LP-261

SKU: orb1297994

Description

LP-261 is a colchicine-site tubulin inhibitor that arrests the cell cycle at the G2/M phase. It is a research tool for studying cytoskeleton dynamics and mechanisms of antimitotic agents in both in vitro cell-based assays and in vivo preclinical cancer models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 915412-67-8
• MW: 421.47
• Purity: 99.91% (May vary between batches)
• Formula: C₂₂H₁₉N₃O₄S
• SMILES: COc1cc(ccn1)C(=O)c1cc(NS(C)(=O)=O)cc(c1)-c1cccc2[nH]ccc12
• Target: Microtubule Associated
• Solubility: DMSO:22 mg/mL (52.2 mM)

Bioactivity

• Target IC50:
  Tubulin polymerization:3.2 μM (EC50)
• In Vivo:
  LP-261 significantly inhibits growth of a human non-small-cell lung tumor (NCI-H522) in a mouse xenograft model.
• In Vitro:
  LP-261 was tested as a single agent in colon adenocarcinoma (SW620) and prostate cancer (LNCaP and PC3) xenografts, evaluating several different dosing schedules. LP-261 was also used in combination with bevacizumab in the SW620 xenograft model. LP-261 also exhibited high oral bioavailability and apparent lack of efflux by intestinal transporters such as ABCB1. LP-261 is a very potent inhibitor of angiogenesis, preventing microvessel outgrowth in the rat aortic ring assay and HUVEC cell proliferation at nanomolar concentrations. Complete inhibition of tumor growth was achieved in the PC3 xenograft model and shown to be schedule dependent. Excellent inhibition of tumor growth in the SW620 model was observed, comparable with paclitaxel.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cancer, BXPC-3, anti-mitotic, NCI-H522, MicrotubuleAssociated, Microtubule/Tubulin, Microtubule Associated, Jurkat, inhibit, LP261, LP-261, LP 261, H522, Inhibitor, MCF-7, SW-620, tubulin polymerization, tumor

Compound Identifiers

PubChem CID

15603282