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AZD8330

Catalog No.S2134 1 Review(s)
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AZD8330 Chemical Structure

  • AZD6244 (Selumetinib)

    AZD6244 (Selumetinib, ARRY-142886) is highly potent to inhibit MEK1 with IC50 of 14 nM.

  • CI-1040 (PD184352)

    CI-1040 (PD184352) is a MEK 1/2 inhibitor. Ki of 300nM

  • PD0325901

    PD0325901 is MEK inhibitor and non-competitive with ATP, Kiapp of 1 nM against activated MEK1 and MEK2.

  • RDEA119 (BAY 869766)

    MEK inhibitor with EC50 of 73 nM.

  • U0126-EtOH

    U0126-EtOH is an inhibitor of both MEK1 and MEK2 with an IC50 of 72 nM and 58 nM respectively.

  • PD98059

    PD 98059 is an inhibitor of MEK1 and MEK2 with IC50 values of 4 μM and 50 μM respectively.

  • AS703026

    AS703026 is a highly selective and potent noncompetitive inhibitor of MEK1/2 with an IC50 range of 5-11 nM.

  • BIX 02188

    BIX02188 is a MEK5-selective inhibitor with an IC50 of 0.8 ± 1.0 μM.

  • BIX 02189

    BIX 02189 is a selective MEK5/ERK5 inhibitor with an IC50 of 59 nM.

  • PD318088

    PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor.

Biological Activity

AZD8330 is an orally active, selective MEK inhibitor with an IC50 of 7 nM. AZD8330 has potential antineoplastic activity. AZD8330 specifically inhibits mitogen- activated protein kinase kinase 1 (MEK or MAP/ERK kinase1), resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth. Constitutive activation of this pathway has been implicated in many cancers. [1][2]

References on AZD8330
  • [2] Journal of Hematology & Oncology 2010;3:8
Molecular Weight (WM): 461.23
Formula:

C16H17FIN3O4

CAS No.: 869357-68-6
Synonyms:
N/A
Dissolve in (25°C): DMSO ≥92mg/mL 
Water <1mg/mL 
Ethanol ≥92mg/mL 
Storage: 2 years-20°CPowder
1 week-4°Cin DMSO
1 month-80°in DMSO

Quality Control & MSDS

View current batch:
COA H-NMR HPLC

Research Area

MAPK >> MEK >> MEK Inhibitors
Notes:

Related Inhibitors

Recommended Screening Libraries

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  • Click to enlarge

    After starved in serum-free medium for 24h, T47D cells incubated with the indicated concentrations of AZD8330 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.

  • After starved in serum-free medium for 24h, T47D cells incubated with the indicated concentrations of AZD8330 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.

  • Data independently produced by Dr. Zhang of Tianjin Medical University
    AZD8330 purchased from Selleck

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After starved in serum-free medium for 24h, T47D cells incubated with the indicated concentrations of AZD8330 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.

Data independently produced by Dr. Zhang of Tianjin Medical University

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