RGN6024
Based on 1 Customer Validation
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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- Pureté: 98.99%
- CAS No.: 3055038-20-2
- Formule: C18H21N5O4S
- Masse moléculaire:403.46
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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.
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Cell Line:U87 glioblastoma cells
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Concentration:100 nM
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Incubation Time:48 h
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Result:Showed loss of MT bundles and changes in cell shape relative to DMSO-treated cells.
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Cell Line:U87 glioblastoma cells
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Concentration:250 nM
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Incubation Time:48 h
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Result:Induced G2/M arrest in U87 cells.
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.
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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]
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Dosage:7.5, 15 mg/kg daily or 25 mg/kg 5days-on/2days-off (combined with Temozolomide)
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Administration:p.o. daily or 5days-on/2days-off (combined with Temozolomide) for 49 days
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Result:Reduced tumor growth by 72% and 60% at doses of 7.5 and 15 mg/kg, respectively.
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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]
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Dosage:15 mg/kg once daily 15 mg/kg twice daily, 20 mg/kg once daily and 20 mg/kg on alternate days
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Administration:p.o. for 49 days
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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
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CAS No. 3055038-20-2
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Appearance Solid
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Masse moléculaire 403.46
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Formule C18H21N5O4S
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Color White to off-white
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SMILES
O=C(NC1=NC=C(OC2=CN=C(N=C2)N3CCOCC3)S1)C45CC(OC)(C5)C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (278 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
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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