RGB-286638
Based on 3 publication(s) in Google Scholar
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.67%
- CAS 番号: 784210-87-3
- 分子式: C29H37Cl2N7O4
- 分子量:618.55
-
保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Epigenetics Compound Library
HY-L005
-
Immunology/Inflammation Compound Library
HY-L007
-
JAK/STAT Compound Library
HY-L008
-
Kinase Inhibitor Library
HY-L009
-
MAPK Compound Library
HY-L010
-
PI3K/Akt/mTOR Compound Library
HY-L015
-
Protein Tyrosine Kinase Compound Library
HY-L016
-
Stem Cell Signaling Compound Library
HY-L017
-
Wnt/Hedgehog/Notch Compound Library
HY-L020
-
Anti-Cancer Compound Library
HY-L025
-
Clinical Compound Library
HY-L026
-
Anti-Aging Compound Library
HY-L034
-
Differentiation Inducing Compound Library
HY-L038
-
Reprogramming Compound Library
HY-L039
-
Oxygen Sensing Compound Library
HY-L045
-
Ferroptosis Compound Library
HY-L051
-
Glycolysis Compound Library
HY-L058
-
Cytoskeleton Compound Library
HY-L060
-
Anti-Alzheimer's Disease Compound Library
HY-L069
-
Anti-Breast Cancer Compound Library
HY-L074
-
Anti-Lung Cancer Compound Library
HY-L075
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
Anti-Blood Cancer Compound Library
HY-L079
-
Anti-Cancer Metabolism Compound Library
HY-L083
-
Neurodegenerative Disease-related Compound Library
HY-L086
-
Anti-Obesity Compound Library
HY-L087
-
Angiogenesis-Related Compound Library
HY-L088
-
Glucose Metabolism Compound Library
HY-L092
-
Anti-Liver Cancer Compound Library
HY-L101
-
Anti-Colorectal Cancer Compound Library
HY-L103
-
Antidepressant Compound Library
HY-L108
-
Anti-Prostate Cancer Compound Library
HY-L124
-
Anti-Pulmonary Fibrosis Compound Library
HY-L125
-
Cancer Stem Cells Compound Library
HY-L135
-
Pain-Related Compound Library
HY-L139
-
Metabolic Enzyme Compound Library
HY-L146
-
Autoimmune Disease Compound Library
HY-L156
-
Highly Selective Inhibitors Library
HY-L158
-
Serine/Threonine Kinase Inhibitor Library
HY-L164
-
Anti-Hematopathy Compound Library
HY-L171
-
Anti-Ovarian Cancer Compound Library
HY-L173
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
Anti-Brain Cancer Compound Library
HY-L188
-
Protein Kinase Compound Library
HY-L196
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
-
Anti-Rheumatic Arthritis Compound Library
HY-L210
-
Posttranslational Modification Library
HY-L226
-
High-Efficiency Gene Editing Compound Library
HY-L244
MedChemExpress（MCE）の使用を引用している文献 RGB-286638
MoreMEK アイソフォーム固有の製品をすべて表示
More
生物活性
|
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) |
Fms 1 nM (IC50) |
TAK1 5 nM (IC50) |
JNK1a1 17 nM (IC50) |
JNK1a2 40 nM (IC50) |
C-src 25 nM (IC50) |
AMPK 41 nM (IC50) |
RGB-286638 is an indenopyrazole-derived CDK inhibitor (CDKI) with Ki-nanomolar activity against transcriptional CDKs. RGB-286638 inhibits several tyrosine and serine/threonine non-CDK enzymes, i.e. GSK-3β, TAK1, AMPK, Jak2, MEK1. The dose- and time-dependent effect of treatment with RGB-286638 (12.5-100nM) is investigated on the growth of human p53-wt (MM.1S, MM.1R, and H929) and p53-mutant (U266, OPM1, and RPMI) MM cells by MTT assay, assessing viability at 24 and 48 hours. The half-maximally effective concentrations (EC50) range between 20 and 70 nM at 48 hours. Dose-dependent differences in growth among p53-wt and -mutant cells are observed after 50nM treatment, with p53-wt MM.1S, MM.1R and H929 being slightly more sensitive to RGB-286638 treatment at 48h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 784210-87-3
-
性状 Solid
-
分子量 618.55
-
分子式 C29H37Cl2N7O4
-
Color Light yellow to yellow
-
SMILES
O=C(NN1CCOCC1)NC2=CC=CC(C3=C4C(C5=CC=C(CN6CCN(CCOC)CC6)C=C5)=NN3)=C2C4=O.[H]Cl.[H]Cl
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
-
Journal Impact Factor
-
Most Recent
-
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 -
溶剤 & 溶解度
DMSO : ≥ 150 mg/mL (242.50 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 25 mg/mL (40.42 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 7.5 mg/mL (12.13 mM); Clear solution
This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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: ≥ 7.5 mg/mL (12.13 mM); Clear solution
This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
プロトコル
Nuclear proteins are isolated from MM.1S cells treated with 50nM RGB-286638 for 1, 4, and 8 h, using Nuclear Extraction Kit. Nuclear protein aliquots are added to the 96-well plate coated with specific double-stranded DNA sequence containing the p53 response element for overnight incubation. p53 in the nuclear extract is detected by addition of a specific primary antibody directed against p53. A secondary antibody conjugated to HRP is added to provide a sensitive colorimetric readout at 450 nm. All experiments are performed in triplicates[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Colorimetric assays are performed to assay drug activity at increasing concentrations of RGB-286638 (0-100nM). Expressing wild-type p53 (MM.1S, MM.1R, H929) or mutant-p53 (U266, OPM1, RPMI) cells from 24- or 48-h cultures are pulsed with 10μL of 5mg/mL MTT to each well, followed by incubation at 37°C for 4h, and addition of 100 μL isopropanol containing 0.04 HCl. Absorbance readings at a wavelength of 570nm (with correction using readings at 630nm) are taken on a spectrophotometer. All experiments are performed in triplicates[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
The in vivo anti-MM activity of RGB-286638 is evaluated in an MM xenograft model. RGB-286638 dosing solutions of 2 and 3 mg/mL in 5% dextrose/water (D5W) pH5.2, as well as D5W pH5.2 for vehicle control dosing group, are prepared and provided by Agennix AG. CB-17 severe combined immunodeficient (SCID) mice are used. Forty male 5-6 week old mice are irradiated (2 Gy [200 rad]) using cesium 137 (137Cs)-irradiator source); 24h after irradiation, 2.5×106 MM.1S cells are inoculated subcutaneously in the upper back. When tumor weight is approximately 100 mg, mice are randomly assigned into 3 cohorts receiving daily IV tail vein injections for 5 consecutive days with either RGB-286638 30 mg/kg (8 mice), 40 mg/kg (9 mice), or control vehicle alone (10 mice). Animals are monitored for body weight and tumor volume by caliper measurements every alternate day. Tumor volume is estimated. Survival is evaluated from the first day of treatment until death. Tumor growth is evaluated using caliper measurements from the first day of treatment until day of first sacrifice. Percentage tumor growth inhibition (TGI) is calculated.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
-
データシート (281 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)
-
取扱説明書 (2659 KB)
参考文献
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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.6167 mL | 8.0834 mL | 16.1668 mL | 40.4171 mL |
| 5 mM | 0.3233 mL | 1.6167 mL | 3.2334 mL | 8.0834 mL | |
| 10 mM | 0.1617 mL | 0.8083 mL | 1.6167 mL | 4.0417 mL | |
| 15 mM | 0.1078 mL | 0.5389 mL | 1.0778 mL | 2.6945 mL | |
| 20 mM | 0.0808 mL | 0.4042 mL | 0.8083 mL | 2.0209 mL | |
| 25 mM | 0.0647 mL | 0.3233 mL | 0.6467 mL | 1.6167 mL | |
| 30 mM | 0.0539 mL | 0.2694 mL | 0.5389 mL | 1.3472 mL | |
| 40 mM | 0.0404 mL | 0.2021 mL | 0.4042 mL | 1.0104 mL | |
| DMSO | 50 mM | 0.0323 mL | 0.1617 mL | 0.3233 mL | 0.8083 mL |
| 60 mM | 0.0269 mL | 0.1347 mL | 0.2694 mL | 0.6736 mL | |
| 80 mM | 0.0202 mL | 0.1010 mL | 0.2021 mL | 0.5052 mL | |
| 100 mM | 0.0162 mL | 0.0808 mL | 0.1617 mL | 0.4042 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
RGB-286638 関連分類
HY-15504 関連分類
Powered by Bioz