ZM306416

ZM306416 is a selective VEGFR1 inhibitor. ZM306416 antagonizes the activity of KDR and Flt VEGF receptors with IC50 values of 100 nM and 2 μM, respectively.

Product information

CAS Number: 690206-97-4

Molecular Weight: 333.74

Formula: C16H13ClFN3O2

Synonym:

ZM-306416

Chemical Name: 4-[(4'-Chloro-2'-fluoro)phenylamino]-6,7-dimethoxyquinazoline

Smiles: COC1=CC2=NC=NC(NC3=CC=C(Cl)C=C3F)=C2C=C1OC

InChiKey: YHUIUSRCUKUUQA-UHFFFAOYSA-N

InChi: InChI=1S/C16H13ClFN3O2/c1-22-14-6-10-13(7-15(14)23-2)19-8-20-16(10)21-12-4-3-9(17)5-11(12)18/h3-8H,1-2H3,(H,19,20,21)

Technical Data

Appearance: Solid Power.

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

Solubility: Soluble in DMSO, not in water

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: ≥360 days 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:

ZM-306416 selective anti-proliferative effect toward the EGFR addicted NSCLC cell lines H3255 and HCC4011 (IC50=0.09±0.007 μM and 0.072±0.001 μM respectively), while sparing the wild type EGFR cell lines A549 and H2030 (IC50>10 μM). ZM-306416 is also found to inhibit the ABL in vitro kinase activity with a less potent IC50 value of 1.3±0.2 μM toward the ABL kinase.

References:

1. Antczak C, Mahida JP, Bhinder B, Calder PA, Djaballah H. A high-content biosensor-based screen identifies cell-permeable activators and inhibitors of EGFR function: implications in drug discovery. J Biomol Screen. 2012 Aug;17(7):885-99. doi: 10.1177/1087057112446174. Epub 2012 May 9. PubMed PMID: 22573732.

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