Microtubule destabilizing agent-2 (Compound 21) is an orally available, effective and selective anti-tumor compound targeting microtubules. Microtubule destabilizing agent-2 can destabilize microtubules and inhibit microtubule polymerization. Microtubule destabilizing agent-2 arrests human tumor cells at the G0/G1 phase and induces apoptosis by activating the caspase cascade pathway. Microtubule destabilizing agent-2 also has anti-inflammatory activity and can inhibit TNF-α and IL-6 production in vitro. Microtubule destabilizing agent-2 can inhibit tumor growth in xenograft mice.

Physicochemical Properties

Molecular Formula	C26H26O4
Molecular Weight	402.48
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	Caspase 3
ln Vitro	Microtubule destabilizing agent-2 (48 h) has a selective antiproliferative effect on human leukemia K-562 cells (IC50: 3.27 μM), compared with IC50 of 82.46 μM (MCF-7) and 31.27 μM (MDA-MB-231) [1].
ln Vivo	Microtubule destabilizing agent-2 (20-80 mg/kg, oral, 28 days) has moderate to low anticancer effects in the K562 xenograft mouse model [1].
Animal Protocol	Animal/Disease Models: K562 xenograft mouse model[1] Doses: 20, 40, 80 mg/kg. Route of Administration: Oral gavage (p.o.). 5 days a week for four weeks Experimental Results: Showed weak anticancer effect at 20 mg/kg (36 % reduction) and 40 mg/kg (31.68 % reduction), but moderate effect at 80 mg/kg (47 %).
References	[1]. 5H-benzocfluorene derivative exhibits antiproliferative activity via microtubule destabilization. Bioorganic chemistry, 2024, 153:107891.

Solubility Data

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.4846 mL	12.4230 mL	24.8460 mL
	5 mM	0.4969 mL	2.4846 mL	4.9692 mL
	10 mM	0.2485 mL	1.2423 mL	2.4846 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.