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AZD8330

Cat. No. M1662
AZD8330 Structure
Synonym:

ARRY-424704, ARRY-704

Size Price Availability Quantity
10mM*1mL in DMSO USD 110  USD110 In stock
5mg USD 105  USD105 In stock
10mg USD 190  USD190 In stock
50mg USD 700  USD700 In stock
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Quality Control
Biological Activity

AZD8330 (ARRY-424704) is a novel, selective, highly efficacious, uncompetitive MEK inhibitor with an IC50 of 7 nM.AZD8330 demonstrates sub-nanomolar potency in mechanistic (pERK) and low to sub-nanomolar potency in functional (proliferation) assays in MEK 1/2 inhibitor sensitive cell lines.

Customer Product Validations & Biological Datas
Source Eur J Cancer (2013). Figure 4. AZD8330
Method Western blot
Cell Lines osteosarcoma cell lines
Concentrations 0.5 μM
Incubation Time 6 h
Results The resistant cell lines KPD, ZK58 and Saos-2 showed no constitutive ERK activation. Exposing MOS, U2OS and 143b to a concentration of 0.5μM of Trametinib, AZD8330 or TAK-733 for 6 hours, led to loss of ERK phosphorylation indicating effective MEK inhibition
Protocol
Cell Experiment
Cell lines HT-29, Malme-3M, MIA PaCa-2, BxPC3, BT474, Zr-75-1 and Malme-3 cell lines
Preparation method Cellular viability assays
Cells plated in 96-well plates were incubated with multiple concentrations of compound for 3 days. The number of viable cells was determined using the CellTiter 96 Aqueous Nonradioactive Cell Proliferation Assay (Promega, Madison, WI).
Concentrations 0~50μM
Incubation time 3 days
Animal Experiment
Animal models HT-29 and BxPC3 xenograft
Formulation 10 mL/kg and 10% ethanol/10% cremophor EL/80% D5W
Dosages 10, 25, 50, or 100 mg/kg BID
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 461.23
Formula C16H17FIN3O4
CAS Number 869357-68-6
Purity 98.60%
Solubility DMSO
Storage at -20°C
References

[1] Ke Feng, et al. Effect of ERK1/2 inhibitor AZD8330 on human Burkitt's lymphoma cell line Raji cells and its mechanism

[2] Yao Yao, et al. Effect of AZD8330 on proliferation and apoptosis of multiple myeloma cells

[3] Caela R Miller, et al. MEK1/2 inhibitors in the treatment of gynecologic malignancies

[4] Akintunde Akinleye, et al. MEK and the inhibitors: from bench to bedside

[5] Roger B Cohen, et al. A phase I dose-finding, safety and tolerability study of AZD8330 in patients with advanced malignancies

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AZD8330, ARRY-424704, ARRY-704 supplier, MEK, inhibitors

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