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

CAS: 915412-67-8 Cat. No.: L655070 Peso molecular: 421.47 PubChem CID: 15603282

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

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)

Specifications

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

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

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Nombres e identificadores

• Isómeros SMILES: COC1=NC=CC(=C1)C(=O)C2=CC(=CC(=C2)C3=C4C=CNC4=CC=C3)NS(=O)(=O)C
• CAS alternativo: 915412-67-8
• PubChem CID: 15603282
• Términos de entrada MeSH: LP 261;LP-261;LP261 cpd;N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide
• Peso molecular: 421.47