1. Membrane Transporter/Ion Channel
    Anti-infection
  2. CRM1
    Fungal
    Antibiotic
  3. Leptomycin B

Leptomycin B (Synonyms: CI 940; LMB)

Cat. No.: HY-16909 Purity: 99.68%
Handling Instructions

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.

For research use only. We do not sell to patients.

Leptomycin B Chemical Structure

Leptomycin B Chemical Structure

CAS No. : 87081-35-4

Size Price Stock Quantity
1 mg USD 380 In-stock
Estimated Time of Arrival: December 31
5 mg USD 1280 In-stock
Estimated Time of Arrival: December 31
10 mg USD 2050 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target

CRM1/exportin 1[1]

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[3]

Cell Line: The non-small cell lung cancer (NSCLC) cell lines A549 and H460
Concentration: 0.5 nM
Incubation Time: 24 and 48 hours
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.

Cell Viability Assay[3]

Cell Line: A549
Concentration: 0.5 nM
Incubation Time: 48 hours
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.
In Vivo

Leptomycin B (LMB) is poorly tolerated in vivo. Maximum tolerated dose (MTD) is 2.5 mg/kg for LMB (single i.v.) in HCT-116 tumor–bearing mice.The limited in vivo efficacy of Leptomycin B is due to off-target effects because our nuclear export inhibitors (NEIs) retain the potent inhibition of CRM1, but are clearly better tolerated in vivo[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

540.73

Formula

C33H48O6

CAS No.
SMILES

O=C(O)/C=C(C)/C[[email protected]](C)[[email protected]@H](O)[[email protected]](C)C([[email protected]](C)/C=C(C)/C=C/C[[email protected]@H](C)/C=C(CC)\C=C\[[email protected]]1[[email protected]@H](C)C=CC(O1)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (184.94 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8494 mL 9.2468 mL 18.4935 mL
5 mM 0.3699 mL 1.8494 mL 3.6987 mL
10 mM 0.1849 mL 0.9247 mL 1.8494 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.62 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.68%

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Leptomycin B
Cat. No.:
HY-16909
Quantity:
MCE Japan Authorized Agent: