937265-83-3

Basic information

• Product Name: ARRY-380
• Synonyms: ARRY-380;6-[5-[[[2-(Methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-N-[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]-4-quinazolinamine;ARRY-380-d3;N-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-Methylphenyl)-6-(5-(((2-(Methylsulfonyl)ethyl)aMino)Methyl)furan-2-yl)quinazolin-4-aMine;HER2-Inhibitor-1;6-[5-[[[2-(Methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-N-[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]-4-quinazolinamine ARRY 380;Arry-380, >=98%;ARRY-380 (analog )
• CAS NO: 937265-83-3
• Molecular Formula: C29H27N7O4S
• Molecular Weight: 569.63418
• EINECS: -0
• Product Categories: Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds;Inhibitors
• Mol File: 937265-83-3.mol
• Article Data: 1

Chemical Properties

• Appearance: /
• Density: 1.43
• Solubility: ≥28.5 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
• PKA: 6.34±0.19(Predicted)
• CAS DataBase Reference: ARRY-380(CAS DataBase Reference)
• NIST Chemistry Reference: ARRY-380(937265-83-3)
• EPA Substance Registry System: ARRY-380(937265-83-3)

Safety Data

• Hazardous Substances Data: 937265-83-3(Hazardous Substances Data)

Usage

Description

ARRY-380 is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2, designed as an inhibitor of EGFR (ErbB1). It is a potent and selective HER2 inhibitor with an IC50 of 8 nM and also inhibits EGFR with an IC50 of 4 μM.

Uses

Used in Pharmaceutical Industry:
ARRY-380 is used as a potent and selective HER2 inhibitor for treating cancer, particularly breast cancer, due to its ability to inhibit the growth and proliferation of cancer cells.
Used in Cancer Research:
ARRY-380 is used as a research tool for studying the role of EGFR and HER2 in cancer cell growth and proliferation, as well as for evaluating the effectiveness of targeted therapies against these receptors.
Used in Drug Development:
ARRY-380 is used as a lead compound in the development of new drugs targeting EGFR and HER2, with the potential to improve treatment outcomes for various types of cancer.

references

[1] s. l. moulder, v. borges, s. k. l. chia, t. baetz, e. barrett, j. garrus, k. guthrie, c. kass, e. laird, j. lyssikatos, f. marmsater, e. wallace. arry-380, a selective her2 inhibitor: from drug design to clinical evaluation. poster of aacr-nci-eortc, nov 12-16, 2011, san francisco, ca.[2] victoria dinkel, deborah anderson, shannon winski, jim winkler, kevin koch and patrice lee. arry-380, a potent, small molecule inhibitor of erbb2, increases survival in intracranial erbb2+ xenograft models in mice. poster available at www.arraybiopharma.com[3] s. chia, t. baetz, s. d'aloisio, g. fernetich, b. freeman, e. barrett, c. kass, j. kang, b. sajan, s. moulder, and j. garrus. a phase 1 study to assess the safety, tolerability and pharmacokinetics of arry-380 – an oral inhibitor of her2. cancer res 2009;69(24 suppl):abstract nr 5111.

InChI:InChI=1S/C29H27N7O4S/c1-19-13-21(4-7-26(19)39-22-9-11-36-28(15-22)32-18-34-36)35-29-24-14-20(3-6-25(24)31-17-33-29)27-8-5-23(40-27)16-30-10-12-41(2,37)38/h3-9,11,13-15,17-18,30H,10,12,16H2,1-2H3,(H,31,33,35)

Relevant articles and documents

Processes and intermediates for the preparation of N4-phenyl-quinazoline-4-amine derivatives

This invention provides compounds of Formula (I), wherein B, G, A, E, R1, R2, R3, m and n are as defined herein, which are useful as type I receptor tyrosine kinase inhibitors, and methods of use thereof in the treatment of hyperproliferative disorders in mammals.