1. Cell Cycle/DNA Damage Cytoskeleton
  2. Kinesin
  3. Litronesib

Litronesib  (Synonyms: LY2523355)

Cat. No.: HY-14846 Purity: 99.48%
COA Handling Instructions

Litronesib (LY2523355) is a selective mitosis-specific kinesin Eg5 inhibitor, with antitumor activity.

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

Litronesib Chemical Structure

Litronesib Chemical Structure

CAS No. : 910634-41-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 149 In-stock
Solution
10 mM * 1 mL in DMSO USD 149 In-stock
Solid
5 mg USD 132 In-stock
10 mg USD 228 In-stock
50 mg USD 840 In-stock
100 mg USD 1440 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Litronesib:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Litronesib

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Litronesib (LY2523355) is a selective mitosis-specific kinesin Eg5 inhibitor, with antitumor activity[1].

IC50 & Target[1]

Eg5

 

In Vitro

Litronesib (LY2523355) is a selective Eg5 inhibitor. Litronesib (25 nM) induces cancer cells to death during mitotic arrest, and this needs sustained activation of spindle-assembly checkpoint (SAC)[1].

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

In Vivo

Litronesib (LY2523355; 1.1, 3.3, 10, and 30 mg/kg, i.v.) shows antitumor activity in a dose-dependently, and causes a dramatic increase in cancer cells immuno-positive for histone H3 phosphorylation in Colo205 xenograft tumors[1].

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

Clinical Trial
Molecular Weight

511.70

Formula

C23H37N5O4S2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)(C)C(N1[C@@](C2=CC=CC=C2)(CNS(CCNCC)(=O)=O)SC(NC(C(C)(C)C)=O)=N1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (97.71 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9543 mL 9.7713 mL 19.5427 mL
5 mM 0.3909 mL 1.9543 mL 3.9085 mL
View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.89 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.89 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 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References
Cell Assay
[1]

Cancer cells are plated in poly-d-lysine coated 96-well plates and incubated overnight. Cells are then treated with indicated concentrations of Litronesib for various time periods. Cells are then fixed with 3.7% formaldehyde in PBS for 45 minutes or 1× Prefer fixative solution for 30 minutes, at room temperature, and permeabilized with cold methanol for 10 minutes and then 0.2% Triton X-100 in PBS for 10 minutes. Cells are washed three times with PBS. Cells are then incubated with 100 μg/mL DNase-free RNase and 10 μg/mL of propidium iodide for 1 hour and scanned for mitotic index (MI) measurement based on DNA condensation as percentage of cells with condensed DNA. For MI based on histone H3 phosphorylation or apoptosis analysis, cells are incubated overnight at 4°C with anti-phospho-histone H3 antibody or anti-phospho-histone H2AX at 1:1,000 dilution with 5% bovine serum albumin (BSA) in PBS, respectively. Cells are washed three times with 0.2% Triton-X 100 in PBS and incubated with Alexa 488 secondary antibody (1:1,000 in PBS-2% BSA) for 60 minutes at room temperature. Cells are washed three times again with PBS and stained for 15 minutes in PBS containing 10 μg/mL propidium iodide and 100 μg/mL RNaseA. The stained cells are scanned with an Acumen Explorer eX3 microplate cytometer. The results are expressed as percentage of cells positive for phospho-histone H3-Ser10 or phospho-histone H2AX[1].

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

Animal Administration
[1]

Primary human-tumor xenograft models are established and maintained in nude mice. Antitumor efficacy in subcutaneous xenograft tumor-bearing mice with 10 mice per treatment group from either established cancer cell lines or fragments of human tumor explants is evaluated as tumor volume by serial caliper measurements and is calculated. The p388 syngeneic tumor model is developed for high-content imaging analysis using female BDF1 mice, weighing 20 to 23 g, which are acclimated in-house for one week before their use in experiments. p388 murine lymphocytic leukemia cells are authenticated by STR assay and maintained in RPMI1640 medium containing 10% FBS. For inoculation, the cells are washed with serum-free medium three times and 1.25 million cells are implanted by intraperitoneal injection into mice. On day 5 after implantation, mice are treated with Litronesib, via either intravenous bolus or intravenous infusion at appropriate doses and durations. Mice are euthanized and the ascitic (intraperitoneal) fluid containing the p388 tumor cells is drawn and analyzed by acumen, flow cytometry, and TUNEL assays for phospho-histone H3, G2-M, and apoptosis. For pharmacokinetic study, the blood samples are collected via cardiac puncture and generated plasma with EDTA and determined Litronesib exposure in the plasma[1].

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

References

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9543 mL 9.7714 mL 19.5427 mL 48.8568 mL
5 mM 0.3909 mL 1.9543 mL 3.9085 mL 9.7714 mL
10 mM 0.1954 mL 0.9771 mL 1.9543 mL 4.8857 mL
15 mM 0.1303 mL 0.6514 mL 1.3028 mL 3.2571 mL
20 mM 0.0977 mL 0.4886 mL 0.9771 mL 2.4428 mL
25 mM 0.0782 mL 0.3909 mL 0.7817 mL 1.9543 mL
30 mM 0.0651 mL 0.3257 mL 0.6514 mL 1.6286 mL
40 mM 0.0489 mL 0.2443 mL 0.4886 mL 1.2214 mL
50 mM 0.0391 mL 0.1954 mL 0.3909 mL 0.9771 mL
60 mM 0.0326 mL 0.1629 mL 0.3257 mL 0.8143 mL
80 mM 0.0244 mL 0.1221 mL 0.2443 mL 0.6107 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Litronesib
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