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- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Manabe A, .et al. Upregulation of transient receptor potential melastatin 6 channel expression by rosiglitazone and all-trans-retinoic acid in erlotinib-treated renal tubular epithelial cells, J Cell Physiol, 2018, Nov 21 PMID: 30461012
- Yui Takashina, .et al. Sodium Citrate Increases Expression and Flux of Mg2+ Transport Carriers Mediated by Activation of MEK/ERK/c-Fos Pathway in Renal Tubular Epithelial Cells, Nutrients, 2018, Oct; 10(10): 1345 PMID: 30241394
- Furukawa C, .et al. Up-Regulation of Transient Receptor Potential Melastatin 6 Channel Expression by Tumor Necrosis Factor-α in the Presence of Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor, J Cell Physiol, 2017, Oct;232(10):2841-2850 PMID: 27925186
- Xiaoyu Yang, .et al. Knockdown delta-5-desaturase promotes the formation of a novel free radical byproduct from COX-catalyzed ω-6 peroxidation to induce apoptosis and sensitize pancreatic cancer cells to chemotherapy drugs, Free Radic Biol Med, 2016, Aug; 97: 342-350 PMID: 27368132
Biological Activity
Erlotinib is an epidermal growth factor receptor inhibitor (EGFR inhibitor). Erlotinib HCl was approved. Erlotinib binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. For the signal to be transmitted, two EGFR molecules need to come together to form a homodimer. These then use the molecule of ATP to trans-phosphorylate each other on tyrosine residues, which generates phosphotyrosine residues, recruiting the phosphotyrosine-binding proteins to EGFR to assemble protein complexes that transduce signal cascades to the nucleus or activate other cellular biochemical processes. When erlotinib binds to EGFR, formation of phosphotyrosine residues in EGFR is not possible and the signal cascades are not initiated.
| In vitro (25°C) | DMSO | 68 mg/mL (172.83 mM) | |
| Water | Insoluble | ||
| Ethanol | Warmed: 13 mg/mL | ||
| In vivo | 5% DMSO+30% PEG 300+5% Tween 80+ddH2O | 5 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 | 25.42 mL | 127.08 mL | 254.17 mL |
| 0.5 mM | 5.08 mL | 25.42 mL | 50.83 mL |
| 1 mM | 2.54 mL | 12.71 mL | 25.42 mL |
| 5 mM | 0.51 mL | 2.54 mL | 5.08 mL |
*The above data is based on the productmolecular weight 393.443. 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 | A11416 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 183321-74-6 |
| Formula | C22H23N3O4 |
| M. Wt | 393.443 |
| Purity | >98% |
| Synonyms | CP-358,774, CP-358774, CP358774, OSI-774, OSI 774, OSI774, Erlotinib free base. |
| SMILES | COCCOC1=CC2=NC=NC(NC3=CC=CC(C#C)=C3)=C2C=C1OCCOC |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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