[CAS NO. 87081-35-4] LeptomycinB
PRODUCTS SPECIFICATIONS [87081-35-4]
DESCRIPTION [87081-35-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 540.73 |
| Molecular Formula | C33H48O6 |
| 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 |
4 Publications Citing Use of MCE
Summary
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 IC
50
s 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 IC 50 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.
Appearance
<41°C Solid,>44°C Liquid
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
DMSO : 100 mg/mL ( 184.94 mM ; Need ultrasonic)
H 2 O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
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 |
Synonyms