| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
In the experiment, PP58 inhibits Src with subnanomolar IC50 values. PP58 can function as a titration reagent at greater concentrations of Src protein. PP58 matrix selectively reduces Src from total lysates by immunoblotting analysis using particular antisera, and when free inhibitor is present, it prevents binding to PP58 beads. On PP58 beads, FGFR1 receptor tyrosine kinase that was ectopically expressed was selectively retained. A novel affinity reagent for the purification of targets of pyrido[2,3-d]pyrimidine inhibitors in cells could be the PP58 matrix. Protein kinases from a wide range of families and groups are identified by PP58 affinity chromatography, proving that pyrido[2,3-d]pyrimidine inhibitors are not specific to a group of phylogenetically related members of the human kinome. For p38α and JNK2, the Ki values of PP58 are 3.8±1.9 nM and 0.32±0.04 μM, respectively. A number of protein kinases that lack this structural characteristic and have a much lower affinity for the pyrido[2,3-d]pyrimidine inhibitor PP58 can also be effectively purified using the PP58 affinity matrix. With an IC50 less than 10 nM, PP58 inhibits anisomycin-activated p38 in a dose-dependent manner. PP58 has a cellular IC50 value of about 3 nM and can effectively inhibit the production of TNF-α stimulated by LPS [1]. The T341M mutation eliminates sensitivity to PP58 inhibition by increasing the cellular IC50 value more than 1000 times to about 10 nM. Low nanomolar concentrations of PP58 effectively inhibited the cellular wild-type FGFR1 activity, while the FGFR1-V561M mutant showed a notable development of resistance. The IC50 value of PP58, which inhibits CSK activity, is roughly 100 nM (2].
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| ln Vivo |
In vivo, PP58 can show some selectivity at low nanomolar doses [1].
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| References |
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| Molecular Formula |
C₂₂H₁₉CL₂N₅O₂
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|---|---|
| Molecular Weight |
456.32
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| Exact Mass |
455.091
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| CAS # |
212391-58-7
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| PubChem CID |
5327904
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
663.7±65.0 °C at 760 mmHg
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| Flash Point |
355.2±34.3 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.681
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| LogP |
2.93
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
31
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| Complexity |
648
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MAXZESONWXTISA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H19Cl2N5O2/c1-29-20-13(11-16(21(29)30)19-17(23)3-2-4-18(19)24)12-26-22(28-20)27-14-5-7-15(8-6-14)31-10-9-25/h2-8,11-12H,9-10,25H2,1H3,(H,26,27,28)
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| Chemical Name |
2-[4-(2-aminoethoxy)anilino]-6-(2,6-dichlorophenyl)-8-methylpyrido[2,3-d]pyrimidin-7-one
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| Synonyms |
PP 58PP-58PP58
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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 : ~62.5 mg/mL (~136.97 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.56 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1914 mL | 10.9572 mL | 21.9144 mL | |
| 5 mM | 0.4383 mL | 2.1914 mL | 4.3829 mL | |
| 10 mM | 0.2191 mL | 1.0957 mL | 2.1914 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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