Olmutinib (Synonyms: HM61713; BI 1482694)

Name: Olmutinib
Brand: MedChemExpress
SKU: HY-19730
Rating: 5.0 (11 reviews)

Cat. No.: HY-19730 Pureza: 99.49%: Ficha de datos
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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.

Para uso exclusivo en investigación. No vendemos a pacientes.

No. CAS : 1353550-13-6

Tamaño	Stock	Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	En stock	Estimated Time of Arrival: December 31
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1 g	Obtener un presupuesto

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Revisión del cliente

Based on 11 publication(s) in Google Scholar

Other Forms of Olmutinib:

Olmutinib hydrochloride Obtener un presupuesto

11 Publications Citing Use of MCE Olmutinib

: 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).

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas EGFR:

Ver todas las isoformas

EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Actividad biológica
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

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)

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.

Ensayo clínico

Peso molecular

486.59

Fòrmula

C₂₆H₂₆N₆O₂S

No. CAS

1353550-13-6

Appearance

Solid

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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Solvente y solubilidad

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Calculadora de molaridad
Calculadora de dilución

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Pureza y Documentación

Purity: 99.88%

Select Batch:

Ficha de datos (273 KB) SDS (393 KB)

COA (247 KB) HNMR (212 KB) LCMS (119 KB)

Instrucciones de manejo (2659 KB)

Referencias

[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.

Complete Stock Solution Preparation Table

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

Olmutinib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Olmutinib1353550-13-6HM61713 BI 1482694HM 61713HM-61713BI1482694BI 1482694BI-1482694EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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Olmutinib (Synonyms: HM61713; BI 1482694)

Revisión del cliente

Other Forms of Olmutinib:

Olmutinib Related Antibodies

11 Publications Citing Use of MCE Olmutinib

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas EGFR:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

Olmutinib Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

Olmutinib Related Classifications

Keywords:

Productos vistos recientemente:

Revisión del cliente

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SAFETY DATA SHEET (SDS)

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