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$0.00 - Shi P, .et al. The Third-Generation EGFR Inhibitor, Osimertinib, Promotes c-FLIP Degradation, Enhancing Apoptosis Including TRAIL-Induced Apoptosis in NSCLC Cells with Activating EGFR Mutations, Transl Oncol, 2019, Mar 8;12(5):705-713 PMID: 30856555
Biological Activity
Pelitinib (EKB-569) is a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity.
Targets
| Target | Value |
|---|---|
| EGFR | IC50: 38.5nM |
| Src | IC50: 282nM |
| MEK/ERK | IC50: 800nM |
| ErbB2 | IC50: 1.255μM |
| Raf | IC50: 3.353μM |
| c-Met | IC50: 4.1μM |
| CDK4 | IC50: >20μM |
| In vitro (25°C) | DMSO | 13 mg/mL (27.78 mM) | |
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | 30% PEG400/0.5% Tween80/5% propylene glycol | 30 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 21.37 mL | 106.86 mL | 213.72 mL |
| 0.5 mM | 4.27 mL | 21.37 mL | 42.74 mL |
| 1 mM | 2.14 mL | 10.69 mL | 21.37 mL |
| 5 mM | 0.43 mL | 2.14 mL | 4.27 mL |
*The above data is based on the productmolecular weight 467.9 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A10706 |
|---|---|
| Actions | Inhibitor |
| M. Wt | 467.9 |
| Formula | C24H23ClFN5O2 |
| Solubility | DMSO |
| Purity | >98% |
| Storage | at -20°C 3 years Powder |
| CAS No. | 257933-82-7 |
| Synonyms | WAY-EKB 569 |
| SMILES | CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)F)Cl)C#N)NC(=O)/C=C/CN(C)C |
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