[CAS NO. 2407957-87-1]  EGFR-IN-8

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PRODUCTS SPECIFICATIONS [2407957-87-1]

Distributor
Catalog
AS951008
Brand
Arctom Scientific
CAS
2407957-87-1

DESCRIPTION [2407957-87-1]

Overview

MDL-
Molecular Weight662.02
Molecular FormulaC32H23ClF3N7O4
SMILESO=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

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

Summary

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]


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 IC 50 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] .

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] .

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.

Appearance

Solid


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)

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
* Please refer to the solubility information to select the appropriate solvent.