| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg | |||
| Other Sizes |
| Targets |
WEHI-345 analog targets Src, a non-receptor tyrosine kinase that plays important roles in cell proliferation, migration, adhesion, and survival. Src is a member of the Src family kinases (SFKs) and is involved in various signaling pathways downstream of growth factor receptors, integrins, and other cell surface receptors. Src is frequently overexpressed or hyperactivated in cancer and is a validated therapeutic target. The WEHI-345 analog is extracted from patent WO/2012003544A1, compound example 71. The compound's mechanism of action involves inhibition of Src kinase activity, leading to modulation of downstream signaling pathways.
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| ln Vitro |
WEHI-345 analog demonstrates in vitro activity as a Src inhibitor. The compound is extracted from patent WO/2012003544A1, compound example 71. Its activity is characterized in kinase assays measuring the inhibition of Src kinase activity. The parent compound WEHI-345 is a potent and specific RIPK2 kinase inhibitor with an IC50 of 0.13 microM. The analog's activity is concentration-dependent, with inhibition observed at appropriate concentrations. The compound is used as a research tool to study Src signaling pathways and their role in various biological processes. Comprehensive in vitro activity data are available from the patent literature.
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| ln Vivo |
In vivo activity of WEHI-345 analog has not been extensively characterized in the public domain. As a Src inhibitor, the compound would be expected to have effects on cell proliferation, migration, and survival. Src inhibitors have been studied in various animal models of cancer and other diseases. However, comprehensive in vivo efficacy studies using the WEHI-345 analog specifically have not been widely published. The compound is primarily used as a research tool for in vitro studies. Further research is needed to determine the in vivo activity of this compound.
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| Enzyme Assay |
In vitro kinase assays for WEHI-345 analog involve measuring the inhibition of Src kinase activity. Recombinant Src kinase is incubated with varying concentrations of the test compound, ATP, and a peptide substrate. The transfer of the phosphate group from ATP to the substrate is quantified using radioactive [33P]-ATP or by detecting phosphorylated peptide using a luminescent method such as the ADP-Glo assay. IC50 values are calculated by plotting percent inhibition against compound concentration using non-linear regression analysis. Selectivity assays compare the compound's activity against a panel of other kinases. Each concentration is typically tested in duplicate or triplicate with appropriate positive controls (known Src inhibitors) and vehicle controls. The compound is extracted from patent WO/2012003544A1.
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| Cell Assay |
In vitro cellular assays for WEHI-345 analog are performed using cell lines that express Src, such as cancer cell lines. Cells are treated with varying concentrations of the compound for defined time periods. Src phosphorylation and downstream signaling (e.g., FAK, STAT3, ERK) are assessed by Western blot using phospho-specific antibodies. Cell proliferation and viability are measured using MTT or CellTiter-Glo assays. Cell migration and invasion are assessed using wound healing or transwell assays. Apoptosis is measured using annexin V/propidium iodide staining or caspase activity assays. Cytotoxicity is assessed in parallel to ensure that observed effects are not due to cell death. IC50 values for inhibition of cell proliferation or signaling are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies for WEHI-345 analog have not been extensively reported in the public domain. As a Src inhibitor, the compound could potentially be evaluated in mouse xenograft models of cancer or other disease models where Src plays a role. In such studies, the compound would be administered via oral gavage or intraperitoneal injection, and endpoints would include tumor growth, metastasis, and survival. However, comprehensive in vivo efficacy studies have not been widely published. The compound is primarily used as a research tool for in vitro studies.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of WEHI-345 analog have not been extensively characterized in the public domain. The compound has a molecular formula of C23H25N7O and a molecular weight of 415.49 g/mol. Its IUPAC name is N-[2-[4-amino-3-(4-methylphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]-2-methylpropyl]-3-methylpyridine-2-carboxamide. The compound is soluble in DMSO and other organic solvents. Comprehensive pharmacokinetic parameters including half-life, volume of distribution, clearance, and oral bioavailability have not been reported.
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| Toxicity/Toxicokinetics |
WEHI-345 analog is intended for laboratory research use only and has not undergone comprehensive toxicology testing. As a kinase inhibitor, the compound would be expected to have effects on cell signaling and proliferation. Standard in vitro cytotoxicity assays in cell lines are typically performed alongside efficacy studies to rule out nonspecific toxicity. In vivo, animals would be monitored for signs of toxicity if the compound were to be evaluated in animal studies. Comprehensive toxicological characterization including genotoxicity and repeated-dose toxicity studies has not been reported. The compound is not approved for human use and is strictly intended for research purposes.
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| References |
WO/2012003544A1
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| Additional Infomation |
WEHI-345 analog is a Src inhibitor extracted from patent WO/2012003544A1, compound example 71. WEHI-345, the parent compound, is a potent RIPK2 inhibitor with an IC50 of 0.13 microM. The analog has a molecular formula of C23H25N7O and a molecular weight of 415.49 g/mol. WEHI-345 analog has not entered clinical trials and is available for research purposes only.
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| Molecular Formula |
C23H25N7O
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|---|---|
| Molecular Weight |
415.490903615952
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| Exact Mass |
415.212
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| CAS # |
1354825-62-9
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| PubChem CID |
56602558
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| Appearance |
White to gray solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
688.0±55.0 °C at 760 mmHg
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| Flash Point |
369.9±31.5 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.678
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| LogP |
2.76
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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 |
5
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| Heavy Atom Count |
31
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| Complexity |
621
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC=C(C=C1)C2=NN(C3=NC=NC(=C23)N)C(C)(C)CNC(=O)C4=C(C=CC=N4)C
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| InChi Key |
ZCZGSEXBXXYQQC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H25N7O/c1-14-7-9-16(10-8-14)19-17-20(24)27-13-28-21(17)30(29-19)23(3,4)12-26-22(31)18-15(2)6-5-11-25-18/h5-11,13H,12H2,1-4H3,(H,26,31)(H2,24,27,28)
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| Chemical Name |
N-[2-[4-amino-3-(4-methylphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]-2-methylpropyl]-3-methylpyridine-2-carboxamide
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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 : ~30 mg/mL (~72.20 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 | 2.4068 mL | 12.0340 mL | 24.0680 mL | |
| 5 mM | 0.4814 mL | 2.4068 mL | 4.8136 mL | |
| 10 mM | 0.2407 mL | 1.2034 mL | 2.4068 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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