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BMS-599626 (Hydrochloride)

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

Product Specifications

CAS Number

[873837-23-1]

Product Name Alternative

AC480 (Hydrochloride)

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-Hydrochloride.html

Purity

99.68

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(OC[C@H]1NCCOC1)NC2=CN(C3=C2C)N=CN=C3NC4=CC5=C(C=C4)N(CC6=CC(F)=CC=C6)N=C5.Cl

Molecular Formula

C27H28ClFN8O3

Molecular Weight

567.01

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.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Phase 1

Citation 01

Life Sci. 2021 Dec 16;289:120231.|BMC Pulm Med. 2023 May 11;23 (1) :162.|Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.

Available Sizes

Curated Selection

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