Microtubule destabilizing agent-2
Microtubule destabilizing agent-2 (Compound 21) is an orally active and selective antitumor compound targeting microtubule protein. Microtubule destabilizing agent-2 destabilizes microtubule proteins and inhibits microtubule polymers. Microtubule destabilizing agent-2 arrests the G0/G1 phase in human tumor cells. Microtubule destabilizing agent-2 induces Apoptosis by activating the cascade pathway of caspases. Microtubule destabilizing agent-2 has anti-inflammatory activity, as inhibiting TNF-α and IL-6 in vitro. Microtubule destabilizing agent-2 reduces tumors growth in xenograft mice.
For research use only. We do not sell to patients.
- Formula: C26H26O4
- Molecular Weight:402.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
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Caspase 3 |
Microtubule destabilizing agent-2 (48 h) has a selective antiproliferative effect on human leukemia cell K-562 (IC50: 3.27 μM), with IC50s of 82.46 μM (MCF-7), 31.27 μM (MDA-MB-231)[1].
Microtubule destabilizing agent-2 (5 μM, 24 h) induces G0/G1 phase arrest in K562 cells[1].
Microtubule destabilizing agent-2 (4-64 μM) significantly induces early and late apoptosis in K562 leukemia cells, and activates caspase 3 (activation rate: 2.13 %-26.53 %)[1].
Microtubule destabilizer-2 (2.5-10 μM, 60 min) destabilizes microtubule proteins[1].
Microtubule destabilizer-2 (1-10 µg/mL) exhibits moderate anti-inflammatory activity and inhibits LPS (HY-D1056)-induced TNF-α and IL-6 production in primary macrophages[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Microtubule destabilizing agent-2 (5-1000 mg/kg, p.o.) induces minor adverse reactions in Swiss albino mice, but is well tolerated[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:K562 xenograft mouse model[1]
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Dosage:20, 40, 80 mg/kg.
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Administration:Oral gavage (p.o.). 5 days a week for four weeks
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Result: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 %).
Chemical Information
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Molecular Weight 402.48
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Formula C26H26O4
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SMILES
OC1=C(C2=C(C[C@]([H])(CCC3=C4C=CC(OCC5=CC=CC=C5)=C3)[C@@]24[H])C=C1OC)OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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