EGFR-IN-11

EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFRL858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1.

Product information

CAS Number: 2463200-44-2

Molecular Weight: 573.71

Formula: C29H35N9O2S

Chemical Name: 9-[(3R)-1-(cyclopropanesulfonyl)pyrrolidin-3-yl]-N2-[4-(4-methylpiperazin-1-yl)phenyl]-N8-phenyl-9H-purine-2,8-diamine

Smiles: CN1CCN(CC1)C1C=CC(=CC=1)NC1=NC2=C(C=N1)N=C(NC1C=CC=CC=1)N2[C@H]1CN(CC1)S(=O)(=O)C1CC1

InChiKey: RNEHWYIFHKBZAW-XMMPIXPASA-N

InChi: InChI=1S/C29H35N9O2S/c1-35-15-17-36(18-16-35)23-9-7-22(8-10-23)31-28-30-19-26-27(34-28)38(29(33-26)32-21-5-3-2-4-6-21)24-13-14-37(20-24)41(39,40)25-11-12-25/h2-10,19,24-25H,11-18,20H2,1H3,(H,32,33)(H,30,31,34)/t24-/m1/s1

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 125 mg/mL (217.88 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-11 (Compound D9; 0.0001-10 µM; 72 hours) shows significantly potent anti-proliferation against HCC827 and H1975 cell lines with IC50s of 0.88 nM and 0.20 µM, respectively. EGFR-IN-11 (0.01-1.00 µM for HCC827 cells; 0.1-10.00 µM for H1975 and A549 cells; 8 hours) suppresses EGFR phosphorylation in a concentration-dependent manner in the HCC827, H1975 and A549 cell line. EGFR-IN-11 (1 µM; 24 h) potently induces the apoptosis of HCC827 cells. EGFR-IN-11 (1 µM; 24 h) induces cell cycle arrests in HCC827 cell.

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