Arry-380

• Catalog No.: S2752
• CAS Number: 937265-83-3
• M. F.: C29H27N7O4S
• M. W.: 569.63418
• Storage: -20°C

SYNONYMS

• IUPAC name: 6-(5-{[(2-methanesulfonylethyl)amino]methyl}furan-2-yl)-N-(3-methyl-4-{[1,2,4]triazolo[1,5-a]pyridin-7-yloxy}phenyl)quinazolin-4-amine
• IUPAC Traditional name: 6-(5-{[(2-methanesulfonylethyl)amino]methyl}furan-2-yl)-N-(3-methyl-4-{[1,2,4]triazolo[1,5-a]pyridin-7-yloxy}phenyl)quinazolin-4-amine

DATABASE IDS

• CAS Number: 937265-83-3

PROPERTIES

• Target: HER2
• Salt Data: Free Base
• Storage Condition: -20°C

DETAILS

Description (English)

Research Area

• Description: Solid tumours , Breast cancer

Biological Activity

• Description: ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM.
• Targets: HER2; p95-HER2
• IC50: 8 nM; 7 nM ^[1]
• In Vitro: ARRY-380 is equipotent against truncated p95-HER2 with IC50 of 7 nM. ^[1] However, ARRY-380 suppresses EGFR with IC50 of 4 μM. ARRY-380 is about 500-fold selective for HER2 versus EGFR. ^[1]
• In Vivo: ARRY-380 significantly prevents the growth of tumor in multiple HER2-dependent tumor xenograft models and displays additive activity in combination with standard-of-care agents. ^[1]
• Clinical Trials: ARRY-380 is in a phase I clinical trial for the treatment of breast cancer.

References

• References: [1] Moulder SL, et al. Molecular Cancer Therapeutics. 2011, 10(11), Abstracts #143.

REFERENCES

• Moulder SL, et al. Molecular Cancer Therapeutics. 2011, 10(11), Abstracts #143.