ARRY-380 Chemical Properties

Density 

1.43

storage temp. 

Store at -20°C

solubility 

≥28.5 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O

form 

solid

pka

6.34±0.19(Predicted)

color 

Light brown to brown

ARRY-380 Usage And Synthesis

Description

Arry-380 analog was designed as an inhibitor of EGFR (ErbB1).

Uses

ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM and also inhibits EGFR with IC50 of 4 μM.

Uses

Labelled ARRY-380. ARRY-380 is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2.

target

p95-HER2

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.

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