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Olmutinib

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Purity:99.27%

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COA HPLC HNMR LCMS

Olmutinib

Catalog No. T6918Cas 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.

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Pack Size	Price	Availability
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

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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.
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, BI 1482694, HM61713

Chemical Properties

Molecular Weight	486.59
Formula	C26H26N6O2S
Cas No.	1353550-13-6

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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

DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	2.0551 mL	10.2756 mL	20.5512 mL	102.7559 mL
5 mM	0.4110 mL	2.0551 mL	4.1102 mL	20.5512 mL
10 mM	0.2055 mL	1.0276 mL	2.0551 mL	10.2756 mL
20 mM	0.1028 mL	0.5138 mL	1.0276 mL	5.1378 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0411 mL	0.2055 mL	0.4110 mL	2.0551 mL
100 mM	0.0206 mL	0.1028 mL	0.2055 mL	1.0276 mL

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

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mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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