EGFR-IN-5

Name: EGFR-IN-5
Brand: MedChemExpress
SKU: HY-111415
Rating: 4.5 (1 reviews)

Cat. No.: HY-111415 Purity: 99.49%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

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.

For research use only. We do not sell to patients.

EGFR-IN-5 Chemical Structure

CAS No. : 2225887-26-1

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All EGFR Isoform Specific Products:

View All Isoforms

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

Biological Activity
Purity & Documentation
References
Customer Review

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)

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]
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]

Molecular Weight

571.69

Formula

C₃₁H₃₈FN₉O

CAS No.

2225887-26-1

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

Molarity Calculator
Dilution Calculator

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: ≥ 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

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.

Purity & Documentation

Purity: 99.49%

Select Batch:

Data Sheet (271 KB) SDS (251 KB)

COA (249 KB) HNMR (268 KB) CNMR (263 KB) RP-HPLC (260 KB) LCMS (130 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

EGFR-IN-5 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:

EGFR-IN-52225887-26-1EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

EGFR-IN-5

Customer Review

EGFR-IN-5 Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All EGFR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

EGFR-IN-5 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report