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| Targets |
PD166326 targets Src and Abl tyrosine kinases as a dual inhibitor. It has IC50 values of 6 nM for Src kinase and 8 nM for Abl tyrosine kinase. The compound is an ATP-competitive inhibitor belonging to the pyrido[2,3-d]pyrimidine class. By inhibiting Bcr-Abl and Src signaling, PD166326 induces apoptosis and inhibits proliferation in Bcr-Abl-positive cells.
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| ln Vitro |
In vitro, PD166326 potently inhibits Src kinase with an IC50 of 6 nM and Abl tyrosine kinase with an IC50 of 8 nM. It induces apoptosis and inhibits proliferation in Bcr-Abl-positive cells, making it a valuable compound for cancer research. The compound is used to explore resistance mechanisms and validate kinase targets in oncology.
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| ln Vivo |
In vivo, PD166326 alleviates splenomegaly and prolongs survival in a mouse model of chronic myeloid leukemia. The compound is orally active and has shown efficacy in preclinical models of Bcr-Abl-positive leukemia. These results support its potential as a therapeutic agent for CML.
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| Enzyme Assay |
Specific cell-free enzyme/receptor binding assay protocols for PD166326 involve kinase activity assays using purified Src and Abl recombinant proteins. IC50 values of 6 nM (Src) and 8 nM (Abl) are determined by measuring inhibition of kinase-mediated phosphorylation of peptide substrates using radiolabeled ATP or luminescent kinase assays.
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| Cell Assay |
In vitro cell-based assays for PD166326 use Bcr-Abl-positive leukemia cell lines. Cells are treated with PD166326, and cell proliferation is measured using MTT or CellTiter-Glo assays. Apoptosis is assessed by Annexin V staining or caspase activation. Bcr-Abl and Src signaling inhibition is confirmed by Western blot analysis of downstream targets.
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| Animal Protocol |
In vivo animal studies for PD166326 have been conducted in a mouse model of chronic myeloid leukemia. Mice bearing Bcr-Abl-positive tumors are treated with PD166326 orally, and endpoints include splenomegaly alleviation and survival prolongation. Tumor growth inhibition and pharmacodynamic markers are also assessed.
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| ADME/Pharmacokinetics |
PD166326 has a molecular formula of C21H16Cl2N4O2 and a molecular weight of approximately 427.28 g/mol. The chemical name is 6-(2,6-dichlorophenyl)-2-((3-(hydroxymethyl)phenyl)amino)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one. It has a UNII of 0H77F2T4U3. Purity is ≥95%.
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| Toxicity/Toxicokinetics |
Specific toxicological data for PD166326 are not detailed in the available literature. The compound is classified for research use only and is not intended for human therapeutic applications. As a Src/Abl kinase inhibitor, potential toxicities may relate to effects on normal cell proliferation and signaling.
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| References |
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| Additional Infomation |
PD166326 (CAS 185039-91-2) is an orally active, ATP-competitive dual Src/Abl kinase inhibitor with IC50s of 6 nM (Src) and 8 nM (Abl). It induces apoptosis in Bcr-Abl-positive cells and alleviates splenomegaly and prolongs survival in a CML mouse model. No clinical trial data are available.
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| Molecular Formula |
C21H16CL2N4O2
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|---|---|
| Molecular Weight |
427.28334
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| Exact Mass |
426.065
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| CAS # |
185039-91-2
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| PubChem CID |
447700
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
646.3±65.0 °C at 760 mmHg
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| Flash Point |
344.7±34.3 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.706
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| LogP |
3.04
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
624
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZIQFYVPVJZEOFS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H16Cl2N4O2/c1-27-19-13(9-15(20(27)29)18-16(22)6-3-7-17(18)23)10-24-21(26-19)25-14-5-2-4-12(8-14)11-28/h2-10,28H,11H2,1H3,(H,24,25,26)
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| Chemical Name |
6-(2,6-dichlorophenyl)-2-[3-(hydroxymethyl)anilino]-8-methylpyrido[2,3-d]pyrimidin-7-one
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| Synonyms |
PD 166326; PD166326; PD166326
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~100 mg/mL (~234.04 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3404 mL | 11.7019 mL | 23.4039 mL | |
| 5 mM | 0.4681 mL | 2.3404 mL | 4.6808 mL | |
| 10 mM | 0.2340 mL | 1.1702 mL | 2.3404 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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