| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
YS-67 targets the epidermal growth factor receptor (EGFR), a receptor tyrosine kinase that plays a critical role in cell proliferation, survival, and migration. EGFR is frequently overexpressed or mutated in various cancers, including non-small cell lung cancer. By inhibiting EGFR kinase activity with an IC50 of 5.2 nM, YS-67 suppresses downstream signaling pathways including the AKT pathway, leading to inhibition of cell proliferation and induction of apoptosis.
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| ln Vitro |
YS-67 shows potent in vitro activity as an EGFR inhibitor with an IC50 of 5.2 nM. The compound significantly inhibits p-EGFR and p-AKT, demonstrating effective inhibition of EGFR signaling. YS-67 inhibits the proliferation of A549, PC-9, and A431 cells with IC50 values of 4.1, 0.5, and 2.1 μM, respectively. The compound arrests the cell cycle at the G0/G1 phase and induces apoptosis.
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| ln Vivo |
In vivo activity of YS-67 has been suggested based on its potent in vitro EGFR inhibitory activity and antitumor effects. As an orally available compound, YS-67 is suitable for convenient administration via oral gavage. The compound is being investigated for the treatment of non-small cell lung cancer. However, detailed in vivo efficacy data have not been extensively reported in the available literature.
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| Enzyme Assay |
Non-cell-based kinase assays for YS-67 typically involve measuring the inhibition of recombinant EGFR kinase activity using a radioactive or fluorescence-based assay. A standard protocol includes incubating purified EGFR kinase with a peptide substrate and ATP in kinase buffer. YS-67 is added at various concentrations (0.001–100 nM), and the phosphorylation of the substrate is measured using a scintillation proximity assay or time-resolved fluorescence resonance energy transfer (TR-FRET). IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cellular assays for YS-67 typically involve EGFR-dependent cancer cell lines such as A549 (lung cancer), PC-9 (lung cancer), and A431 (epidermoid carcinoma). A representative protocol includes culturing cells in appropriate medium, treating with YS-67 at various concentrations (0.01–100 μM) for 48–72 hours, and assessing cell viability using MTT or CellTiter-Glo assays. To confirm on-target activity, p-EGFR and p-AKT levels are measured by Western blot. Cell cycle analysis and apoptosis assays are performed by flow cytometry.
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| Animal Protocol |
In vivo animal studies with YS-67 have not been extensively reported in the available literature. If conducted, a typical protocol would involve xenograft mouse models of non-small cell lung cancer (e.g., A549 or PC-9 xenografts), with administration of the compound via oral gavage at doses determined from pharmacokinetic studies, monitoring tumor growth and body weight, and harvesting tumors for analysis of p-EGFR and p-AKT levels by Western blot.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of YS-67 have not been extensively reported in the available literature. As an orally active small molecule with a molecular weight of 522.64 g/mol, it is expected to have reasonable oral bioavailability and tissue distribution. The compound is typically stored as a powder at -20°C. Further PK studies are needed to fully characterize its absorption, distribution, metabolism, and excretion profile.
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| Toxicity/Toxicokinetics |
As a research compound, YS-67 is not intended for human therapeutic use, and comprehensive toxicological data are limited to preclinical studies. Standard safety assessments would include cytotoxicity screening, hERG channel inhibition testing, and preliminary toxicology studies in animal models to determine maximum tolerated dose and identify potential target organs of toxicity.
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| References | |
| Additional Infomation |
YS-67 (CAS 2761327-15-3) is a potent, orally available, and selective EGFR inhibitor with an IC50 of 5.2 nM. The compound significantly inhibits p-EGFR and p-AKT and inhibits the proliferation of A549, PC-9, and A431 cells with IC50 values of 4.1, 0.5, and 2.1 μM, respectively. YS-67 arrests the cell cycle at the G0/G1 phase and induces apoptosis, and is being investigated for the treatment of non-small cell lung cancer.
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| Molecular Formula |
C32H34N4O3
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| Molecular Weight |
522.64
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| CAS # |
2761327-15-3
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| Appearance |
Light yellow to light brown solid powder
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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 :~20 mg/mL (~38.27 mM; with sonication (<60°C))
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (3.83 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 20.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then add 450 μL of physiological saline to make 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 mg/mL (3.83 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 20.0 mg/mL clear DMSO stock solution and add it to 900 μL corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9134 mL | 9.5668 mL | 19.1336 mL | |
| 5 mM | 0.3827 mL | 1.9134 mL | 3.8267 mL | |
| 10 mM | 0.1913 mL | 0.9567 mL | 1.9134 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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