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

LP-261 

Cat. No.: HY-14389
Handling Instructions

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
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 99 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
25 mg USD 250 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 750 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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].

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

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].

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.
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)

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
10 mM 0.2373 mL 1.1863 mL 2.3726 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

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

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

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

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LP-261
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HY-14389
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