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BMS-599626 Hydrochloride

Catalog No. T5390 CAS 873837-23-1

Synonyms: AC480 Hydrochloride

BMS-599626 Hydrochloride (AC480 Hydrochloride) is an orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases (IC50 =22, 32 and 190 nM, respectively) with potential antineoplastic activity. BMS-599626 Hydrochloride inhibits human epidermal growth factor receptors (HER) HER1, HER2 and HER4, thereby inhibiting the proliferation of tumor cells that overexpress these receptors.

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BMS-599626 Hydrochloride Chemical Structure

BMS-599626 Hydrochloride, CAS 873837-23-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 37.00
5 mg	In stock	$ 87.00
10 mg	In stock	$ 133.00
25 mg	In stock	$ 253.00
50 mg	In stock	$ 447.00
100 mg	In stock	$ 659.00
1 mL * 10 mM (in DMSO)	In stock	$ 109.00

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Purity: 100%

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Storage & Solubility Information

Description	BMS-599626 Hydrochloride (AC480 Hydrochloride) is an orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases (IC50 =22, 32 and 190 nM, respectively) with potential antineoplastic activity. BMS-599626 Hydrochloride inhibits human epidermal growth factor receptors (HER) HER1, HER2 and HER4, thereby inhibiting the proliferation of tumor cells that overexpress these receptors.
Targets&IC50	HER1:22 nM, HER2:32nM, HER4:190 nM
In vitro	BMS-599626 Hydrochloride abrogates HER1 and HER2 signaling and inhibited the proliferation of tumor cell lines that are dependent on these receptors, with IC50s in the range of 0.24 to 1 μM.In GEO cells, HER1 phosphorylation is stimulated by treatment with EGF and is inhibited by BMS-599626 Hydrochloride (IC50=0. 75 μM).There is also nearly complete inhibition of EGF-dependent MAPK (0. 8 μM) but only partial inhibition of AKT signaling.The latter likely reflects the activation of AKT by multiple upstream signals.Treatment of N87 cells with BMS-599626 Hydrochloride leads to the inhibition of HER2 (0. 38 μM), which is expressed to a high level because of gene amplification, as well as MAPK and AKT phosphorylation (0.35 μM for both) [1].
In vivo	BMS-599626 Hydrochloride given before and during irradiation improved the radioresponse of HN5 tumors in vivo [2].

Synonyms	AC480 Hydrochloride
Molecular Weight	567.01
Formula	C27H28ClFN8O3
CAS No.	873837-23-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90.0 mg/mL (158.7 mM), Sonification is recommended.

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Compound Library Bioactive Compound Library Kinase Inhibitor Library Bioactive Compounds Library Max

Related Products

Related compounds with same targets

HER2/neu (654-662) GP2 acetate Guanfu base A Tucatinib ARRY-380 (analog ) BMS 599626 2HCl (873837-23-1(HCl)) PF04929113 CUDC-101 Mollugin

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

BMS-599626 Hydrochloride 873837-23-1 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors HER AC 480 Hydrochloride BMS599626 Hydrochloride AC480 Hydrochloride AC-480 Hydrochloride BMS 599626 Hydrochloride inhibitor inhibit

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