| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
VEGFR2 (IC50 = 19.32 nM)
WAY-340935 targets VEGFR2 (vascular endothelial growth factor receptor 2), a key receptor tyrosine kinase involved in tumor angiogenesis. By inhibiting VEGFR2 with an IC50 of 19.32 nM, it effectively targets VEGFR2-mediated signaling, which is critical for tumor angiogenesis, thereby inhibiting tumor growth and metastasis. |
|---|---|
| ln Vitro |
A series of novel 4-alkoxyquinazoline derivatives were prepared and synthesized and their biological activities were evaluated as potential inhibitors of vascular endothelial growth factor receptor 2 (VEGFR2). Of these compounds, compound 3j demonstrated the most potent inhibitory activities against VEGFR2 tyrosine kinase and cell proliferation, the IC50 values of this compound reaching up to 2.72 nM and 0.35 μM, respectively, compared with Tivozanib (3.40 nM and 0.38 μM). The obtained results, along with a 3D-QSAR study and molecular docking that was used for investigating the probable binding mode, could provide an important basis for further optimization of compound 3j as a potential tyrosine kinase inhibitor[1].
In vitro, WAY-340935 exhibits an IC50 of 19.32 nM for VEGFR2 inhibition. It produces anti-proliferative activity against the H460 cell line, which is mediated partly by its interaction with the VEGFR protein. The compound effectively targets VEGFR2-mediated signaling. |
| ln Vivo |
In vivo, WAY-340935 is expected to show efficacy in animal models of cancer by inhibiting VEGFR2-driven angiogenesis and tumor growth. Its ability to inhibit VEGFR2-mediated signaling suggests it could be effective in various cancer types where this pathway is active. However, specific in vivo efficacy data are not detailed in the available literature.
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| Enzyme Assay |
In vitro enzyme assays for WAY-340935 typically involve kinase activity assays using purified recombinant VEGFR2 enzyme. The compound is incubated with the enzyme, ATP, and a specific peptide substrate. The phosphorylation of the substrate is measured using techniques such as radioactive (33P-ATP) or luminescence-based detection methods. The IC50 value of 19.32 nM is determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for WAY-340935 are performed using cancer cell lines such as H460. Cells are treated with various concentrations of the compound, and cell proliferation is assessed using MTT or CellTiter-Glo assays. The anti-proliferative effect is measured to confirm the compound's activity.
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| Animal Protocol |
In vivo animal studies with WAY-340935 would typically be conducted in mouse xenograft models of cancer to evaluate its anti-angiogenic and antitumor efficacy. The compound would be administered orally or intraperitoneally, and tumor growth inhibition would be assessed. However, specific protocols are not detailed in the available literature.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of WAY-340935 are not extensively reported. It has a molecular weight of 315.16 and is soluble in DMSO at 10 mM. It is typically stored as a powder at -20°C for up to 3 years. Specific parameters such as oral bioavailability, half-life, and tissue distribution are not detailed.
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| Toxicity/Toxicokinetics |
The toxicity profile of WAY-340935 is not extensively reported in the available literature. As a research compound, it is for research use only and not for human therapeutic use. No specific toxicity data are detailed.
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| References | |
| Additional Infomation |
WAY-340935 (VEGFR2-IN-2, compound 6e) is a potent and specific VEGFR2 inhibitor with an IC50 of 19.32 nM. It is used in anti-cancer research, particularly for studying anti-angiogenic therapies. The compound is available for research purposes only.
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| Molecular Formula |
C15H11BRN2O
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|---|---|
| Molecular Weight |
315.16
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| Exact Mass |
314.00548
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| Elemental Analysis |
C, 57.16; H, 3.52; Br, 25.35; N, 8.89; O, 5.08
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| CAS # |
737818-56-3
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| PubChem CID |
2368291
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| Appearance |
White to off-white solid powder
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| LogP |
4.2
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
19
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| Complexity |
281
|
| Defined Atom Stereocenter Count |
0
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| SMILES |
N1=C2C(C=CC=C2)=C(OCC2=CC=C(Br)C=C2)N=C1
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| InChi Key |
DADJIQURPZZXBT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H11BrN2O/c16-12-7-5-11(6-8-12)9-19-15-13-3-1-2-4-14(13)17-10-18-15/h1-8,10H,9H2
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| Chemical Name |
4-[(4-bromophenyl)methoxy]quinazoline
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| Synonyms |
WAY-340935; WAY340935; WAY 340935; VEGFR2-IN-2; MLS000516729; CHEMBL1605411
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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 (~317.30 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.93 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 (7.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1730 mL | 15.8650 mL | 31.7299 mL | |
| 5 mM | 0.6346 mL | 3.1730 mL | 6.3460 mL | |
| 10 mM | 0.3173 mL | 1.5865 mL | 3.1730 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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