2. Cell Cycle/DNA Damage Cytoskeleton
  3. Microtubule/Tubulin
  4. RGN6024

RGN6024 is a brain-penetrant, orally active and reversible small molecule tubulin destabilizer. RGN6024 inhibits microtubule polymerization both in biochemical and cellular assays, binds to the colchicine binding pocket of β-tubulin (SPR: Kd = 6.7 μM; tryptophan assay: Kd = 7.4 μM), and triggers G2/M arrest in glioblastoma (GB) cells. RGN6024 retains activity in βIII-tubulin overexpressing cells. RGN6024 inhibits tumor growth in a GB xenograft mouse model. RGN6024 can be used for the study of glioblastoma (GB).

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RGN6024

RGN6024 Chemical Structure

CAS No. : 3055038-20-2

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RGN6024 Related Antibodies

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Description

RGN6024 is a brain-penetrant, orally active and reversible small molecule tubulin destabilizer. RGN6024 inhibits microtubule polymerization both in biochemical and cellular assays, binds to the colchicine binding pocket of β-tubulin (SPR: Kd = 6.7 μM; tryptophan assay: Kd = 7.4 μM), and triggers G2/M arrest in glioblastoma (GB) cells. RGN6024 retains activity in βIII-tubulin overexpressing cells. RGN6024 inhibits tumor growth in a GB xenograft mouse model. RGN6024 can be used for the study of glioblastoma (GB)[1].

In Vitro

RGN6024 (100 nM, 48 h) binds to the colchicine binding site of β-tubulin and disrupts microtubule morphology in U87 glioblastoma cells[1].
RGN6024 (72 h) reversibly decreases the viability of glioblastoma cells with IC50 values of 85 nM (U87), 23 nM (LN-18) and 120 nM (BT142)[1].
RGN6024 (0.001-100 μM, 6 h) demonstrates high reversibility in U87 cell viability washout experiments, with an IC50 of 2482 nM after washout (30-fold shift from 81.6 nM no-washout)[1].
RGN6024 (250 nM, 48 h) induces G2/M arrest in U87 cells and is not susceptible to βIII-tubulin overexpression in HeLa cells[1].

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

RGN6024 Related Antibodies

Immunofluorescence[1]

Cell Line: U87 glioblastoma cells
Concentration: 100 nM
Incubation Time: 48 h
Result: Showed loss of MT bundles and changes in cell shape relative to DMSO-treated cells.

Cell Cycle Analysis[1]

Cell Line: U87 glioblastoma cells
Concentration: 250 nM
Incubation Time: 48 h
Result: Induced G2/M arrest in U87 cells.
In Vivo

RGN6024 (7.5-25 mg/kg, p.o., daily or 5days-on/2days-off, 15 days) inhibits tumor growth in a Temozolomide (TMZ) (HY-17364)-resistant GB xenograft mouse model[1].
RGN6024 (15-20 mg/kg, p.o., once or twice daily or once every two days, 49 days) inhibits tumor growth and prolongs survival in an orthotopic GB xenograft mouse model[1].

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

Animal Model: LN-18 cells (10×106) in 0.2 mL PBS/Matrigel (50:50) were injected subcutaneously into the upper right flank of female CB17 SCID mice aged 6-8 weeks[1]
Dosage: 7.5, 15 mg/kg daily or 25 mg/kg 5days-on/2days-off (combined with Temozolomide)
Administration: p.o. daily or 5days-on/2days-off (combined with Temozolomide) for 49 days
Result: Reduced tumor growth by 72% and 60% at doses of 7.5 and 15 mg/kg, respectively.
Animal Model: BT142 mut/cells (IDH1 R132H) engineered to express luciferase (BT142-Luc) were stereotactically inoculated into the caudate nucleus of the right brain hemisphere of 6-8-week-old anesthetized BALB/c nude female mice[1]
Dosage: 15 mg/kg once daily 15 mg/kg twice daily, 20 mg/kg once daily and 20 mg/kg on alternate days
Administration: p.o. for 49 days
Result: Showed a statistically significant decrease in tumor size treated with 15 mg/kg twice daily and 20 mg/kg once daily.
Showed no significant change in the body weight.
Improved survival relative to control animals.
Molecular Weight

403.46

Formula

C18H21N5O4S
CAS No.
SMILES

O=C(NC1=NC=C(OC2=CN=C(N=C2)N3CCOCC3)S1)C45CC(OC)(C5)C4
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
References
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RGN6024 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RGN60243055038-20-2RGN 6024RGN-6024Microtubule/TubulinglioblastomatubulinU87 cellsLN-18 cellsInhibitorinhibitorinhibit

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