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KPT330,(E)-

Catalog No. T1844   CAS 1421923-86-5
Synonyms: (E)-RN, KPT-330, KPT330, KPT 330

(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.

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KPT330,(E)- Chemical Structure
KPT330,(E)-, CAS 1421923-86-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 35.00
2 mg In stock $ 48.00
5 mg In stock $ 72.00
10 mg In stock $ 93.00
25 mg In stock $ 198.00
50 mg In stock $ 357.00
100 mg In stock $ 529.00
1 mL * 10 mM (in DMSO) In stock $ 98.00
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Purity: 99.26%
Purity: 99.03%
Purity: 98.69%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description (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.
In vitro 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]
Kinase Assay 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].
Cell Research 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)
Synonyms (E)-RN, KPT-330, KPT330, KPT 330
Molecular Weight 443.31
Formula C17H11F6N7O
CAS No. 1421923-86-5

Storage

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

Solubility Information

DMSO: 4.43 mg/mL (10 mM)

TargetMolReferences and Literature

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

TargetMolCitations

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

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Clinical Compound Library Inhibitor Library Bioactive Compounds Library Max Ion Channel Inhibitor Library Preclinical Compound Library FDA-Approved & Pharmacopeia Drug Library

Related Products

Related compounds with same targets
CRM1-IN-1 KPT185 CRM1-IN-2 Verdinexor Leptomycin A Selinexor (KPT-330) LFS-1107 KPT276

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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 inhibit

 

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