BMS-599626

BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy[1][2].

Product Specifications

CAS Number

[714971-09-2]

Product Name Alternative

AC480

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

EGFR

Type

Reference compound

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/bms-599626.html

Purity

98.56

Solubility

DMSO : 110 mg/mL (ultrasonic)

Smiles

O=C(NC1=CN2C(C(NC3=CC4=C(N(CC5=CC=CC(F)=C5)N=C4)C=C3)=NC=N2)=C1C)OC[C@H]6NCCOC6

Molecular Formula

C27H27FN8O3

Molecular Weight

530.55

Precautions

H302, H315, H319, H335

References & Citations

[1]Wong TW, et al. Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling. Clin Cancer Res. 2006 Oct 15;12 (20 Pt 1) :6186-93.|[2]Torres MA, et al. AC480, formerly BMS-599626, a pan Her inhibitor, enhances radiosensitivity and radioresponse of head and neck squamous cell carcinoma cells in vitro and in vivo. Invest New Drugs. 2011 Aug;29 (4) :554-61.