Art. -Nr.: HY-176537

RGN6024

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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: K_d = 6.7 μM; tryptophan assay: K_d = 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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Reinheit: 98.99%
CAS. Nr.: 3055038-20-2
Formel: C₁₈H₂₁N₅O₄S
Molecular Weight:403.46

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

RGN6024 Chemical Structure

CAS. Nr.: 3055038-20-2

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Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

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	T_max	T_1/2	AUC_0-t	F	C_max
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.

Chemical Information

CAS. Nr. 3055038-20-2
Appearance Solid
Molecular Weight 403.46
Formel C₁₈H₂₁N₅O₄S
Color White to off-white
SMILES

O=C(NC1=NC=C(OC2=CN=C(N=C2)N3CCOCC3)S1)C45CC(OC)(C5)C4
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4786 mL

12.3928 mL

24.7856 mL

5 mM

0.4957 mL

2.4786 mL

4.9571 mL

10 mM

0.2479 mL

1.2393 mL

2.4786 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Patrón LA, et al. RGN6024 Is a Brain-Penetrant, Small-Molecule Tubulin Destabilizer for the Treatment of Glioblastoma. Mol Cancer Ther. 2025 Aug 1;24(8):1129-1144. doi: 10.1158/1535-7163.MCT-24-1208 [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

RGN6024

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

RGN6024 Related Classifications

HY-176537 Related Classifications