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KPT330,(E)-

KPT330,(E)-

产品编号 T1844   CAS 1421923-86-5
别名: (E)-RN, KPT-330, KPT330, KPT 330

(E)-RN (KPT 330) 是一种 CRM1 选择性核输出抑制剂。它抑制细胞核中的蛋白质运输并诱导间皮瘤细胞中的细胞周期停滞和凋亡

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KPT330,(E)- Chemical Structure
KPT330,(E)-, CAS 1421923-86-5
规格 价格/CNY 货期 数量
1 mg ¥ 262 现货
2 mg ¥ 472 现货
5 mg ¥ 703 现货
10 mg ¥ 903 现货
25 mg ¥ 1,920 现货
50 mg ¥ 3,450 现货
100 mg ¥ 4,910 现货
500 mg ¥ 10,500 现货
1 mL * 10 mM (in DMSO) ¥ 818 现货
其他形式的 KPT330,(E)-:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: KPT330,(E)- (T1844)
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纯度: 99.26%
纯度: 99.03%
纯度: 98.69%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 (E)-RN (KPT 330) is a CRM1-selective inhibitor of nuclear export. It inhibits protein trafficking from the nucleus and induces cell cycle arrest and apoptosis in mesothelioma cells.
体外活性 As the Clinicalal candidate analog of KPT-185, KPT-330 exhibits similar effects on the viability of T-ALL cells and elicits rapid apoptotic response. KPT-330 also reduces cell growth in MOLT-4, Jurkat, HBP-ALL, KOPTK-1, SKW-3, and DND-41 cell lines, with IC50 values of 34-203 nM. [1]
激酶实验 KiNativ profiling of XMD8-92 is carried out with both an ATP and ADP acylphosphate-desthiobiotin with the following modifications. HeLa cell lysates (5 mg/mL total protein) are incubated in the presence of XMD8-92 at 50 μM, 10 μM, 2 μM, 0.8 μM, and 0 μM for 15 minutes prior to addition of the ATP or ADP acylphosphate probe (5 μM final probe concentration). All reactions are performed in duplicate. Probe reactions proceeded for 10 minutes and the reaction stopped by the addition of urea and processed for MS analysis. Samples are analyzed by LC-MS/MS on a linear ion trap mass spectrometer using a time segmented "target list" designed to collect MS/MS spectra from all kinase peptide-probe conjugates that can be detected in HeLa cell lysates. This target list is generated and validated by prior exhaustive analysis of HeLa lysates. Up to four characteristic fragment ions for each kinase peptide-probe conjugate are used to extract signals for each kinase, and a comparison of inhibitor treated to control (untreated) lysates allow for precise determination of % inhibition at each point. A manuscript describing the details of this targeted mass spectrometry approach is in preparation[1].
细胞实验 Cell lines are cultured in RPMI 1640 medium, supplemented with 10% fetal bovine serum and penicillin/streptomycin. Cell Titer Glo assay is used to assess cell viability upon treatment with either dimethyl sulfoxide (DMSO) or KPT-330. Cells are plated at a density of 10 000 cells per well in a 96-well plate and incubated with DMSO or increasing concentrations of KPT-330. The cell viability is measured after 72 h exposure to KPT-330 and reported as a percentage of DMSO control cells. Jurkat cells that overexpress BCL2 are generated using MSCV-IRES-GFP retroviral expression system. Jurkat cells infected with BCL2 or control vector viruses are sorted by flow cytometry and the expression of BCL2 confirmed by Western blot analysis using BCL2 antibody.(Only for Reference)
别名 (E)-RN, KPT-330, KPT330, KPT 330
分子量 443.31
分子式 C17H11F6N7O
CAS No. 1421923-86-5

存储

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

溶解度

DMSO: 4.43 mg/mL (10 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 2.2558 mL 11.2788 mL 22.5576 mL 56.3939 mL
5 mM 0.4512 mL 2.2558 mL 4.5115 mL 11.2788 mL
10 mM 0.2256 mL 1.1279 mL 2.2558 mL 5.6394 mL

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TargetMol Library Books参考文献

1. Etchin J, et al. Br J Haematol. 2013, 161(1), 117-127. 2. Tai YT, et al. Leukemia. 2014, 28(1), 155-165.

TargetMol Library Books文献引用

1. Yuan M, Hu W, Feng Y, et al. Development and validation of an LC–MS/MS method for simultaneous determination of remdesivir and its hydrolyzed metabolite and nucleoside, and its application in a pharmacokinetic study of normal and diabetic nephropathy mice. Biomedical Chromatography. 2022: e5380 2. Yuan M, Hu W, Feng Y, et al. Development and validation of a LC‐MS/MS method for simultaneous determination of remdesivir and its hydrolyzed metabolite and nucleoside, and its application in a pharmacokinetic study of normal and diabetic nephropathy mice. Biomedical Chromatography. 2022: e5380
CRM1-IN-1 KPT185 Verdinexor CRM1-IN-2 Leptomycin A Selinexor (KPT-330) KPT276 LFS-1107

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌活性化合物库 抗癌临床化合物库 抑制剂库 膜蛋白靶向化合物库 抗癌上市药物库 药物功能重定位化合物库 已知活性化合物库 经典已知活性库 离子通道库

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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。

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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

KPT330,(E)- 1421923-86-5 Membrane transporter/Ion channel Others CRM1 KPT330, RN (E)-RN KPT-330,(E)- KPT-330 KPT330 KPT330,(E) KPT 330 Inhibitor inhibitor inhibit

 

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