HER2-IN-15
HER2-IN-15 (Compound 1) is an inhibitor for HER2, which inhibits the Her YVMA exon 20 insertion mutation (HER2 YVMA) with an IC50 <200 nM. HER2-IN-15 inhibits proliferation of HER2 YVMA mutated BaF3 cells with an IC50 <200 nM and amliorates non-small-cell lung cancer (NSCLC).
For research use only. We do not sell to patients.
- CAS No.: 3031412-82-2
- Formula: C28H29N9O2
- Molecular Weight:523.59
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All EGFR Isoforms
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Biological Activity
Description
IC50 & Target
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Her2 exon 20 YVMA insertion <200 nM (IC50) |
Chemical Information
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CAS No. 3031412-82-2
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Molecular Weight 523.59
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Formula C28H29N9O2
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SMILES
CC1=CC(NC2=NC=NN3C=CC(C4CN(C4)C(/C=C/CN(C)C)=O)=C23)=CC=C1OC5=CC6=NC=NN6C=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (95.49 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
Purity & Documentation
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9099 mL | 9.5495 mL | 19.0989 mL | 47.7473 mL |
| 5 mM | 0.3820 mL | 1.9099 mL | 3.8198 mL | 9.5495 mL | |
| 10 mM | 0.1910 mL | 0.9549 mL | 1.9099 mL | 4.7747 mL | |
| 15 mM | 0.1273 mL | 0.6366 mL | 1.2733 mL | 3.1832 mL | |
| 20 mM | 0.0955 mL | 0.4775 mL | 0.9549 mL | 2.3874 mL | |
| 25 mM | 0.0764 mL | 0.3820 mL | 0.7640 mL | 1.9099 mL | |
| 30 mM | 0.0637 mL | 0.3183 mL | 0.6366 mL | 1.5916 mL | |
| 40 mM | 0.0477 mL | 0.2387 mL | 0.4775 mL | 1.1937 mL | |
| 50 mM | 0.0382 mL | 0.1910 mL | 0.3820 mL | 0.9549 mL | |
| 60 mM | 0.0318 mL | 0.1592 mL | 0.3183 mL | 0.7958 mL | |
| 80 mM | 0.0239 mL | 0.1194 mL | 0.2387 mL | 0.5968 mL |