GW2974

Names

[ CAS No. ]:
202272-68-2

[ Name ]:
GW2974

[Synonym ]:
Lopac-G-0668
N4-(1-Benzyl-1H-indazol-5-yl)-N6,N6-dimethyl-pyrido[3,4-d]pyrimidine-4,6-diamine
GW2974

Biological Activity

[Description]:

GW2974 is a potent dual inhibitor of EGFR and HER2 with IC50 value of 0.007 μM and 0.016 μM, respectively. GW2974 demonstrates in vitro inhibition of the EGFR and HER2 and inhibits the growth of tumor cell. GW2974 can be used for glioblastoma multiforme (GBM) disease research[1][2].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> EGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

[Target]

EGFRL858R/T790M:0.007 μM (IC50)

HER2:0.016 μM (IC50)

[References]

[1]. Wang L, et al. Differential effects of low- and high-dose GW2974, a dual epidermal growth factor receptor and HER2 kinase inhibitor, on glioblastoma multiforme invasion. J Neurosci Res. 2013 Jan;91(1):128-37.

[2]. Rusnak DW, et al. The characterization of novel, dual ErbB-2/EGFR, tyrosine kinase inhibitors: potential therapy for cancer. Cancer Res. 2001 Oct 1;61(19):7196-20.

Chemical & Physical Properties

[ Boiling Point ]:
645.6ºC at 760 mmHg

[ Molecular Formula ]:
C₂₃H₂₁N₇

[ Molecular Weight ]:
395.46

[ Flash Point ]:
344.3ºC

[ Exact Mass ]:
395.18600

[ PSA ]:
71.76000

[ LogP ]:
4.30540

[ Vapour Pressure ]:
1.47E-16mmHg at 25°C

[ Index of Refraction ]:
1.71

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Articles

Loss of desmocollin-2 confers a tumorigenic phenotype to colonic epithelial cells through activation of Akt/β-catenin signaling.

Mol. Biol. Cell 22 , 1121-1134, (2011)

Desmocollin-2 (Dsc2) and desmoglein-2 (Dsg2) are transmembrane cell adhesion proteins of desmosomes. Reduced expression of Dsc2 has been reported in colorectal carcinomas, suggesting that Dsc2 may pla...

Gene network dynamics controlling keratinocyte migration.

Mol. Syst. Biol. 4 , 199, (2008)

Translation of large-scale data into a coherent model that allows one to simulate, predict and control cellular behavior is far from being resolved. Assuming that long-term cellular behavior is reflec...

Association of constitutively activated hepatocyte growth factor receptor (Met) with resistance to a dual EGFR/Her2 inhibitor in non-small-cell lung cancer cells.

Br. J. Cancer 100 , 941-9, (2009)

There is a pressing need to identify new drug targets and novel approaches for treatment of non-small-cell lung carcinoma (NSCLC). Members of the epidermal growth factor receptor (EGFR) and Met recept...