GSK1904529A

GSK1904529A is a potent, selective, orally active, and ATP-competitive inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR), with IC50s of 27 and 25 nM, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity[1][2].

Product Specifications

CAS Number

[1089283-49-7]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; IGF-1R; Insulin Receptor

Type

Reference compound

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Endocrinology

Assay Protocol

https://www.medchemexpress.com/GSK1904529A.html

Purity

99.03

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(C1=CC(C2=C(N3C=CC=CC3=N2)C4=NC(NC5=CC(CC)=C(C=C5OC)N6CCC(CC6)N7CCN(CC7)S(=O)(C)=O)=NC=C4)=CC=C1OC)NC8=C(C=CC=C8F)F

Molecular Formula

C44H47F2N9O5S

Molecular Weight

851.96

Precautions

H302, H315, H319, H335

References & Citations

[1]Sabbatini P, et al. Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase. Clin Cancer Res, 2009, 15 (9), 3058-3067.|[2]Zhou Q, et, al. GSK1904529A, an insulin-like growth factor-1 receptor inhibitor, inhibits glioma tumor growth, induces apoptosis and inhibits migration. Mol Med Rep. 2015 Sep;12 (3) :3381-3385.