| Size | Price | Stock | Qty |
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| Targets |
PP3 targets the epidermal growth factor receptor (EGFR) tyrosine kinase, inhibiting its kinase activity. EGFR is a receptor tyrosine kinase that plays a critical role in cell proliferation, survival, and differentiation, and is frequently overexpressed or mutated in various cancers. By inhibiting EGFR kinase activity, PP3 blocks downstream signaling pathways including the Ras-Raf-MEK-ERK and PI3K-Akt pathways. The compound's IC50 of 2.7 µM indicates moderate potency. It is used as a research tool to study EGFR-dependent cellular processes.
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| ln Vitro |
In vitro, PP3 demonstrates EGFR tyrosine kinase inhibitory activity with an IC50 of 2.7 µM. In cell-based assays, the compound inhibits EGFR phosphorylation and downstream signaling in cells expressing EGFR. PP3 has been shown to inhibit the proliferation of EGFR-dependent cancer cell lines. The compound's effects are concentration-dependent and correlate with its ability to inhibit EGFR kinase activity. As a research tool, PP3 is used to validate the role of EGFR in various cellular processes and to differentiate EGFR-dependent effects from those mediated by other kinases.
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| ln Vivo |
In vivo, PP3 has been evaluated in animal models of cancer and other EGFR-dependent diseases. Administration of the compound has been shown to inhibit tumor growth in xenograft models of EGFR-overexpressing cancers. The compound's in vivo efficacy is limited by its moderate potency and potential pharmacokinetic limitations. PP3 is primarily used as a research tool to study EGFR function in vivo, providing proof-of-concept for EGFR-targeted therapies. However, more potent EGFR inhibitors have been developed for clinical use.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for PP3 typically involve EGFR kinase inhibition studies using purified EGFR enzyme preparations. The enzyme is incubated with ATP, a peptide substrate, and varying concentrations of PP3. Kinase activity is measured by quantifying the phosphorylation of the peptide substrate using radioactive [γ-³²P]-ATP or by using antibody-based detection methods. IC50 values are calculated from dose-response curves. Selectivity profiling against other kinases is conducted to assess the compound's specificity.
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| Cell Assay |
In vitro cellular assays for PP3 utilize cancer cell lines expressing EGFR, such as A431 (overexpressing EGFR) or other EGFR-positive cell lines. Cells are treated with PP3 at concentrations ranging from 0.1 to 100 µM for 24-72 hours. EGFR phosphorylation is assessed by Western blotting using phospho-specific antibodies. Downstream signaling (ERK, Akt phosphorylation) is evaluated. Cell proliferation is measured using MTT or CCK-8 assays. Apoptosis is assessed by caspase activity or Annexin V staining. The compound's effects are compared to those of known EGFR inhibitors.
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| Animal Protocol |
In vivo animal experiments for PP3 typically involve mouse xenograft models using EGFR-overexpressing human cancer cell lines. The compound is administered via intraperitoneal or oral routes at doses ranging from 10 to 100 mg/kg. Tumor growth is monitored by caliper measurement, and tumor tissues are collected for analysis of EGFR phosphorylation and downstream signaling. Body weight and general health are monitored to assess tolerability. The compound's in vivo efficacy is compared to that of more potent EGFR inhibitors.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for PP3 are limited, as the compound is primarily used as a research tool rather than a drug candidate. As a small molecule with a molecular weight of 211.22 g/mol, PP3 is likely to have reasonable oral bioavailability. However, its moderate potency (IC50 of 2.7 µM) and potential metabolic instability may limit its in vivo efficacy. Detailed pharmacokinetic parameters including half-life, tissue distribution, and metabolism have not been extensively characterized.
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| Toxicity/Toxicokinetics |
Toxicity data for PP3 are limited. In animal studies, the compound has been administered at various doses without reports of severe toxicity. However, comprehensive toxicology studies have not been conducted. As with any experimental kinase inhibitor, potential off-target effects should be considered. The compound is intended for research use only and is not approved for human therapeutic applications.
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| Additional Infomation |
1-Phenylon-4-pyrazolo[3,4-d]pyrimidineamine is a cyclic compound belonging to the pyrazole class of compounds.
PP3 is a small molecule EGFR tyrosine kinase inhibitor with an IC50 of 2.7 µM. It has a molecular formula of C11H9N5 and a molecular weight of 211.22 g/mol. The compound is a structural analog of PP1 and is used as a research tool to study EGFR signaling pathways. PP3 is soluble in water, DMSO, methanol, ethanol, and DMF. It is intended for research use only and is not approved for human therapeutic applications. |
| Molecular Formula |
C11H9N5
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|---|---|
| Molecular Weight |
211.2227
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| Exact Mass |
211.085
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| CAS # |
5334-30-5
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| Related CAS # |
5334-30-5;
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| PubChem CID |
4879
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
364.0±35.0 °C at 760 mmHg
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| Melting Point |
214-217 °C
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| Flash Point |
173.9±25.9 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
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| Index of Refraction |
1.770
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| LogP |
1.59
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
16
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| Complexity |
241
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KKDPIZPUTYIBFX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H9N5/c12-10-9-6-15-16(11(9)14-7-13-10)8-4-2-1-3-5-8/h1-7H,(H2,12,13,14)
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| Chemical Name |
1-phenylpyrazolo[3,4-d]pyrimidin-4-amine
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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 : ≥ 100 mg/mL (~473.44 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.84 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 (11.84 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (11.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.7344 mL | 23.6720 mL | 47.3440 mL | |
| 5 mM | 0.9469 mL | 4.7344 mL | 9.4688 mL | |
| 10 mM | 0.4734 mL | 2.3672 mL | 4.7344 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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