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Products Details
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
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