| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
CGP60474 targets multiple cyclin-dependent kinases (CDKs) including CDK1, CDK2, CDK4, CDK5, CDK7, and CDK9. It also inhibits VEGFR-2 (IC₅₀ = 84 nM) and is an ATP-competitive PKC inhibitor. By inhibiting CDKs, CGP60474 blocks cell cycle progression and transcription, leading to reduced cell proliferation. The compound's anti-endotoxemic activity is mediated through inhibition of inflammatory cytokine production, particularly IL-6.
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| ln Vitro |
CGP60474 (Compound A) has an IC50 of 84 nM, making it a strong inhibitor of VEGFR-2 [1]. Another PKC inhibitor with competitive kinetics against ATP is CGP60474 [2].
In vitro, CGP60474 inhibits CDK1/CyclinB, CDK2/CyclinE, CDK2/CyclinA, CDK5/p25, CDK7/CyclinH, CDK4/CyclinD, and CDK9/CycT with IC₅₀ values of 26, 3, 4, 216, 10, 200, and 13 nM, respectively. It also inhibits VEGFR-2 with an IC₅₀ of 84 nM. The compound is soluble in DMSO at 117.5 mg/mL (330.22 mM). Specific IC₅₀ values for PKC inhibition are documented in the literature. It shows potent activity against a broad range of kinase targets. |
| ln Vivo |
In the LPS endotoxemia paradigm, CGP-60474 (10?mg/kg; ip) reduces IL-6 levels and increases survival [2].
In vivo, CGP60474 (10 mg/kg; i.p.) inhibits IL-6 levels and improves survival in the LPS endotoxemia model. The compound's anti-endotoxemic activity has been demonstrated in animal models of sepsis. Its potential applications in cancer treatment are being investigated, particularly in tumors characterized by uncontrolled CDK activity. Further studies are needed to fully characterize its therapeutic potential. |
| Enzyme Assay |
Kinase inhibition assays are performed using purified CDK/cyclin complexes, PKC, or VEGFR-2 enzymes. Kinase activity is measured by phosphorylation of peptide substrates using radiolabeled ATP or fluorescence-based detection. CGP60474 is tested at various concentrations, and IC₅₀ values are calculated. ATP-competition assays determine the mechanism of inhibition. Binding affinity is determined using surface plasmon resonance or isothermal titration calorimetry.
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| Cell Assay |
In vitro cellular assays use various cancer cell lines to assess CDK inhibition and antiproliferative activity. Cells are treated with CGP60474 at various concentrations. Cell viability is measured by MTT assay. Cell cycle analysis is performed by flow cytometry using propidium iodide staining. Apoptosis is evaluated by Annexin V staining or caspase activity assays. The compound is dissolved in DMSO for stock solutions and diluted in culture media.
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| Animal Protocol |
Animal/Disease Models: C57Bl/6 mice (LPS endotoxemia model) [2]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results:higher survival rate. In vivo efficacy is evaluated in animal models, including the LPS endotoxemia model where CGP60474 (10 mg/kg; i.p.) inhibits IL-6 levels and improves survival. Murine xenograft models are used to assess antitumor activity. The compound is administered intraperitoneally or orally. Tumor growth is monitored by caliper measurements. Inflammatory markers and survival are assessed in endotoxemia models. Pharmacokinetic studies are conducted to determine plasma concentrations. |
| ADME/Pharmacokinetics |
CGP60474 has a molecular weight of 355.82 and molecular formula C₁₈H₁₈ClN₅O with CAS number 164658-13-3. It is soluble in DMSO at 117.5 mg/mL (330.22 mM) and insoluble in water (<0.1 mg/mL). For storage, powder should be kept at -20°C for up to 3 years, and in solvent at -80°C for 1 year. For in vivo studies, a formulation of 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline is recommended.
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| Toxicity/Toxicokinetics |
Specific toxicity data for CGP60474 are documented in preclinical studies. As a CDK inhibitor, its safety profile is consistent with other compounds in this class. Common adverse effects may include myelosuppression, gastrointestinal disturbances, and fatigue. The compound's anti-endotoxemic activity suggests potential for treating inflammatory conditions. Standard laboratory safety precautions should be followed when handling this compound. It is intended for research use only.
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| References |
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| Additional Infomation |
3-[[4-[2-(3-chloroanilino)-4-pyrimidinyl]-2-pyridinyl]amino]-1-propanol is a substituted aniline.
CGP60474 is a potent multi-kinase inhibitor targeting CDKs, PKC, and VEGFR-2. It shows potent inhibition of a broad range of CDKs with IC₅₀ values ranging from 3 to 216 nM. The compound also demonstrates anti-endotoxemic activity by inhibiting IL-6 production and improving survival in LPS models. Its potential applications include cancer treatment, particularly in tumors with uncontrolled CDK activity, and treatment of inflammatory conditions. It is commercially available as a research compound. |
| Molecular Formula |
C18H18CLN5O
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|---|---|
| Molecular Weight |
355.83
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| Exact Mass |
355.12
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| CAS # |
164658-13-3
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| PubChem CID |
644215
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.356g/cm3
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| Boiling Point |
630.6ºC at 760mmHg
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| Flash Point |
335.2ºC
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| Vapour Pressure |
9.02E-17mmHg at 25°C
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| Index of Refraction |
1.685
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| LogP |
3.224
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
25
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| Complexity |
389
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IYNDTACKOAXKBJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H18ClN5O/c19-14-3-1-4-15(12-14)23-18-22-9-6-16(24-18)13-5-8-21-17(11-13)20-7-2-10-25/h1,3-6,8-9,11-12,25H,2,7,10H2,(H,20,21)(H,22,23,24)
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| Chemical Name |
3-[[4-[2-(3-chloroanilino)pyrimidin-4-yl]pyridin-2-yl]amino]propan-1-ol
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| Synonyms |
CGP 60474 CGP-60474 CGP60474
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 50 mg/mL (~140.52 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8103 mL | 14.0517 mL | 28.1033 mL | |
| 5 mM | 0.5621 mL | 2.8103 mL | 5.6207 mL | |
| 10 mM | 0.2810 mL | 1.4052 mL | 2.8103 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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