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Purity: ≥98%
PD166866, a member of a new structural class of tyrosine kinase inhibitors, the 6-aryl-pyrido[2,3-d]pyrimidines, is a a new nanomolar potent and selective small molecule inhibitor of FGFR (fibroblast growth factor-1 receptor) tyrosine kinase inhibitor with an IC50 of 52.4 nM. In NIH 3T3 cells expressing endogenous FGFR-1 and in L6 cells overexpressing the human FGFR-1 tyrosine kinase, PD 166866 is a strong inhibitor of FGFR autophosphorylation. Additionally, in L6 cells, PD 166866 prevents bFGF-induced tyrosine phosphorylation of the 44- and 42-kDa (ERK 1/2) mitogen-activated protein kinase isoforms. PD 166866 may be useful as an antiproliferative/antiangiogenic agent for treating conditions like tumor growth and atherosclerotic plaque neovascularization.
| Targets |
FGFR1 (IC50 = 52.4 nM)
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| ln Vitro |
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| Enzyme Assay |
PD166866 is a novel small molecule inhibitor of FGFR (fibroblast growth factor-1 receptor) tyrosine kinase with an IC50 of 52.4 nM. It belongs to a new structural class of tyrosine kinase inhibitors, the 6-aryl-pyrido[2,3-d]pyrimidines. In L6 cells that overexpress the human FGFR-1 tyrosine kinase and NIH 3T3 cells that express endogenous FGFR-1, PD 166866 is a strong inhibitor of FGFR autophosphorylation. Furthermore, PD 166866 prevents L6 cells' bFGF-induced tyrosine phosphorylation of the 44- and 42-kDa (ERK 1/2) mitogen-activated protein kinase isoforms. For therapeutic targets like tumor growth and atherosclerotic plaque neovascularization, PD 166866 has potential application as an antiproliferative/antiangiogenic agent.
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| Cell Assay |
After HeLa cells are exposed to PD166866 for a full day, the growth medium is removed, PBS is used to wash the cells, and they are fixed for one hour at 25°C using a recently prepared paraformaldheyde solution (4% in PBS). After giving the samples another PBS wash, the endogenous oxidases were blocked for two minutes in the absence of light. After that, more PBS washes are performed, and the unspecified sites are blocked for an hour at 25°C. By using a polyclonal antibody to target the N-terminal proteolytic fragment for immunolocalization, PARP is demonstrated. After incubation at 4°C for 16 hours, the immunoreaction is exposed by a secondary anti-rabbit antibody. The samples are thoroughly cleaned in PBS and then incubated in solution ABC for half an hour. The samples are then incubated for 10 minutes in the dark after the addition of DAB (3,3'-Diaminobenzidine). After another wash, the plates are sealed and prepared for microscopic inspection.
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| Animal Protocol |
Female nude mice
20 mg/kg i.p. |
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| References |
| Molecular Formula |
C20H24N6O3
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| Molecular Weight |
396.44
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| Exact Mass |
396.19
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| Elemental Analysis |
C, 60.59; H, 6.10; N, 21.20; O, 12.11
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| CAS # |
192705-79-6
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| Related CAS # |
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| Appearance |
white solid powder
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| SMILES |
CC(C)(C)NC(=O)NC1=C(C=C2C=NC(=NC2=N1)N)C3=CC(=CC(=C3)OC)OC
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| InChi Key |
NHJSWORVNIOXIT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H24N6O3/c1-20(2,3)26-19(27)25-17-15(8-12-10-22-18(21)24-16(12)23-17)11-6-13(28-4)9-14(7-11)29-5/h6-10H,1-5H3,(H4,21,22,23,24,25,26,27)
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| Chemical Name |
1-[2-amino-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]-3-tert-butylurea
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (2.52 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 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O: 0.5mg/mL Solubility in Formulation 4: 3.33 mg/mL (8.40 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; Need ultrasonic and warming and heat to 40°C. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5224 mL | 12.6122 mL | 25.2245 mL | |
| 5 mM | 0.5045 mL | 2.5224 mL | 5.0449 mL | |
| 10 mM | 0.2522 mL | 1.2612 mL | 2.5224 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.
Assessment of cell survival after treatment with PD166866.
Intracellular concentration of malonyl-dihaldehyde (MDA) after treatment with PD166866.J Exp Clin Cancer Res.2009 Dec 11;28:151. |
An extensive DNA damage is caused by treatment with PD166866.J Exp Clin Cancer Res.2009 Dec 11;28:151. |
Accumulation Poly-ADP-Ribose-Polymerase (PARP) in cells treated with PD166866 evidenced by imuno-histochemistry.J Exp Clin Cancer Res.2009 Dec 11;28:151. |
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