Reagenti e strumenti per immunologia, biologia cellulare e biologia molecolare

Olmutinib [1353550-13-6]

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Cat# T6918-10mg

Size : 10mg

Marca : TargetMol

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Olmutinib

(Synonyms: HM61713, BI 1482694, HM61713, BI 1482694, 1802181-20-9) Copy Product Info

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.

Cas No. 1353550-13-6

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

Batch Information

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Purity:99.63%

Color:White

Resource Download

COA HNMR LCMS HPLC

Product Information

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	EGFR L858R/T790M:10 nM (cell assay), BTK:13.9 nM, EGFR (exon 19 deletion):9.2 nM (cell assay)
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].
Synonyms	HM61713, BI 1482694, HM61713, BI 1482694, 1802181-20-9

Chemical Properties

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 & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 22 mg/mL (45.21 mM), Sonication is recommended.

DMSO: 250 mg/mL (513.78 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

In Vivo Formulation

10% DMSO+90% Saline: < 10 mg/mL (20.55 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 10 mg/mL (20.55 mM), Solution.

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

Ethanol/DMSO

	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

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the .label-data{font-weight:bold;min-width:100px;}.label-data,.data{display:inline-block;min-width:100px;}.description table{word-break:break-all;}.description table td{min-width:200px;}