| Name | Olmutinib |
| Description | Olmutinib (HM61713, BI 1482694) is an orally available small molecule, a mutant-selective inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Olmutinib binds to and inhibits mutant forms of EGFR, thereby leading to cell death of EGFR-expressing tumor cells. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced as compared to non-selective EGFR inhibitors which also inhibit the EGFR wild-type form. |
| In vitro | HM61713 causes potent inhibition in cell lines H1975 (L858R and T790M) and HCC827 (exon 19 deletion). It has a low potency for NSCLC cell line H358 harboring wild-type EGFR (GI50 of 2225 nM)[1]. |
| In vivo | HM61713 has a half-life of over 24 h for EGFR inhibition. In the in vivo studies of xenograft models with grafts of H1975 and HCC827, HM61713 is active against the tumors without showing any side effects[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : 22 mg/mL (45.2 mM)
DMSO : 90 mg/mL (185 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | 1802181-20-9 | Olmutinib | HM-61713 | ErbB-1 | BI1482694 | inhibit | HM61713, BI1482694 | BI-1482694 | HER1 | EGFR | HM61713, BI-1482694 | Epidermal growth factor receptor | Inhibitor | HM 61713 |
| Inhibitors Related | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Afatinib Dimaleate | Erlotinib hydrochloride | Erlotinib | Neratinib | Chalcone | Genistein | Gefitinib |
| Related Compound Libraries | Apoptosis Compound Library | Cysteine Covalent Library | Cytokine Inhibitor Library | Approved Drug Library | Drug-induced Liver Injury (DILI) Compound Library | Tyrosine Kinase Inhibitor Library | Anti-Prostate Cancer Compound Library | Orally Active Compound Library | Covalent Inhibitor Library | Anti-Liver Cancer Compound Library |
United States
