RGB-286638 free base
Based on 3 publication(s) in Google Scholar
RGB-286638 free base is a potent inhibitor of CDK and MAPK9. RGB-286638 free base inhibits the activities of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3 and p35-CDK5, with IC50 values of 1, 2, 3, 4, 5 and 5 nM, respectively. RGB-286638 free base inhibits GSK-3β and TAK1, with IC50 values of 3 nM and 5 nM, respectively. RGB-286638 free base induces caspase-dependent Apoptosis in cells. RGB-286638 free base delays tumor growth in an orthotopic glioblastoma mouse model. RGB-286638 free base extends survival in multiple myeloma models. RGB-286638 free base can be used in research related to glioblastoma and multiple myeloma.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.76%
- CAS. Nr.: 784210-88-4
- Formel: C29H35N7O4
- Molecular Weight:545.63
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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HY-15504
RGB-286638 -
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Abemaciclib (Standard) -
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Ribociclib succinate
Publications Citing Use of MedChemExpress (MCE) RGB-286638 free base
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
T1-CDK9 1 nM (IC50) |
cyclin B1-CDK1 2 nM (IC50) |
cyclin E-CDK2 3 nM (IC50) |
cyclin D1-CDK4 4 nM (IC50) |
cyclin E-CDK3 5 nM (IC50) |
p35-CDK5 5 nM (IC50) |
cyclin H-CDK7 44 nM (IC50) |
cyclin D3-CDK6 55 nM (IC50) |
GSK-3β 3 nM (IC50) |
JAK2 50 nM (IC50) |
MEK1 54 nM (IC50) |
JNK2 |
In Vitro
RGB-286638 (0-20 μM; 72 h) free base potently reduces viability in U87, U251, T98G, U138, GBM8, and a subset of GSC glioblastoma models, with IC50 values ranging from 0.01 to 0.03 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U87, U251, T98G, U138, HT29, GBM8, patient-derived glioblastoma sphere cultures (GSCs)
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Concentration:0-20 μM
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Incubation Time:72 h
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Result:Induced near-complete viability inhibition in U87, U251, T98G, U138, and HT29 cell lines, with IC50 values ranging from 0.01 to 0.03 μM.
Caused approximately one-third of GSC models to show high sensitivity matching established cell lines, one-third to show incomplete response with 5-30% viability after exposure to 1 μM, and one-third to show resistance.
In Vivo
RGB-286638 (30-40 mg/kg; i.v.; daily; 5 consecutive days) free base achieves a log10 cell kill of 1.6, maximum tumor growth inhibition of 85.06-86.34%, and prolonged survival in a mouse multiple myeloma xenograft model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:athymic nude-Fox1nu (female, 6-8 weeks old, orthotopic glioblastoma model via intracranial injection of luciferase- and mCherry-expressing GBM8 primary GBM cells)[1]
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Dosage:40 mg/kg
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Administration:i.v.; daily; 5 consecutive days
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Result:Reduced in vivo luminescence signals (tumor growth measure) significantly compared to vehicle and control groups.
Showed no significant difference in median overall survival (53 days) versus vehicle-treated mice (47 days).
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Animal Model:CB-17 severe combined immunodeficient (SCID) (male, 5-6 weeks old, irradiated with 2 Gy 24 hours prior to subcutaneous inoculation of MM.1S cells)[2]
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Dosage:30 mg/kg; 40 mg/kg
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Administration:i.v.; daily; 5 consecutive days
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Result:Achieved a maximum tumor growth inhibition (TGI) of 85.06% at day 14 post-treatment.
Achieved a maximum tumor growth inhibition (TGI) of 86.34% at day 14 post-treatment.
Achieved a log10 cell kill of 1.6.
Prolonged survival, with the first death occurring at day 43 compared to day 24 in controls.
Caused maximum body weight loss of 8.4% at day 5, with subsequent weight recovery within two weeks.
Caused maximum body weight loss of 9.9% at day 15, with subsequent weight recovery within two weeks.
Resulted in no toxic deaths during the study.
Chemical Information
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CAS. Nr. 784210-88-4
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Appearance Solid
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Molecular Weight 545.63
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Formel C29H35N7O4
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Color Light yellow to green yellow
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SMILES
O=C(NN1CCOCC1)NC2=CC=CC(C3=C4C(C5=CC=C(CN6CCN(CCOC)CC6)C=C5)=NN3)=C2C4=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
Cancers (Basel)
Identification of New Vulnerabilities in Conjunctival Melanoma Using Image-Based High Content Drug Screening. [Abstract]2022 Mar 19;14(6):1575. PMID: 35326726 -
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (183.27 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : < 1 mg/mL (insoluble)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (9.16 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (9.16 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 17% Solutol HS-15 in Saline
Solubility: 10 mg/mL (18.33 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
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.
Reinheit & Dokumentation
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Data Sheet (289 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
Verweise
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8327 mL | 9.1637 mL | 18.3274 mL | 45.8186 mL |
| 5 mM | 0.3665 mL | 1.8327 mL | 3.6655 mL | 9.1637 mL | |
| 10 mM | 0.1833 mL | 0.9164 mL | 1.8327 mL | 4.5819 mL | |
| 15 mM | 0.1222 mL | 0.6109 mL | 1.2218 mL | 3.0546 mL | |
| 20 mM | 0.0916 mL | 0.4582 mL | 0.9164 mL | 2.2909 mL | |
| 25 mM | 0.0733 mL | 0.3665 mL | 0.7331 mL | 1.8327 mL | |
| 30 mM | 0.0611 mL | 0.3055 mL | 0.6109 mL | 1.5273 mL | |
| 40 mM | 0.0458 mL | 0.2291 mL | 0.4582 mL | 1.1455 mL | |
| 50 mM | 0.0367 mL | 0.1833 mL | 0.3665 mL | 0.9164 mL | |
| 60 mM | 0.0305 mL | 0.1527 mL | 0.3055 mL | 0.7636 mL | |
| 80 mM | 0.0229 mL | 0.1145 mL | 0.2291 mL | 0.5727 mL | |
| 100 mM | 0.0183 mL | 0.0916 mL | 0.1833 mL | 0.4582 mL |
RGB-286638 free base Related Classifications
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