LP-261 - 10mM in DMSO , CAS No.915412-67-8

CAS: 915412-67-8 Cat. No.: L655070 分子式: C₂₂H₁₉N₃O₄S 分子量: 421.47 PubChem CID: 15603282

グレード＆純度 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

LP-261 is a potent and orally active anti-mitotic agent and shows an inhibition of in vitro tubulin polymerization with an EC 50 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

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 IC 50 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. LP-261 exhibits low micromolar potency in the tubulin polymerization assay, the EC 50 value of LP-261 is 5.0 μM. LP-261 has the ability to compete with colchicine for binding to tubulin in a [ 3 H]colchicine competition binding assay, the EC 50 (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. 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 (T max =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 (V ss ) is 1.25 L/kg . LP-261 (oral gavage; 15 or 50 mg/kg; twice daily; 28 days) at 50mg/kg results in an approximately tumor volume of 130 mm 3 versus 3769 mm 3 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 . 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 NC r-nu mice 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.

IC50& Target:EC50: 3.2 μM (tubulin polymerization)

仕様

仕様と純度

10mM in DMSO

生化学的・生理学的メカニズム

LP-261 is a potent and orally active anti-mitotic agent and shows an inhibition of in vitro tubulin polymerization with an EC 50 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 rese

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

名前と識別子

異性体SMILES

COC1=NC=CC(=C1)C(=O)C2=CC(=CC(=C2)C3=C4C=CNC4=CC=C3)NS(=O)(=O)C

代替CAS番号

915412-67-8

PubChem CID

15603282

MeSH用語

LP 261;LP-261;LP261 cpd;N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide

分子量

421.47

よくある質問

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 915412-67-8, the molecular formula is C22H19N3O4S, and the molecular weight is 421.47 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.