EGFR-IN-8


Catalog No. Size PriceQuantity
M27697-C Contact sales@xcessbio.com for quotation $100Unavailable

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.

Product information

CAS Number: 2407957-87-1

Molecular Weight: 662.02

Formula: C32H23ClF3N7O4

Chemical Name: N-(3-chloro-4-{5-[3-({[4-cyclopropaneamido-3-(trifluoromethyl)phenyl]carbamoyl}amino)phenyl]-1,2,4-oxadiazol-3-yl}phenyl)pyridine-3-carboxamide

Smiles: O=C(NC1C=C(Cl)C(=CC=1)C1=NOC(=N1)C1C=C(C=CC=1)NC(=O)NC1=CC(=C(C=C1)NC(=O)C1CC1)C(F)(F)F)C1=CN=CC=C1

InChiKey: IIUNSVLRVWGJRM-UHFFFAOYSA-N

InChi: InChI=1S/C32H23ClF3N7O4/c33-25-15-22(38-29(45)19-4-2-12-37-16-19)8-10-23(25)27-42-30(47-43-27)18-3-1-5-20(13-18)39-31(46)40-21-9-11-26(24(14-21)32(34,35)36)41-28(44)17-6-7-17/h1-5,8-17H,6-7H2,(H,38,45)(H,41,44)(H2,39,40,46)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 8.33 mg/mL (12.58 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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.

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.

Products are for research use only. Not for human use.

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