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 analog was designed as an inhibitor of EGFR (ErbB1).

Uses

Different sources of media describe the Uses of 937265-83-3 differently. You can refer to the following data:
1. ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM and also inhibits EGFR with IC50 of 4 μM.
2. Labelled ARRY-380. ARRY-380 is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2.

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.