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Lenalidomide

产品编号 T1642 CAS 191732-72-6

别名: 来那度胺, CC-5013

Lenalidomide (CC-5013) 是 Thalidomide 的衍生物，也是具有口服活性免疫调节剂，以分子胶的方式作用。它是泛素 E3 连接酶 cereblon (CRBN) 的配体，可通过 CRBN-CRL4 泛素连接酶对两种淋巴转录因子 IKZF1 和 IKZF3 进行选择性泛素化和降解。

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Lenalidomide, CAS 191732-72-6

规格	价格/CNY	货期
1 mg	￥ 112	现货
5 mg	￥ 226	现货
10 mg	￥ 318	现货
25 mg	￥ 518	现货
50 mg	￥ 759	现货
100 mg	￥ 1,120	现货
200 mg	￥ 1,320	现货
500 mg	￥ 1,630	现货
1 g	￥ 2,450	现货
5 g	￥ 4,870	现货
1 mL * 10 mM (in DMSO)	￥ 245	现货

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其他形式的 Lenalidomide:

Lenalidomide hemihydrate
现货

选择批次

纯度: 99.97%

纯度: 99.52%

纯度: 99.5%

纯度: 98%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Lenalidomide (CC-5013) is a potent inhibitor of TNF-α that, at 10 μM, alters gene expression and cell viability in a range of cancer cell lines.
靶点活性	TNF-α:13 nM
体外活性	Lenalidomide significantly inhibited the proliferation of NSCLC cells (Lu-99, H1299, H460 and A549) in a concentration-dependent manner. In particular, H460 cells had the highest sensitivity for lenalidomide. 3-fold more mRNAs were downregulated (474 mRNAs) than upregulated (158 mRNAs) by lenalidomide (10 μM) treatment in H460 cells [1]. The ubiquitously expressed E3 ligase protein cereblon (CRBN) mediated antiproliferative activities of lenalidomide in myeloma cells, as well as lenalidomide-induced cytokine production in T cells. Lenalidomide inhibited autoubiquitination of CRBN in HEK293T cells expressing thalidomide-binding competent wild-type CRBN, but not thalidomide-binding defective CRBN(YW/AA) [2].
体内活性	Doses of 15 mg/kg IV, 22.5 mg/kg IP, and 45 mg/kg PO lenalidomide caused no observable toxicity up to 24 h postdose. Administration of 0.5 and 10 mg/kg resulted in systemic bioavailability ranges of 90-105% and 60-75% via IP and oral routes, respectively. Lenalidomide was detectable in the brain only after IV dosing of 5 and 10 mg/kg [3]. Oral administration of lenalidomide attenuates growth factor-induced angiogenesis in vivo; the rat mesenteric window assay was utilized to show that lenalidomide significantly inhibits vascularization in a dose-dependent manner [4].
细胞实验	The human NSCLC cell lines Lu-99, H1299, A549, EBC1, and H460 were cultured in RPMI-1640 medium containing 10% fetal bovine serum and antibiotics at 37°C in a humidified chamber containing 5% CO2. Cells were seeded into 60-mm culture dishes (2x10^5 cells per dish) with various concentrations of lenalidomide and incubated for various times [1].
动物实验	Mice were administered sterile preparations of lenalidomide normalized to body weight. Intravenously (IV) dosed animals received drug by bolus tail vein injections, and extravascularly dosed mice received drug by bolus intraperitoneal injections (IP) or oral gavage (PO). Dosing solution, concentrations were adjusted so dose volumes ranged between approximately 100 and 150 μL for IV injections and between approximately 150 and 250 μL for IP and PO dosing in the pharmacokinetic study. However, for the range-finding study, increased dose volumes were used (up to 200 μL IV, 300 μL IP, and 600 μL PO, per approved animal use protocol) to explore elevated lenalidomide doses. The bolus injection rates for all IV, IP, or PO injections were less than 5 s. Concentrations of dosing solutions were verified by liquid chromatography-mass spectrometry [4].

别名	来那度胺, CC-5013
分子量	259.26
分子式	C13H13N3O3
CAS No.	191732-72-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 25.9 mg/mL(100 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.8571 mL	19.2857 mL	38.5713 mL	96.4283 mL
	5 mM	0.7714 mL	3.8571 mL	7.7143 mL	19.2857 mL
	10 mM	0.3857 mL	1.9286 mL	3.8571 mL	9.6428 mL
	20 mM	0.1929 mL	0.9643 mL	1.9286 mL	4.8214 mL
	50 mM	0.0771 mL	0.3857 mL	0.7714 mL	1.9286 mL
	100 mM	0.0386 mL	0.1929 mL	0.3857 mL	0.9643 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Kim K, et al. Lenalidomide induces apoptosis and alters gene expression in non-small cell lung cancer cells. Oncol Lett. 2013 Feb;5(2):588-592. 2. Lopez-Girona A, et al. Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide. Leukemia. 2012 Nov;26(11):2326-35. 3. Rozewski DM, et al. Pharmacokinetics and tissue disposition of lenalidomide in mice. AAPS J. 2012 Dec;14(4):872-82. 4. Dredge K, et al. Orally administered lenalidomide (CC-5013) is anti-angiogenic in vivo and inhibits endothelial cell migration and Akt phosphorylation in vitro. Microvasc Res. 2005 Jan;69(1-2):56-63. 6. Nagashima, Takeyuki, et al. PHARMACEUTICAL COMPOSITION COMPRISING BICYCLIC NITROGEN-CONTAINING AROMATIC HETEROCYCLIC AMIDE COMPOUND AS ACTIVE INGREDIENT. Patent. 20170360780A1.

文献引用

1. Durbin A D, Wang T, Wimalasena V K, et al. EP300 Selectively Controls the Enhancer Landscape of MYCN-Amplified NeuroblastomaEP300 Controls Enhancers and MYCN in Neuroblastoma. Cancer Discovery. 2022-12 (3) P730

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Lenalidomide 191732-72-6 Apoptosis PROTAC TNF Ligand for E3 Ligase Molecular Glues myeloma Inhibitor CRL4 ligase IKZF1 Ligands for E3 Ligase E3 ligase-recruiting Moiety immunomodulatory cereblon analog multiple CC5013 inhibit ligand CC 5013 IKZF3 来那度胺 degradation CC-5013 inhibitor

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Lenalidomide

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords