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Olmutinib (BI1482694) is a Novel Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $30 | In Stock | In Stock | |
| 5 mg | $52 | In Stock | In Stock | |
| 10 mg | $85 | In Stock | In Stock | |
| 25 mg | $133 | In Stock | In Stock | |
| 50 mg | $195 | In Stock | In Stock | |
| 100 mg | $297 | In Stock | In Stock | |
| 200 mg | $488 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $57 | In Stock | In Stock |
| Description | Olmutinib (BI1482694) is a Novel Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor |
| Targets&IC50 | EGFR (exon 19 deletion):9.2 nM (Cell Assay), EGFR L858R/T790M:10 nM (cell Assay) |
| In vitro | Olmutinib at 3 μM significantly reversed drug resistance mediated by ABCG2, but not by ABCB1 and ABCC1, by antagonizing the drug efflux function in ABCG2-overexpressing cells.?In addition, olmutinib at reversal concentration affected neither the protein expression level nor the localization of ABCG2.?The results observed from the accumulation/efflux study of olmutinib showed that olmutinib reversed ABCG2-mediated MDR with an increasing intracellular drug accumulation due to inhibited drug efflux.?We also had consistent results with the ATPase assay that olmutinib stimulated ATPase activity of ABCG2 up to 3.5-fold.?Additionally, the molecular interaction between olmutinib and ABCG2 was identified by docking simulation.?Olmutinib not only interacts directly with ABCG2 but also works as a competitive inhibitor of the transport protein[1] |
| Synonyms | HM61713, BI1482694 |
| Molecular Weight | 486.59 |
| Formula | C26H26N6O2S |
| Cas No. | 1802181-20-9 |
| Smiles | O=C(C=C)NC=1C=CC=C(OC2=NC(=NC=3C=CSC23)NC4=CC=C(C=C4)N5CCN(C)CC5)C1 |
| Relative Density. | no data available |
| Color | White |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 55 mg/mL (113.03 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (10.28 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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