimen. Inhibition of antigen specific T-cell immune responses is also seen for RK-24466. After administration of RK-24466 twice daily (100 mg/kg po) for 3 days during the in vivo priming phase, a 70% inhibition of IFNγ production is seen upon subsequent antigen-specific (KLH) challenge of lymphocytes from the draining lymph nodes in vitro. RK-24466 suppresses the migration of VSMCs from endothelium-removed aortic rings, as well as neointima formation following rat carotid balloon injury

参考文献：

1. Arnold LD, et al. Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I. Bioorg Med Chem Lett. 2000 Oct 2;10(19):2167-70. 2. Seo HH, et al. 7-cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d] pyrimidin-4-ylamine inhibits the proliferation and migration of vascular smooth muscle cells by suppressing ERK and Akt pathways. Eur J Pharmacol. 2017 Mar 5;798:35-42. 3. Burchat AF, et al. Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitorsof lck II. Bioorg Med Chem Lett. 2000 Oct 2;10(19):2171-4.

溶解性：

DMSO : 45 mg/mL (121.47 mM; Need ultrasonic)

保存条件：

2-8℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.699 ml	13.497 ml	26.994 ml
5 mM	0.54 ml	2.699 ml	5.399 ml
10 mM	0.27 ml	1.35 ml	2.699 ml
50 mM	0.054 ml	0.27 ml	0.54 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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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

RK-24466 (KIN 001-51)

7-CYCLOPENTYL-5-(4-PHENOXY)PHENYL-7H-PYR

参考文献

质检证书(COA)

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)