Microtubule destabilizing agent-3
Microtubule destabilizing agent-3, a B32B3 (HY-12240) analog, is a microtubule destabilizing agent. Microtubule destabilizing agent-3 exerts its antimyeloma phenotypes by destabilizing microtubules and promoting mitotic arrest, leading to cell death. Microtubule destabilizing agent-3 induces G2/M phase arrest and caspase-dependent apoptosis. Microtubule destabilizing agent-3 can be used for the research of multiple myeloma.
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- Formel: C20H21N5S
- Molecular Weight:363.48
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Speicherung:
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Biologische Aktivität
Beschreibung
In Vitro
Microtubule destabilizing agent-3 (VPR8) (500 nM; 24-48 h) demonstrates significant cell death (IC50 of ~190 nM) and G2M arrest, and induces apoptosis in JJN3 cells[1].
Microtubule destabilizing agent-3 (500 nM; 1-24 h) upregulates G2M and autophagy-related signatures and downregulated a MYC signature[1].
Microtubule destabilizing agent-3 (0.25-20 μM; 24 h) does not reduce H2AT120P and EZH2 or H3K27me3 levels in multiple myeloma cells. Microtubule destabilizing agent-3 demonstrates thermal stabilization of DCAF1 in CETSA[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:JJN3 cells
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Concentration:500 nM
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Incubation Time:24 h, 48 h
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Result:Reduced cell viability in multiple myeloma cell lines, with an IC50 of approximately 190 nM.
Induced G2M cell cycle arrest. G2M phase was significantly prolonged, and cells spent more time in G2M before dying.
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Cell Line:JJN3 cells
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Concentration:500 nM
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Incubation Time:24 h, 48 h
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Result:Triggered cell surface phosphatidylserine exposure and accumulation of cells in a sub-G1 peak, features of apoptotic cell death.
Parmacokinetics
| Species | Dose | Route | T1/2 | Cmax |
|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 1.5 h | 3.6 μM |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD.Cg-Prkdcscid IL2rgtmIWjl/Szj (NSG) mice bearing JJN3Luc2 myeloma cells[1]
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Dosage:15 mg/kg
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Administration:i.p., five daily doses followed by 2 days of rest
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Result:Tumor progression was significantly delayed in NSG mice bearing luciferase-tagged JJN3 xenografts and overall survival was significantly prolonged (median 27 days for vehicle vs. 33 days). No overt hematopoietic toxicity was observed, as evidenced by preserved peripheral blood leukocyte and platelet counts and hemoglobin concentration.
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Animal Model:Ptprca mice bearing EμMyc lymphoma cells[1]
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Dosage:15 mg/kg
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Administration:i.p., five daily doses followed by 2 days of rest
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Result:Tumor progression was significantly suppressed in Ptprca mice transplanted with EμMyc lymphoma cells, as indicated by reduced spleen weight, peripheral blood, and nodal tumor burden. Continued treatment (10 days) significantly improved overall survival (median 17 days for vehicle vs. 22 days).
Chemical Information
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Molecular Weight 363.48
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Formel C20H21N5S
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SMILES
CC1=C(C2=C(N1)C=CC=C2)/C=N\NC3=NC=NC4=C3C5CCCCC5S4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Microtubule destabilizing agent-3 Related Classifications
HY-179695 Related Classifications
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