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ARRY-380

Cat. No. M3560
ARRY-380 Structure
Size Price Availability Quantity
5mg USD 135  USD135 In stock
10mg USD 225  USD225 In stock
50mg USD 850  USD850 In stock
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Quality Control & Documentation
Biological Activity

ARRY-380 is an orally bioavailable, potent, selective, small-molecule tyrosine kinase HER2 and p95-HER2 inhibitor with an IC50 of 8 and 7 nM, respectively. However, ARRY-380 inhibits EGFR with an IC50 of 4 μM. ARRY-380 is about 500-fold selective for HER2 versus EGFR. ARRY-380 produces significantly antitumor activities in multiple HER2-dependent tumor xenograft models and generates additive activity in combination with standard-of-care agents. ARRY-380 is in a phase I clinical trial for the treatment of breast cancer

Chemical Information
Molecular Weight 569.63
Formula C29H27N7O4S
CAS Number 937265-83-3
Solubility (25°C) DMSO 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] No authors listed. Tucatinib

[2] Euphemia Y Leung, et al. Derivation of Breast Cancer Cell Lines Under Physiological (5%) Oxygen Concentrations

[3] Stacy L Moulder, et al. Phase I Study of ONT-380, a HER2 Inhibitor, in Patients with HER2 +-Advanced Solid Tumors, with an Expansion Cohort in HER2 + Metastatic Breast Cancer (MBC)

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  Catalog
Abmole Inhibitor Catalog




Keywords: ARRY-380 supplier, EGFR/HER2, inhibitors, activators


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