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Product Description
– 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].
Web ID
– HY-10251
Shipping
– Room temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C27H27FN8O3
Citations
– BMC Pulm Med. 2023 May 11;23(1):162.|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.|Life Sci. 2021 Dec 16;289:120231.
References
– [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.
CAS Number
– 714971-09-2
Molecular Weight
– 530.55
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
Clinical Information
– Phase 1
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– EGFR
Pathway
– JAK/STAT Signaling;Protein Tyrosine Kinase/RTK
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
