Cat. No.: HY-19730

Olmutinib

(Synonyms: HM61713; BI 1482694)

12 Cited Publications

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Based on 12 publication(s) in Google Scholar

Olmutinib (HM61713; BI-1482694) is an orally active and irreversible third EGFR tyrosine kinase inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib is used for NSCLC.

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Pureté: 99.49%
CAS No.: 1353550-13-6
Formule: C₂₆H₂₆N₆O₂S
Masse moléculaire:486.59

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Olmutinib Chemical Structure

CAS No.: 1353550-13-6

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Essai clinique
Chemical Information
Publications (12)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Olmutinib (HM61713; BI-1482694) is an orally active and irreversible third EGFR tyrosine kinase inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib is used for NSCLC^[1]^[2].

IC₅₀ & Target^[1]

EGFR^{Exon 19 deletion}

9.2 nM (IC₅₀, Cell Assay)

EGFR^L858R/T790M

10 nM (IC₅₀, Cell Assay)

Voir tous les produits spécifiques à Isoform EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	5.29 μM Compound: Olmutinib	Antiproliferative activity against human A-431 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human A-431 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
A549	IC₅₀	0.028 μM Compound: Olmutinib	Antiproliferative activity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32402937]
A549	IC₅₀	4.29 μM Compound: Olmutinib	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
A549	IC₅₀	4.29 μM Compound: Olmutinib	Antiproliferation activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferation activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32912435]
HeLa	IC₅₀	9.27 μM Compound: Olmutinib	Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
HeLa	IC₅₀	9.27 μM Compound: Olmutinib	Antiproliferation activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferation activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32912435]
L02	IC₅₀	0.026 μM Compound: Olmutinib	Cytotoxicity against human L0-2 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human L0-2 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32402937]
L02	IC₅₀	25.48 μM Compound: Olmutinib	Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
L02	IC₅₀	25.76 μM Compound: Olmutinib	Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32912435]
MCF7	IC₅₀	6.9 μM Compound: Olmutinib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
MCF7	IC₅₀	6.9 μM Compound: Olmutinib	Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32912435]
NCI-H1975	IC₅₀	0.52 μM Compound: Olmutinib	Antiproliferation activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutation assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferation activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutation assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32912435]
NCI-H1975	IC₅₀	10 nM Compound: HM61713	Inhibition of EGFR L858R/T790M double mutant in human NCI-H1975 cells assessed as suppression of cell proliferation Inhibition of EGFR L858R/T790M double mutant in human NCI-H1975 cells assessed as suppression of cell proliferation	[PMID: 26968253]
NCI-H1975	IC₅₀	520.5 nM Compound: Olmutinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell viability measured after 72 hrs by MTT assay	[PMID: 32679450]
NCI-H1975	IC₅₀	9.61 μM Compound: Olmutinib	Antiproliferative activity against human H1975 cells harboring EGFR L858R/T790M double mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human H1975 cells harboring EGFR L858R/T790M double mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32402937]
PC-9	IC₅₀	16.51 μM Compound: Olmutinib	Antiproliferative activity against human PC9 cells harboring EGFRdel19 mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human PC9 cells harboring EGFRdel19 mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32402937]

In Vitro

Olmutinib potently inhibits EGFR in HCC827 cells expressing EGFR^DEL19 (IC₅₀=9.2 nM) and H1975 cells expressing EGFR^L858R/T790M (IC₅₀=10 nM). In contrast, the IC₅₀ of olmutinib against cells expressing EGFR^WT is 2225 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1353550-13-6
Appearance Solid
Masse moléculaire 486.59
Formule C₂₆H₂₆N₆O₂S
Color Light yellow to yellow
SMILES

C=CC(NC1=CC=CC(OC2=C3C(C=CS3)=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1)=O
Synonyms

HM61713; BI 1482694
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (12)

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Acta Pharm Sin B

Olmutinib (HM61713) reversed multidrug resistance by inhibiting the activity of ATP-binding cassette subfamily G member 2 in vitro and in vivo. [Abstract]

2018 Jul;8(4):563-574. PMID: 30109181

Olmutinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2018 Jul;8(4):563-574. [Abstract]

The protein levels of ABCG2 in MDR cells after different concentrations Olmutinib stimulation for 48 h are measured by Western blot analysis (GAPDH as loading control).
J Pharm Anal

Synergistic effects of methyl 2-cyano-3,11-dioxo-18beta-olean-1,-12-dien-30-oate and erlotinib on erlotinib-resistant non-small cell lung cancer cells. [Abstract]

2021 Dec;11(6):799-807. PMID: 35028186
Mol Syst Biol

Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]

2024 Jan;20(1):28-55. PMID: 38177929
RSC Adv

Investigation of the metabolic stability of olmutinib by validated LC-MS/MS: quantification in human plasma. [Abstract]

2018 Dec 4;8(70):40387-40394. PMID: 35558213
Rheumatology (Oxford)

Autophagy inhibitors block pathogenic NET release in immune-mediated inflammatory disease without impairing host defence. [Abstract]

2025 Aug 13:keaf437. PMID: 40802538
Biomedicines

Extracellular Vesicles and Exosomes: Novel Insights and Perspectives on Lung Cancer from Early Detection to Targeted Treatment. [Abstract]

2024 Jan 7;12(1):123. PMID: 38255228
J Sep Sci

Detection and characterization of olmutinib reactive metabolites by LC-MS/MS: Elucidation of bioactivation pathways. [Abstract]

2020 Feb;43(4):708-718. PMID: 31788977
Biochem Biophys Res Commun

2026 Feb 12:800:153165. PMID: 41548485
J Biomol Struct Dyn

Spectroscopic, molecular docking and dynamic simulation studies of binding between the new anticancer agent olmutinib and human serum albumin. [Abstract]

2022;40(24):14236-14246. PMID: 34766879
Med Sci Monit

Olmutinib Reverses Doxorubicin Resistance in ETS1-Overexpressing Leukemia Cells. [Abstract]

2020 Aug 24:26:e924922. PMID: 32830792
bioRxiv

Scalable longitudinal imaging and transcriptomics of cells in dynamic enclosures. [Abstract]

2026 May 8:2026.05.05.723030. PMID: 42146668
Patent

US20220177473A1.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (205.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0551 mL

10.2756 mL

20.5512 mL

5 mM

0.4110 mL

2.0551 mL

4.1102 mL

10 mM

0.2055 mL

1.0276 mL

2.0551 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 6.25 mg/mL (12.84 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 6.25 mg/mL (12.84 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 6.25 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 6.25 mg/mL (12.84 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 6.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (273 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Kim ES, et al. Olmutinib: First Global Approval. Drugs. 2016 Jul;76(11):1153-7. [Content Brief]

[2]. Mohamed W. Attwa, et al. Detection and characterization of olmutinib reactive metabolites by LC‐MS/MS: Elucidation of bioactivation pathways. Journal of Separation science. 18 November 2019.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0551 mL	10.2756 mL	20.5512 mL	51.3780 mL
	5 mM	0.4110 mL	2.0551 mL	4.1102 mL	10.2756 mL
	10 mM	0.2055 mL	1.0276 mL	2.0551 mL	5.1378 mL
	15 mM	0.1370 mL	0.6850 mL	1.3701 mL	3.4252 mL
	20 mM	0.1028 mL	0.5138 mL	1.0276 mL	2.5689 mL
	25 mM	0.0822 mL	0.4110 mL	0.8220 mL	2.0551 mL
	30 mM	0.0685 mL	0.3425 mL	0.6850 mL	1.7126 mL
	40 mM	0.0514 mL	0.2569 mL	0.5138 mL	1.2844 mL
	50 mM	0.0411 mL	0.2055 mL	0.4110 mL	1.0276 mL
	60 mM	0.0343 mL	0.1713 mL	0.3425 mL	0.8563 mL
	80 mM	0.0257 mL	0.1284 mL	0.2569 mL	0.6422 mL
	100 mM	0.0206 mL	0.1028 mL	0.2055 mL	0.5138 mL

Keywords

Olmutinib

12 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Olmutinib

Voir tous les produits spécifiques à Isoform EGFR

Activité biologique

Chemical Information

Publications (12)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Olmutinib Related Classifications

HY-19730 Related Classifications