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Olmutinib

🥰Excellent
Catalog No. T6918Cas No. 1353550-13-6
Alias HM61713, BI 1482694, HM61713, BI 1482694

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.

Olmutinib

Olmutinib

🥰Excellent
Purity: 99.27%
Catalog No. T6918Alias HM61713, BI 1482694, HM61713, BI 1482694Cas No. 1353550-13-6
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 SizePriceAvailabilityQuantity
2 mg$33In Stock
5 mg$52In Stock
10 mg$81In Stock
25 mg$139In Stock
50 mg$189In Stock
100 mg$297In Stock
200 mg$486In Stock
1 mL x 10 mM (in DMSO)$54In Stock
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Purity:99.27%
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Product Introduction

Bioactivity
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].
AliasHM61713, BI 1482694, HM61713, BI 1482694
Chemical Properties
Molecular Weight486.59
FormulaC26H26N6O2S
Cas No.1353550-13-6
SmilesCN1CCN(CC1)c1ccc(Nc2nc(Oc3cccc(NC(=O)C=C)c3)c3sccc3n2)cc1
Relative Density.1.336 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.0551 mL10.2756 mL20.5512 mL102.7559 mL
5 mM0.4110 mL2.0551 mL4.1102 mL20.5512 mL
10 mM0.2055 mL1.0276 mL2.0551 mL10.2756 mL
20 mM0.1028 mL0.5138 mL1.0276 mL5.1378 mL
DMSO
1mg5mg10mg50mg
50 mM0.0411 mL0.2055 mL0.4110 mL2.0551 mL
100 mM0.0206 mL0.1028 mL0.2055 mL1.0276 mL

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