AZD8330

SKU: orb1301088

Description

AZD8330 (ARRY-704) is a potent and selective allosteric inhibitor of MEK1/2, demonstrating an IC50 of 7 nM. This investigational compound has been utilized in preclinical in vitro and in vivo studies to explore its potential in oncology research, particularly targeting the MAPK signaling pathway.

Research Area

Signal Transduction

Images & Validation

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Key Properties

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CAS Number	869357-68-6
MW	461.23
Purity	99.91% (May vary between batches)
Formula	C₁₆H₁₇FIN₃O₄
SMILES	Cc1cc(C(=O)NOCCO)c(Nc2ccc(I)cc2F)n(C)c1=O
Target	ERK,MEK
Solubility	H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:85 mg/mL (184.29 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2.5 mg/mL (5.42 mM);Ethanol:85 mg/mL (184.29 mM)

Bioactivity

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Target IC50	MEK1/2:7 nM
In Vivo	In a Calu-6 rat xenograft pharmacokinetic/pharmacodynamic (PK/PD) model a single, 1.25 mg/kg oral dose of AZD8330 inhibits ERK phosphorylation by > 90% for between 4 and 8 hours. Doses as low as 0.4 mg/kg once daily are sufficient for > 80% tumor growth inhibition in the Calu-6 nude rat xenograft model. In the Calu-6 model, AZD8330 inhibits tumor growth in a dose-dependent fashion, at 0.3 mg/kg and 1.0 mg/kg once daily. Read more...
In Vitro	AZD8330 potently and strongly inhibits MEK 1/2. AZD8330 has no inhibitory activity against over 200 other kinases including at concentrations up to 10 μM. 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. Read more...
Cell Research	Malme-3M melanoma cells are plated in 96-wells and treated with various concentrations of AZD8330 for 1 hour at 37 °C. The cells are fixed, permeabilized, and incubated with an anti-phospho-ERK antibody and an anti-ERK 1/2 antibody. Plates are washed and fluorescently-labeled secondary antibodies are added. Plates are analyzed on a LICOR fluorescence imager. The pERK signal is normalized to the total ERK signa (Only for Reference) Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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MEK, MEK1/2, MAPKK, MAP2K, Inhibitor, ERK phosphorylation, Mitogen-activated protein kinase kinase, inhibit, AZD8330, AZD-8330, ARRY704, ARRY-704, ARRY424704, ARRY-424704, ARRY 704, ARRY 424704, AZD 8330

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Compound Identifiers

PubChem CID

16666708 ↗

Key Properties

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No computed properties available.

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AZD8330 (orb1301088)

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Purity:	>98% (HPLC)
CAS Number:	869357-68-6
MW:	461.2267
Formula:	C₁₆H₁₇FIN₃O₄

AZD8330

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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