2. Cell Cycle/DNA Damage Cytoskeleton
  3. Microtubule/Tubulin
  4. LP-261

LP-261 is a potent and orally active anti-mitotic agent and shows an inhibition of in vitro tubulin polymerization with an EC50 of 3.2 μM. LP-261 inhibits growth of a human non-small-cell lung tumor (NCI-H522) in vivo and can be used for cancer research.

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

LP-261 Chemical Structure

LP-261 Chemical Structure

CAS No. : 915412-67-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 99 In-stock
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid
5 mg USD 90 In-stock
10 mg USD 150 In-stock
25 mg USD 250 In-stock
50 mg USD 450 In-stock
100 mg USD 750 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

LP-261 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

LP-261 is a potent and orally active anti-mitotic agent and shows an inhibition of in vitro tubulin polymerization with an EC50 of 3.2 μM[1]. LP-261 inhibits growth of a human non-small-cell lung tumor (NCI-H522) in vivo and can be used for cancer research[1].

IC50 & Target

EC50: 3.2 μM (tubulin polymerization)[1]
In Vitro

LP-261 shows potent G2/M block activity in multiple cell lines and exhibits a range of activity from 0.01μM to 0.38 μM across the tested cell lines, the IC50 values for MCF-7, H522, Jurkat, SW-620, BXPC-3, and PC-3 values are 0.01 μM, 0.01 μM, 0.02 μM, 0.05 μM, 0.05μM and 0.07 μM, respectively[1].
LP-261 exhibits low micromolar potency in the tubulin polymerization assay, the EC50 value of LP-261 is 5.0 μM[1]. LP-261 has the ability to compete with colchicine for binding to tubulin in a [3H]colchicine competition binding assay, the EC50 (3.2 μM) for LP-261 to inhibit the binding with a potency similar to that of colchicine itself, and it exhibits a 79% inhibition at a conctration of 30 μM[1].

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

LP-261 Related Antibodies
In Vivo

LP-261 (oral gavage; 4 mg/kg; single dose) displays rapid adsorption by the oral route (Tmax=2.0 h), the terminal half-life of 1.4 h ( 0.2 h indicated a moderate rate of elimination in rat, and the volume of distribution (Vss) is 1.25 L/kg[1].
LP-261 (oral gavage; 15 or 50 mg/kg; twice daily; 28 days) at 50mg/kg results in an approximately tumor volume of 130 mm3 versus 3769 mm3 in the vehicle treated group, this represents a 96% reduction in mean tumor volume. Meanwhile, LP-261 at 15 mg/kg leads to a 41% inhibition after 28 days in this mouse model[1].

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

Animal Model: Human tumor xenograft model (Injected with NCI-H522 human non-small-cell) in NCr-nu mice[1]
Dosage: 15 or 50 mg/kg
Administration: Oral gavage; 15 or 50 mg/kg; twice daily; 28 days
Result: Had potent anti-tumor efficacy at high dosage and exhibited no significant changes in body weights.
Molecular Weight

421.47

Formula

C22H19N3O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CS(=O)(NC1=CC(C(C2=CC(OC)=NC=C2)=O)=CC(C3=CC=CC4=C3C=CN4)=C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (79.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3726 mL 11.8632 mL 23.7265 mL
5 mM 0.4745 mL 2.3726 mL 4.7453 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
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

×
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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.93 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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. 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 2.3726 mL 11.8632 mL 23.7265 mL 59.3162 mL
5 mM 0.4745 mL 2.3726 mL 4.7453 mL 11.8632 mL
10 mM 0.2373 mL 1.1863 mL 2.3726 mL 5.9316 mL
15 mM 0.1582 mL 0.7909 mL 1.5818 mL 3.9544 mL
20 mM 0.1186 mL 0.5932 mL 1.1863 mL 2.9658 mL
25 mM 0.0949 mL 0.4745 mL 0.9491 mL 2.3726 mL
30 mM 0.0791 mL 0.3954 mL 0.7909 mL 1.9772 mL
40 mM 0.0593 mL 0.2966 mL 0.5932 mL 1.4829 mL
50 mM 0.0475 mL 0.2373 mL 0.4745 mL 1.1863 mL
60 mM 0.0395 mL 0.1977 mL 0.3954 mL 0.9886 mL
  • 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.

LP-261 Related Classifications

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.

Keywords:

LP-261915412-67-8LP261LP 261Microtubule/Tubulinanti-mitotictubulin polymerizationNCI-H522cancertumorMCF-7H522JurkatSW-620BXPC-3Inhibitorinhibitorinhibit

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:
LP-261
Cat. No.:
HY-14389
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (251 KB) Français - FR (251 KB) Deutsch - DE (251 KB) Norwegian - NO (251 KB) Español - ES (251 KB) Swedish - SV (251 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.