D64131

SKU: orb1224087

Description

D-64131 is a tubulin polymerization inhibitor with an IC50 value of 0.53 μM. The polymerization of bovine brain tubulin as well as binding of [3H] colchicine to biotinylated αβ-tubulin was dose-dependently inhibited by D-64131. Many Y cells display abnormal microtubule structures, such as fragmented mitotic spindles or multiple spindle poles after treatment with D-64131. Nuclear blebbing and abnormal nuclear structures typical for apoptotic cells are detectable in many cells treated with D-64131. In nude mice, D-64131 proved to be well tolerated and highly active against the human amelanoic melanoma MEXF 989 tumor xenograft. D-64131 treatment resulted in significant tumor growth inhibition during treatment.

Key Properties

• CAS Number: 74588-78-6
• MW: 251.28
• Purity: >98% (HPLC)
• Formula: C₁₆H₁₃NO₂
• SMILES: O=C(C(N1)=CC2=C1C=CC(OC)=C2)C3=CC=CC=C3
• Target: Microtubule/Tubulin
• Solubility: Soluble in DMSO

Bioactivity

• In Vivo:
  D-64131 (200-400 mg/kg; p.o. ; daily; days 1-5, 8-9, and 15-18) significantly inhibits tumor growth in the human amelanoic melanoma MEXF 989 tumor xenograft mice model. D-64131 has oral bioavailability and is well tolerated at efficacious doses. Animal model: Outbred nude mice (6-8 weeks), human amelanoic melanoma MEXF 989 tumor xenograft model. Dosage: 200 mg/kg, 400 mg/kg. Administration: Oral administration, daily, on days 1-5, 8-9, and 15-18 after xenograft. Result: Resulted in significant tumor growth inhibition during treatment.
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• In Vitro:
  D-64131 is antimitotic by binding to β-tubulin, thereby destabilizing microtubules and arresting mitotic cells in the M-phase. D-64131 inhibits the proliferation of tumor cells from 12 of 14 different organs and tissues with mean IC50s of 62 nM. D-64131 is cytotoxic toward MDR/MRP tumor cell lines. D-64131 suppresses U373 proliferation and cell cycle with IC50s of 74 nM and 62.7 nM, respectively. Cell Cycle Analysis Cell line: HeLa/KB cervical carcinoma cells. Concentration: 1 nM-1 μM. Incubation time: 48 hours. Result: Induced dose-dependently arrested in G2-M before induction of apoptotic cell death.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

D-64131 | D 64131 | D64131

Quick Database Links

Gene Symbol

Microtubule/Tubulin