Microtubule destabilizing agent-3

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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.

For research use only. We do not sell to patients.

Microtubule destabilizing agent-3 Chemical Structure

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Biological Activity
Purity & Documentation
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Description

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.

Cell Cycle Analysis^[1]

Cell Line:	JJN3 cells
Concentration:	500 nM
Incubation Time:	24 h, 48 h
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.

Apoptosis Analysis^[1]

Cell Line:	JJN3 cells
Concentration:	500 nM
Incubation Time:	24 h, 48 h
Result:	Triggered cell surface phosphatidylserine exposure and accumulation of cells in a sub-G1 peak, features of apoptotic cell death.

Parmacokinetics

Species	Dose	Route	T_1/2	C_max
Mice^[1]	10 mg/kg	i.p.	1.5 h	3.6 μM

In Vivo

Microtubule destabilizing agent-3 (VPR8) (15 mg/kg, i.p., five daily doses followed by 2 days of rest) significantly delays tumor progression and improves survival in a multiple myeloma and lymphoma mouse xenograft model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NOD.Cg-Prkdc^scid IL2rg^tmIWjl/Szj (NSG) mice bearing JJN3Luc2 myeloma cells^[1]
Dosage:	15 mg/kg
Administration:	i.p., five daily doses followed by 2 days of rest
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.

Animal Model:	Ptprca mice bearing EμMyc lymphoma cells^[1]
Dosage:	15 mg/kg
Administration:	i.p., five daily doses followed by 2 days of rest
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).

Molecular Weight

363.48

Formula

C₂₀H₂₁N₅S

SMILES

CC1=C(C2=C(N1)C=CC=C2)/C=N\NC3=NC=NC4=C3C5CCCCC5S4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Susanto O, et al. Discovery and characterisation of VPRBP/DCAF1 kinase inhibitor analogues as microtubular destabilising agents with potent anti-myeloma activity. Mol Cancer Ther. 2025 Nov 4. [Content Brief]