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

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Solid
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Based on 1 publication(s) in Google Scholar

RGN6024 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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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.
Parmacokinetics
Species Dose Route Tmax T1/2 AUC0-t F Cmax
Mice[1] 3 mg/kg i.v. 0.083 h 0.354 h 1580 ng/L.h / /
Mice[1] 30 mg/kg p.o. 0.250 h 2.640 h 17900 ng·h/mL 113 % 7020 ng/mL
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.
Appearance

Solid

Color

White to off-white

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (247.86 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4786 mL 12.3928 mL 24.7856 mL
5 mM 0.4957 mL 2.4786 mL 4.9571 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4786 mL 12.3928 mL 24.7856 mL 61.9640 mL
5 mM 0.4957 mL 2.4786 mL 4.9571 mL 12.3928 mL
10 mM 0.2479 mL 1.2393 mL 2.4786 mL 6.1964 mL
15 mM 0.1652 mL 0.8262 mL 1.6524 mL 4.1309 mL
20 mM 0.1239 mL 0.6196 mL 1.2393 mL 3.0982 mL
25 mM 0.0991 mL 0.4957 mL 0.9914 mL 2.4786 mL
30 mM 0.0826 mL 0.4131 mL 0.8262 mL 2.0655 mL
40 mM 0.0620 mL 0.3098 mL 0.6196 mL 1.5491 mL
50 mM 0.0496 mL 0.2479 mL 0.4957 mL 1.2393 mL
60 mM 0.0413 mL 0.2065 mL 0.4131 mL 1.0327 mL
80 mM 0.0310 mL 0.1549 mL 0.3098 mL 0.7746 mL
100 mM 0.0248 mL 0.1239 mL 0.2479 mL 0.6196 mL
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RGN6024 Related Classifications

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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