| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 2mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| Other Sizes |
|
Leptomycin B (NSC-364372; Elactocin; LMB; Mantuamycin) is a potent inhibitor of the nuclear export of proteins-CRM1 and RNA translation with anticancer activity. It inhibits CRM1 with IC50 values ranging from 0.1 to 10 nM against various cancer cell lines.
| ln Vitro |
Leptomycin B (LMB) has IC50 values ranging from 0.1 to 10 nM, making it extremely effective against a wide range of cancer cell types in vitro. After 72 hours of exposure, leptomycin B (LMB) inhibits SiHa, HCT-116, and SKNSH cells with IC50 values of 0.4, 0.3, and 0.4 nM, respectively [2]. In A549 and H460 cell lines, leptomycin B (LMB) (0.5 nM) has a synergistic impact against gefitinib (0–32 μM)-induced cytotoxicity. When gefitinib (0–32 μM) and leptomycin B (0.5 nM) were administered concurrently, A549 displayed synergistic cytotoxic effects at 24 and 48 hours, as opposed to gefitinib alone [3].
|
|---|---|
| ln Vivo |
In vivo, leptomycin B (LMB) is not well tolerated. The maximum tolerated dosage (MTD) of LMB (single intravenous injection) in tumor-bearing HCT-116 mice was 2.5 mg/kg. Leptomycin B's poor in vivo efficacy is caused by off-target effects; in contrast, our nuclear export inhibitors (NEIs) appear to be more well tolerated in vivo while maintaining strong CRM1 inhibition [4].
|
| Cell Assay |
Cell viability assay [3]
Cell Types: Non-small cell lung cancer (NSCLC) cell lines A549 and H460 Tested Concentrations: 0.5 nM Incubation Duration: 24 and 48 hrs (hours) Experimental Results: The IC50 of gefitinib at 48 hrs (hours) is 32.0±2.5 μM, while with After combination with 0.5 nM Leptomycin B, its concentration was Dramatically diminished to 25.0±2.1 μM. The significant synergistic cytotoxic effect of co-treatment of 0.5 nM Leptomycin B with gefitinib was also confirmed in the H460 cell line. Cell viability assay[3] Cell Types: A549 Tested Concentrations: 0.5 nM Incubation Duration: 48 hrs (hours) Experimental Results: 0.5 nM Leptomycin B plus gefitinib or gefitinib alone diminished p-EGFR(Tyr1068) expression compared to control . p-Akt (Ser473) was inhibited by gefitinib treatment in a dose-response manner, but was enhanced by combined gefitinib + linbumycin B treatment compared with gefitinib alone. A549 treated with gefitinib + light mycin B had higher expression of p-Erk1/2 (Thr202/Tyr204) than A549 treated with gefitinib alone. |
| References |
|
| Additional Infomation |
Leptomycin B is a leptomycin having a (2E,10E,12E,16Z,18E)-double bond configuration as well as an ethyl substituent at position 17. It has a role as an antifungal agent and a bacterial metabolite. It is a leptomycin and a hydroxy polyunsaturated fatty acid. It is functionally related to a tetracosanoic acid.
Leptomycin B has been reported in Streptomyces with data available. |
| Molecular Formula |
C33H48O6
|
|---|---|
| Molecular Weight |
540.741
|
| Exact Mass |
540.345
|
| CAS # |
87081-35-4
|
| PubChem CID |
6917907
|
| Appearance |
White to yellow <41°C powder,>44°C liquid
|
| Density |
1.1±0.1 g/cm3
|
| Boiling Point |
725.8±60.0 °C at 760 mmHg
|
| Melting Point |
41-44ºC
|
| Flash Point |
224.8±26.4 °C
|
| Vapour Pressure |
0.0±5.3 mmHg at 25°C
|
| Index of Refraction |
1.542
|
| LogP |
6.66
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
15
|
| Heavy Atom Count |
39
|
| Complexity |
1020
|
| Defined Atom Stereocenter Count |
7
|
| SMILES |
C(/[C@@H]1OC(=O)C=C[C@@H]1C)=C\C(\CC)=C/[C@H](C)C/C=C/C(/C)=C/[C@@H](C)C(=O)[C@@H](C)[C@H](O)[C@@H](C)C/C(/C)=C/C(=O)O
|
| InChi Key |
YACHGFWEQXFSBS-XYERBDPFSA-N
|
| InChi Code |
InChI=1S/C33H48O6/c1-9-28(14-15-29-24(5)13-16-31(36)39-29)19-22(3)12-10-11-21(2)17-25(6)32(37)27(8)33(38)26(7)18-23(4)20-30(34)35/h10-11,13-17,19-20,22,24-27,29,33,38H,9,12,18H2,1-8H3,(H,34,35)/b11-10+,15-14+,21-17+,23-20+,28-19-/t22-,24+,25-,26+,27-,29+,33-/m1/s1
|
| Chemical Name |
(2E,5S,6R,7S,9R,10E,12E,15R,16Z,18E)-17-ethyl-6-hydroxy-3,5,7,9,11,15-hexamethyl-19-[(2S,3S)-3-methyl-6-oxo-2,3-dihydropyran-2-yl]-8-oxononadeca-2,10,12,16,18-pentaenoic acid
|
| Synonyms |
LMB NSC364372Elactocin NSC-364372Leptomycin B
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~184.94 mM)
H2O : < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.62 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8493 mL | 9.2466 mL | 18.4932 mL | |
| 5 mM | 0.3699 mL | 1.8493 mL | 3.6986 mL | |
| 10 mM | 0.1849 mL | 0.9247 mL | 1.8493 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
