EGFR-IN-8

Name: EGFR-IN-8
Brand: MedChemExpress
SKU: HY-126320
Rating: 4.5 (1 reviews)

Cat. No.: HY-126320 Purity: 98.01%: FAQs
Data Sheet SDS COA Handling Instructions

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EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC.

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

EGFR-IN-8 Chemical Structure

CAS No. : 2407957-87-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 408	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 408	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 440	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1100	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1450	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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

Biological Activity
Purity & Documentation
References
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Description

EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC^[1].

IC₅₀ & Target

EGFR; c-Met^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.2 μM Compound: 48	Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31446247]
A549	IC₅₀	0.3 μM Compound: 48	Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31446247]
CL97	IC₅₀	0.5 μM Compound: 48	Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31446247]
CL97	IC₅₀	0.6 μM Compound: 48	Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31446247]
MDA-MB-231	IC₅₀	0.2 μM Compound: 48	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31446247]
NCI-H1975	IC₅₀	0.3 μM Compound: 48	Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31446247]
NCI-H1975	IC₅₀	0.3 μM Compound: 48	Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31446247]
PC-9	IC₅₀	0.5 μM Compound: 48	Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31446247]
PC-9	IC₅₀	0.6 μM Compound: 48	Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31446247]

In Vitro

EGFR-IN-8 (0-20 μM; 24-72 hours) exhibits a time- and dose-dependent inhibitory effect on the viability of A549, PC9, H1975, CL68, and CL97 cells at different time intervals, with IC₅₀ values ranging from 0.3 to 0.6 μM and 0.2-0.5 μM after 48 and 72 h of treatment respectively^[1].
EGFR-IN-8 (0-0.6 μM; 48 hours) suppresses the expression of EGFR and c-Met in these five cell lines irrespective of their mutational status^[1].

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

Cell Viability Assay^[1]

Cell Line:	A549, PC9, H1975, CL68, and CL97 cells
Concentration:	0-20 μM
Incubation Time:	24 hours, 48 hours, 72 hours
Result:	Showed inhibitory effects on different cells.

Western Blot Analysis^[1]

Cell Line:	A549, PC9, H1975, CL68, and CL97 cells
Concentration:	0-0.6 μM
Incubation Time:	48 hours
Result:	Decreased EGFR and c-Met expression.

In Vivo

EGFR-IN-8 (oral gavage; 50 and 150 mg/kg; once daily; 20 days) exhibits a dose-dependent suppression (29% and 60%, respectively) of H1975 xenograft tumor growth at 50 and 150 mg/kg^[1].

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

Animal Model:	Nude mice H1975 xenograft tumor model^[1]
Dosage:	50 and 150 mg/kg
Administration:	Oral gavage; 50 and 150 mg/kg; once daily; 20 days
Result:	Inhibited H1975 xenograft tumor growth.

Molecular Weight

662.02

Formula

C₃₂H₂₃ClF₃N₇O₄

CAS No.

2407957-87-1

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=CC(C(F)(F)F)=C(NC(C2CC2)=O)C=C1)NC3=CC=CC(C4=NC(C5=CC=C(NC(C6=CC=CN=C6)=O)C=C5Cl)=NO4)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 8.33 mg/mL (12.58 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	1.5105 mL	7.5526 mL	15.1053 mL
5 mM	0.3021 mL	1.5105 mL	3.0211 mL
10 mM	0.1511 mL	0.7553 mL	1.5105 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)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.01%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (247 KB) HNMR (287 KB) RP-HPLC (251 KB) MS (76 KB)

Handling Instructions (2659 KB)

References

[1]. Dokla EME, et al. 1,2,4-Oxadiazole derivatives targeting EGFR and c-Met degradation in TKI resistant NSCLC. Eur J Med Chem. 2019 Aug 9;182:111607. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.5105 mL	7.5526 mL	15.1053 mL	37.7632 mL
	5 mM	0.3021 mL	1.5105 mL	3.0211 mL	7.5526 mL
	10 mM	0.1511 mL	0.7553 mL	1.5105 mL	3.7763 mL

EGFR-IN-8 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-82407957-87-1EGFRc-Met/HGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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EGFR-IN-8

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EGFR-IN-8 Related Antibodies

Featured Recommendations

•Related Screening Libraries:

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Biological Activity

Purity & Documentation

References

Customer Review

EGFR-IN-8 Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

EGFR-IN-8 Related Classifications

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