CGP60474
Based on 7 publication(s) in Google Scholar
CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.90%
- CAS. Nr.: 164658-13-3
- Formel: C18H18ClN5O
- Molecular Weight:355.82
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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
Publications Citing Use of MedChemExpress (MCE) CGP60474
More- Nat Immunol. 2024 Apr;25(4):659-670. [Abstract]
- Cell Rep Med. 2025 Aug 19;6(8):102276. [Abstract]
- Clin Cancer Res. 2024 Sep 13;30(18):4179-4189. [Abstract]
- EMBO Mol Med. 2025 Nov 26. [Abstract]
- Sci Rep. 2018 Oct 8;8(1):14969. [Abstract]
- Biomed Pharmacother. 2023 May:161:114486. [Abstract]
- Oncotarget. 2017 Nov 22;8(65):109135-109150. [Abstract]
Customer Validation & Images
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WB
Biologische Aktivität
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CDK1-Cyclin B 26 nM (IC50) |
CDK2/cyclinE 3 nM (IC50) |
cdk2/cyclin A 4 nM (IC50) |
CDK4/cyclin D 216 nM (IC50) |
Cdk5/p25 10 nM (IC50) |
CDK7/cyclin H 200 nM (IC50) |
CDK9/cycT 13 nM (IC50) |
PKC |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
0.11 μM
Compound: 1
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Inhibition of human recombinant SMG1 expressed in HEK293 cells using GST-tagged p53 as substrate after 1 hr by DELFIA assay
Inhibition of human recombinant SMG1 expressed in HEK293 cells using GST-tagged p53 as substrate after 1 hr by DELFIA assay
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[PMID: 23021994] |
| Huh-7 | CC50 |
0.2694 μM
Compound: GNF-Pf-88
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NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
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[PMID: 18579783] |
| Sf9 | IC50 |
0.003 μM
Compound: CGP60474
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Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
0.01 μM
Compound: CGP60474
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Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
0.013 μM
Compound: CGP60474
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Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
0.026 μM
Compound: CGP60474
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Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
0.2 μM
Compound: CGP60474
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Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
0.216 μM
Compound: CGP60474
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Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
CGP60474 (Compound A) is a potent VEGFR-2 inhibitor, with an IC50 of 84 nM[1]. CGP60474 is also a PKC inhibitor, with competitive kinetics relative to ATP[2].
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.
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Animal Model:C57Bl/6 mice (LPS endotoxemia model)[2]
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Dosage:10 mg/kg
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Administration:I.p.
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Result:Had a higher survival rate.
Chemical Information
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CAS. Nr. 164658-13-3
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Appearance Solid
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Molecular Weight 355.82
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Formel C18H18ClN5O
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Color Light yellow to yellow
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SMILES
ClC1=CC(NC2=NC=CC(C3=CC=NC(NCCCO)=C3)=N2)=CC=C1
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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 (7)
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Journal Impact Factor
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Most Recent
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Nat Immunol
2024 Apr;25(4):659-670. PMID: 38499799 -
Cell Rep Med
Computational framework for prioritizing candidate compounds overcoming the resistance of pancancer immunotherapy. [Abstract]2025 Aug 19;6(8):102276. PMID: 40769146 -
Clin Cancer Res
CDK9 inhibition by dinaciclib is a therapeutic vulnerability in epithelioid hemangioendothelioma. [Abstract]2024 Sep 13;30(18):4179-4189. PMID: 39052240 -
EMBO Mol Med
Isomeranzin activates Gnas-AMPK signaling to drive white adipose browning and curb obesity in mice. [Abstract]2025 Nov 26. PMID: 41299101 -
Sci Rep
LINCS L1000 dataset-based repositioning of CGP-60474 as a highly potent anti-endotoxemic agent. [Abstract]2018 Oct 8;8(1):14969. PMID: 30297806 -
Biomed Pharmacother
Discovery of drug targets and therapeutic agents based on drug repositioning to treat lung adenocarcinoma. [Abstract]2023 May:161:114486. PMID: 36906970 -
Oncotarget
2017 Nov 22;8(65):109135-109150. PMID: 29312596
CGP60474 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Nov 22;8(65):109135-109150. [Abstract]
MCF-7 cells are pretreated with the indicated chemical inhibitors for 30min, followed by 15 min treatment with RA (20 μM) + EPA (80 μM).Cell extracts are prepared and subjected to western blotting analysis.
Lösungsmittel & Löslichkeit
DMSO : ≥ 50 mg/mL (140.52 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" 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, 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)
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: ≥ 2.5 mg/mL (7.03 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 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.
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 (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Jorda R, et al. How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?. J Med Chem. 2018;61(20):9105-9120. [Content Brief]
[2]. Han HW, et al. LINCS L1000 dataset-based repositioning of CGP-60474 as a highly potent anti-endotoxemic agent. Sci Rep. 2018;8(1):14969. Published 2018 Oct 8. [Content Brief]
[3]. Stanetty P, et al. Novel and efficient access to phenylamino-pyrimidine type protein kinase C inhibitors utilizing a Negishi cross-coupling strategy. J Org Chem. 2005;70(13):5215-5220. [Content Brief]
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 |
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| DMSO | 1 mM | 2.8104 mL | 14.0520 mL | 28.1041 mL | 70.2602 mL |
| 5 mM | 0.5621 mL | 2.8104 mL | 5.6208 mL | 14.0520 mL | |
| 10 mM | 0.2810 mL | 1.4052 mL | 2.8104 mL | 7.0260 mL | |
| 15 mM | 0.1874 mL | 0.9368 mL | 1.8736 mL | 4.6840 mL | |
| 20 mM | 0.1405 mL | 0.7026 mL | 1.4052 mL | 3.5130 mL | |
| 25 mM | 0.1124 mL | 0.5621 mL | 1.1242 mL | 2.8104 mL | |
| 30 mM | 0.0937 mL | 0.4684 mL | 0.9368 mL | 2.3420 mL | |
| 40 mM | 0.0703 mL | 0.3513 mL | 0.7026 mL | 1.7565 mL | |
| 50 mM | 0.0562 mL | 0.2810 mL | 0.5621 mL | 1.4052 mL | |
| 60 mM | 0.0468 mL | 0.2342 mL | 0.4684 mL | 1.1710 mL | |
| 80 mM | 0.0351 mL | 0.1757 mL | 0.3513 mL | 0.8783 mL | |
| 100 mM | 0.0281 mL | 0.1405 mL | 0.2810 mL | 0.7026 mL |
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