Leptomycin B
Based on 24 publication(s) in Google Scholar
Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle.
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- Pureté: 99.79%
- CAS No.: 87081-35-4
- Formule: C33H48O6
- Masse moléculaire:540.73
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Stockage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Leptomycin B
More- Nat Aging. 2026 Jun;6(6):1208-1226. [Abstract]
- Adv Sci (Weinh). 2025 Aug 11:e04896. [Abstract]
- Adv Sci (Weinh). 2025 May 8:e2501552. [Abstract]
- J Adv Res. 2025 Jun 2:S2090-1232(25)00374-1. [Abstract]
- Sci China Life Sci. 2025 Jun 20. [Abstract]
- Emerg Microbes Infect. 2024 Aug 1:2387910. [Abstract]
- Cell Death Discov. 2024 Oct 26;10(1):453. [Abstract]
- Cell Death Discov. 2023 Jun 29;9(1):199. [Abstract]
- Clin Transl Med. 2023 Dec;13(12):e1494. [Abstract]
- Gastric Cancer. 2025 Sep;28(5):837-851. [Abstract]
- Int J Mol Sci. 2025 Jun 3;26(11):5358. [Abstract]
- Eur J Cell Biol. 2026 Apr 17;105(3):151540. [Abstract]
- iScience. 2024 Jun 4;27(7):110144. [Abstract]
- J Virol. 2025 May 30:e0058425. [Abstract]
- PLoS Genet. 2025 Jul 10;21(7):e1011794. [Abstract]
- Mol Med Rep. 2021 Jun;23(6):454. [Abstract]
- J Immunol. 2021 Jun 1;206(11):2623-2637. [Abstract]
- Biochem Biophys Res Commun. 2025 Jun 30:767:151899. [Abstract]
- Biochem Biophys Res Commun. 2024 Nov 19:734:150740. [Abstract]
- Mutat Res. 2026 Feb 6:832:111929. [Abstract]
- bioRxiv. 2026 Jan 2.
- Technical University of Munich. 2025.
- Research Square Print. November 29th, 2022.
- Research Square Print. November 29th, 2022.
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Activité biologique
CRM1/exportin 1[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.3 nM
Compound: LMB
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Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 1 hrs by CellTiter Glo assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 1 hrs by CellTiter Glo assay
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[PMID: 38105606] |
| HCT-116 | IC50 |
0.3 nM
Compound: LMB
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Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter Glo assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter Glo assay
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[PMID: 38105606] |
| HeLa | EC50 |
0.00822 μM
Compound: Leptomycin B
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Inhibition of HIV1 Rev expressed in human HeLa cells co-expressing renilla luciferase reporter gene assessed as inhibition of renilla luciferase expression after 24 hrs
Inhibition of HIV1 Rev expressed in human HeLa cells co-expressing renilla luciferase reporter gene assessed as inhibition of renilla luciferase expression after 24 hrs
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[PMID: 18625767] |
| HeLa | IC50 |
1 nM
Compound: 128; LMB
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Inhibition of CRM1-mediated nucleocytoplasmic transport in human HeLa cells after 90 mins by immunofluorescence assay
Inhibition of CRM1-mediated nucleocytoplasmic transport in human HeLa cells after 90 mins by immunofluorescence assay
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[PMID: 27996267] |
| MDCK | CC50 |
>0.88 μM
Compound: LMB
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Cytotoxicity against MDCK cells assessed as cell death after 72 hrs by MTT assay
Cytotoxicity against MDCK cells assessed as cell death after 72 hrs by MTT assay
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[PMID: 30753063] |
| SiHa | IC50 |
0.3 nM
Compound: LMB
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Antiproliferative activity against human SiHa cells assessed as inhibition of cell growth incubated for 1 hrs by CellTiter Glo assay
Antiproliferative activity against human SiHa cells assessed as inhibition of cell growth incubated for 1 hrs by CellTiter Glo assay
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[PMID: 38105606] |
| SiHa | IC50 |
0.3 nM
Compound: LMB
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Antiproliferative activity against human SiHa cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter Glo assay
Antiproliferative activity against human SiHa cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter Glo assay
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[PMID: 38105606] |
| SK-N-SH | IC50 |
0.3 nM
Compound: LMB
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Antiproliferative activity against human SK-N-SH cells assessed as inhibition of cell growth incubated for 1 hrs by CellTiter Glo assay
Antiproliferative activity against human SK-N-SH cells assessed as inhibition of cell growth incubated for 1 hrs by CellTiter Glo assay
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[PMID: 38105606] |
| SK-N-SH | IC50 |
0.3 nM
Compound: LMB
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Antiproliferative activity against human SK-N-SH cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter Glo assay
Antiproliferative activity against human SK-N-SH cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter Glo assay
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[PMID: 38105606] |
Leptomycin B (LMB) is very potent in vitro against various cancer cell lines (IC50 values in the 0.1 to 10 nM range). Leptomycin B (LMB) inhibits SiHa, HCT-116, and SKNSH cells with IC50s of 0.4, 0.3 and 0.4 nM for a 72 hour exposure, respectively[2].
Leptomycin B (LMB) (0.5 nM) displays a synergistic effect on Gefitinib (0–32 μM)-induced cytotoxicity in A549 and H460 cell line. The simultaneous treatments of Gefitinib (0–32 μM) and Leptomycin B (0.5 nM) show synergistic cytotoxic effect on A549 as compared to Gefitinib alone at both 24 and 48 hours[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:The non-small cell lung cancer (NSCLC) cell lines A549 and H460
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Concentration:0.5 nM
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Incubation Time:24 and 48 hours
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Result:The IC50 of Gefitinib at 48 hours was 32.0±2.5 μM while it was significantly reduced to 25.0±2.1 μM with the combination of 0.5 nM Leptomycin B. The significant synergistic cytotoxic effect from co-treatment of 0.5 nM Leptomycin B with Gefitinib was also confirmed in H460 cell line.
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Cell Line:A549
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Concentration:0.5 nM
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Incubation Time:48 hours
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Result:0.5 nM Leptomycin B plus Gefitinib or Gefitinib alone had a decreased p-EGFR(Tyr1068) expressions compared with controls.
p-Akt (Ser473) was inhibited in a dose-response manner by Gefitinib treatments, but it was enhanced by gefitinib+Leptomycin B co-treatments compared with gefitinib alone.
A549 treated by Gefitinib+Leptomycin B had a higher expression of p-Erk1/2(Thr202/Tyr204) than A549 treated by Gefitinib alone.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 87081-35-4
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Appearance <41°C Solid,>44°C Liquid
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Masse moléculaire 540.73
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Formule C33H48O6
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Color White to yellow
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SMILES
O=C(O)/C=C(C)/C[C@H](C)[C@@H](O)[C@H](C)C([C@H](C)/C=C(C)/C=C/C[C@@H](C)/C=C(CC)\C=C\[C@H]1[C@@H](C)C=CC(O1)=O)=O
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Synonyms
CI 940; LMB
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (24)
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Journal Impact Factor
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Most Recent
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Nat Aging
Nuclear export of R-loop by the DDX1 and XPO1 complex promotes senescence-associated secretory phenotype and inflammaging. [Abstract]2026 Jun;6(6):1208-1226. PMID: 42303864 -
Adv Sci (Weinh)
Lactylation of HMGB1 at K177 Drives Nuclear Export of TIAR to Promote Hypoxia-Induced Stress Granule Formation. [Abstract]2025 Aug 11:e04896. PMID: 40788094 -
Adv Sci (Weinh)
Fn14 Controls the SIRT2-Mediated Deacetylation of Slug to Inhibit the Metastasis of Epithelial Ovarian Cancer. [Abstract]2025 May 8:e2501552. PMID: 40344622 -
J Adv Res
Voxtalisib inhibits enterovirus 71 replication by downregulating host RAN and restoring IFN-STAT signaling. [Abstract]2025 Jun 2:S2090-1232(25)00374-1. PMID: 40466758
Leptomycin B purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Jun 2:S2090-1232(25)00374-1. [Abstract]
Nuclear and cytoplasmic RAN, pSTAT1/2, and STAT1/2RD in RD cells treated with or without voxtalisib (37 °C, 22 h), leptomycin B (10 ng/mL; 4 h), and IFN-α (10 ng/mL).
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Sci China Life Sci
3-Indolepropionic acid confers PXR-p53 binding to mitigate deoxynivalenol-induced hepatocyte apoptosis. [Abstract]2025 Jun 20. PMID: 40553417 -
Emerg Microbes Infect
Inhibition of RAN attenuates influenza a virus replication and nucleoprotein nuclear export. [Abstract]2024 Aug 1:2387910. PMID: 39087696
Leptomycin B purchased from MedChemExpress. Usage Cited in: Emerg Microbes Infect. 2024 Aug 1:2387910. [Abstract]
Cells were fixed and permeabilized at 2 h or 6 h post-infection and then immunostained for NP. Baf-A1 (100 nM) and Leptomycin (10 ng/mL) were used as nuclear import and export inhibition controls, respectively.
Leptomycin B purchased from MedChemExpress. Usage Cited in: Emerg Microbes Infect. 2024 Aug 1:2387910. [Abstract]
A549 cells treated with bepotastine (30 μM) and Leptomycin (10 ng/mL) were infected with the indicated viruses at an MOI of 10.
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Cell Death Discov
CDK4/6 inhibition initiates cell cycle arrest by nuclear translocation of RB and induces a multistep molecular response. [Abstract]2024 Oct 26;10(1):453. PMID: 39461947
Leptomycin B purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2024 Oct 26;10(1):453. [Abstract]
T24 cells were treated with 1µM PD with or without 0.5nM Leptomycin B for 8 h. The subcellular localization of RB and pRB was analyzed using Western blotting.
Leptomycin B purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2024 Oct 26;10(1):453. [Abstract]
T24 cells were treated with PD, IPZ, Leptomycin B (0.5 nM) mono- or combination therapy for 8h. Immunofluorescence staining was used to determine subcellular localization of RB and pRB. The scale bar equaled 20µm.
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Cell Death Discov
MicroRNA-375 restrains the progression of lung squamous cell carcinoma by modulating the ERK pathway via UBE3A-mediated DUSP1 degradation. [Abstract]2023 Jun 29;9(1):199. PMID: 37385985 -
Clin Transl Med
Selective cargo sorting in stem cell-derived small extracellular vesicles: impact on therapeutic efficacy for intervertebral disc degeneration. [Abstract]2023 Dec;13(12):e1494. PMID: 38037469 -
Gastric Cancer
Nuclear export of transmembrane protein PROM2 is specially regulated by CRM1 and affects the sensitivity of ferroptosis in gastric cancer. [Abstract]2025 Sep;28(5):837-851. PMID: 40679705 -
Int J Mol Sci
Lycorine Inhibits Influenza Virus Replication by Affecting Nascent Nucleoporin Nup93 Synthesis. [Abstract]2025 Jun 3;26(11):5358. PMID: 40508167 -
Eur J Cell Biol
MDC1 promotes nuclear localization of Beclin-1 and supports its role in ATM pathway in response to oxidative stress. [Abstract]2026 Apr 17;105(3):151540. PMID: 42013721 -
iScience
2024 Jun 4;27(7):110144. PMID: 38989466 -
J Virol
2025 May 30:e0058425. PMID: 40444991 -
PLoS Genet
2025 Jul 10;21(7):e1011794. PMID: 40638681 -
Mol Med Rep
GTSE1 promotes SNAIL1 degradation by facilitating its nuclear export in hepatocellular carcin oma cells. [Abstract]2021 Jun;23(6):454. PMID: 33880590 -
J Immunol
β-Arrestin 2 Regulates Inflammatory Responses against Mycobacterium tuberculosis Infection through ERK1/2 Signaling. [Abstract]2021 Jun 1;206(11):2623-2637. PMID: 34001657 -
Biochem Biophys Res Commun
2025 Jun 30:767:151899. PMID: 40315567 -
Biochem Biophys Res Commun
Multi-omic analysis revealed the immunological patterns and diagnostic value of exhausted T cell-derived PTTG1 in patients with psoriasis. [Abstract]2024 Nov 19:734:150740. PMID: 39342798 -
Mutat Res
The oncogenic role of U2AF2/HKDC1 cascade in colorectal cancer by promoting cancer cell glycolysis and malignant phenotypes. [Abstract]2026 Feb 6:832:111929. PMID: 41671784 -
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Solvant et solubilité
DMSO : 100 mg/mL (184.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.62 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.62 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. N Kudo, et al. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue in the central conserved region. Proc Natl Acad Sci U S A. 1999 Aug 3;96(16):9112-7. [Content Brief]
[2]. Sarah C Mutka,et al. Identification of nuclear export inhibitors with potent anticancer activity in vivo. Cancer Res. 2009 Jan 15;69(2):510-7. [Content Brief]
[3]. Zhongwei Liu, et al.Leptomycin B reduces primary and acquired resistance of gefitinib in lung cancer cells. Toxicol Appl Pharmacol. 2017 Nov 15;335:16-27. [Content Brief]
[4]. Sarah C Mutka, et al. Identification of nuclear export inhibitors with potent anticancer activity in vivo. Cancer Res. 2009 Jan 15;69(2):510-7. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8494 mL | 9.2468 mL | 18.4935 mL | 46.2338 mL |
| 5 mM | 0.3699 mL | 1.8494 mL | 3.6987 mL | 9.2468 mL | |
| 10 mM | 0.1849 mL | 0.9247 mL | 1.8494 mL | 4.6234 mL | |
| 15 mM | 0.1233 mL | 0.6165 mL | 1.2329 mL | 3.0823 mL | |
| 20 mM | 0.0925 mL | 0.4623 mL | 0.9247 mL | 2.3117 mL | |
| 25 mM | 0.0740 mL | 0.3699 mL | 0.7397 mL | 1.8494 mL | |
| 30 mM | 0.0616 mL | 0.3082 mL | 0.6165 mL | 1.5411 mL | |
| 40 mM | 0.0462 mL | 0.2312 mL | 0.4623 mL | 1.1558 mL | |
| 50 mM | 0.0370 mL | 0.1849 mL | 0.3699 mL | 0.9247 mL | |
| 60 mM | 0.0308 mL | 0.1541 mL | 0.3082 mL | 0.7706 mL | |
| 80 mM | 0.0231 mL | 0.1156 mL | 0.2312 mL | 0.5779 mL | |
| 100 mM | 0.0185 mL | 0.0925 mL | 0.1849 mL | 0.4623 mL |
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