Cat. No.: HY-111415

EGFR-IN-5

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Based on 1 Customer Validation

EGFR-IN-5 is a EGFR inhibitor with IC₅₀s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFR^L858R, EGFR^L858R/T790M, and EGFR^{L858R/T790M/C797S}, respectively.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté: 99.49%
CAS No.: 2225887-26-1
Formule: C₃₁H₃₈FN₉O
Masse moléculaire:571.69

Stockage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

EGFR-IN-5 Chemical Structure

CAS No.: 2225887-26-1

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Stock

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Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

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

Activité biologique

Description

EGFR-IN-5 is a EGFR inhibitor with IC₅₀s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFR^L858R, EGFR^L858R/T790M, and EGFR^{L858R/T790M/C797S}, respectively.

IC₅₀ & Target^[1]

EGFR

10.4 nM (IC₅₀)

EGFR^L858R

1.1 nM (IC₅₀)

EGFR^L858R/T790M

34 nM (IC₅₀)

EGFR^{L858R/T790M/C797S}

7.2 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	1.06 μM Compound: B30	Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay	[PMID: 29466773]
HCC827	IC₅₀	0.044 μM Compound: B30	Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant after 72 hrs by MTT assay	[PMID: 29466773]
HCC827	IC₅₀	0.04 μM Compound: 39	Antiproliferative activity against human HCC827 assessed as cell growth inhibition Antiproliferative activity against human HCC827 assessed as cell growth inhibition	[PMID: 33992931]
HCC827	IC₅₀	40 nM Compound: 23	Growth inhibition of human HCC827 cells Growth inhibition of human HCC827 cells	[PMID: 34323489]
NCI-H1975	IC₅₀	0.4 μM Compound: B30	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay	[PMID: 29466773]
NCI-H1975	IC₅₀	400 nM Compound: 23	Growth inhibition of human NCI-H1975 cells Growth inhibition of human NCI-H1975 cells	[PMID: 34323489]

Chemical Information

CAS No. 2225887-26-1
Appearance Solid
Masse moléculaire 571.69
Formule C₃₁H₃₈FN₉O
Color Light yellow to yellow
SMILES

OCC(CC1)CCN1C2=NC(NC3=CC=C(F)C=C3)=NC(C=N4)=C2C=C4NC5=NC=C(N6CCC(N(C)C)CC6)C=C5
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : ≥ 100 mg/mL (174.92 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

1.7492 mL

8.7460 mL

17.4920 mL

5 mM

0.3498 mL

1.7492 mL

3.4984 mL

10 mM

0.1749 mL

0.8746 mL

1.7492 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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: ≥ 2.08 mg/mL (3.64 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

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)
μL
Number of Animals Number of Animals

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 (271 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]. Zhang H, et al. Discovery of 2,4,6-trisubstitued pyrido[3,4-d]pyrimidine derivatives as new EGFR-TKIs. Eur J Med Chem. 2018 Mar 25;148:221-237. [Content Brief]

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7492 mL	8.7460 mL	17.4920 mL	43.7300 mL
	5 mM	0.3498 mL	1.7492 mL	3.4984 mL	8.7460 mL
	10 mM	0.1749 mL	0.8746 mL	1.7492 mL	4.3730 mL
	15 mM	0.1166 mL	0.5831 mL	1.1661 mL	2.9153 mL
	20 mM	0.0875 mL	0.4373 mL	0.8746 mL	2.1865 mL
	25 mM	0.0700 mL	0.3498 mL	0.6997 mL	1.7492 mL
	30 mM	0.0583 mL	0.2915 mL	0.5831 mL	1.4577 mL
	40 mM	0.0437 mL	0.2186 mL	0.4373 mL	1.0932 mL
	50 mM	0.0350 mL	0.1749 mL	0.3498 mL	0.8746 mL
	60 mM	0.0292 mL	0.1458 mL	0.2915 mL	0.7288 mL
	80 mM	0.0219 mL	0.1093 mL	0.2186 mL	0.5466 mL
	100 mM	0.0175 mL	0.0875 mL	0.1749 mL	0.4373 mL

Keywords

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EGFR-IN-5

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Voir tous les produits spécifiques à Isoform EGFR

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

EGFR-IN-5

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Voir tous les produits spécifiques à Isoform EGFR

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

EGFR-IN-5 Related Classifications

HY-111415 Related Classifications