| Size | Price | Stock | Qty |
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| 10mg |
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CGP60474 (CGP-60474) is a novel and potent CDK1/2 (cyclin-dependent kinases) with IC50 value of ~17 nM. Also acts as a Protein Kinase C (PKC) inhibitor. It inhibits CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T with IC50s of 26, 3, 4, 216, 10, 200 and 13 nM, respectively.
| 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].
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|---|---|
| ln Vivo |
In the LPS endotoxemia paradigm, CGP-60474 (10?mg/kg; ip) reduces IL-6 levels and increases survival [2].
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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. |
| References |
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| Additional Infomation |
3-[[4-[2-(3-chloroanilino)-4-pyrimidinyl]-2-pyridinyl]amino]-1-propanol is a substituted aniline.
|
| 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)
|
| 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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