| Size | Price | Stock | Qty |
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| 25g |
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| 50g |
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| Other Sizes |
| Targets |
Pyrazoloadenine targets RET (REarranged during Transfection), a receptor tyrosine kinase that is activated in various cancers, including lung cancer. By inhibiting RET kinase activity, it blocks the downstream signaling pathways that promote tumor cell proliferation, survival, and migration. This makes it a valuable tool for studying RET-driven cancers and for developing targeted therapies.
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| ln Vitro |
Numerous protein kinases, including BTK (Bruton's tyrosine kinase), CDK1/2 (cyclin-dependent kinase 1/2), Src kinase, and RIPK1 (receptor-interacting protein kinase), are inhibited by pyrazoloadenine[1].
In vitro, Pyrazoloadenine has been shown to be a potent inhibitor of RET kinase activity. Its inhibitory activity is typically assessed using kinase assays that measure the phosphorylation of a substrate in the presence of the compound. These in vitro studies confirm its potential as a therapeutic agent for RET-driven cancers, including non-small cell lung cancer. |
| ln Vivo |
In vivo activity of Pyrazoloadenine has been studied in animal models of RET-driven cancers. It has shown anticancer activity by inhibiting tumor growth in xenograft models. Its efficacy is attributed to its ability to inhibit RET kinase signaling, thereby blocking tumor cell proliferation and survival. These studies provide evidence for its therapeutic potential.
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| Enzyme Assay |
Cell-free assays for Pyrazoloadenine typically involve measuring its inhibitory activity against RET kinase using a biochemical kinase assay. The compound's IC50 value is determined by measuring the phosphorylation of a peptide substrate in the presence of varying concentrations of the compound. These assays are used to characterize the compound's potency and selectivity against RET.
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| Cell Assay |
In vitro cellular assays are conducted to evaluate the functional activity of Pyrazoloadenine. RET-driven cancer cell lines are treated with the compound, and cell proliferation is measured to assess its anti-proliferative activity. RET phosphorylation is measured to assess the inhibition of RET kinase signaling. These assays confirm that Pyrazoloadenine effectively blocks RET-mediated cellular responses.
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| Animal Protocol |
In vivo animal experiments typically involve xenograft models of RET-driven cancers. Animals are administered the compound via oral gavage or injection. Tumor growth is monitored over time to assess efficacy. Pharmacokinetic studies are conducted to measure plasma concentrations of the compound. These studies provide evidence for the compound's anti-tumor activity.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Pyrazoloadenine are typical of a small molecule kinase inhibitor. Its molecular weight is 135.13 g/mol. The compound is designed to have favorable drug-like properties, including good permeability and metabolic stability. Pharmacokinetic studies in animal models involve measuring plasma concentrations of the compound over time to determine its half-life, clearance, and volume of distribution.
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| Toxicity/Toxicokinetics |
The toxicity profile of Pyrazoloadenine is not extensively documented, but it is likely to be similar to other RET kinase inhibitors. Common adverse effects may include fatigue, diarrhea, and hypertension. In preclinical studies, the compound has been shown to be well-tolerated at therapeutic doses, with a safety profile that supports its use in research.
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| References | |
| Additional Infomation |
Pyrazoloadenine is a research compound used to study RET-driven cancers, including lung cancer. It is a potent RET inhibitor with anticancer activity. The compound is not approved for therapeutic use and is intended for research purposes only.
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| Molecular Formula |
C5H5N5
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|---|---|
| Molecular Weight |
135.13
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| Exact Mass |
193.086
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| CAS # |
2380-63-4
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| PubChem CID |
75420
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| Appearance |
White to light brown solid powder
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| Density |
1.612g/cm3
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| Boiling Point |
431.1ºC at 760mmHg
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| Melting Point |
>325 °C(lit.)
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| Flash Point |
244.4ºC
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| LogP |
0.516
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
10
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| Complexity |
127
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=NNC2=NC=NC(=C21)N
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| InChi Key |
LHCPRYRLDOSKHK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C5H5N5/c6-4-3-1-9-10-5(3)8-2-7-4/h1-2H,(H3,6,7,8,9,10)
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| Chemical Name |
1H-pyrazolo[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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 7.4003 mL | 37.0014 mL | 74.0028 mL | |
| 5 mM | 1.4801 mL | 7.4003 mL | 14.8006 mL | |
| 10 mM | 0.7400 mL | 3.7001 mL | 7.4003 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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