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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $33 | In Stock | |
5 mg | $52 | In Stock | |
10 mg | $81 | In Stock | |
25 mg | $139 | In Stock | |
50 mg | $189 | In Stock | |
100 mg | $297 | In Stock | |
200 mg | $486 | In Stock | |
1 mL x 10 mM (in DMSO) | $54 | In Stock |
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. |
Targets&IC50 | BTK:13.9 nM |
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]. |
Alias | HM61713, BI 1482694, HM61713, BI 1482694 |
Molecular Weight | 486.59 |
Formula | C26H26N6O2S |
Cas No. | 1353550-13-6 |
Smiles | CN1CCN(CC1)c1ccc(Nc2nc(Oc3cccc(NC(=O)C=C)c3)c3sccc3n2)cc1 |
Relative Density. | 1.336 g/cm3 (Predicted) |
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) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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