AZD8330 Chemical Structure
AZD6244 (Selumetinib, ARRY-142886) is highly potent to inhibit MEK1 with IC50 of 14 nM.
CI-1040 (PD184352) is a MEK 1/2 inhibitor. Ki of 300nM
PD0325901 is MEK inhibitor and non-competitive with ATP, Kiapp of 1 nM against activated MEK1 and MEK2.
MEK inhibitor with EC50 of 73 nM.
U0126-EtOH is an inhibitor of both MEK1 and MEK2 with an IC50 of 72 nM and 58 nM respectively.
PD 98059 is an inhibitor of MEK1 and MEK2 with IC50 values of 4 μM and 50 μM respectively.
AS703026 is a highly selective and potent noncompetitive inhibitor of MEK1/2 with an IC50 range of 5-11 nM.
BIX02188 is a MEK5-selective inhibitor with an IC50 of 0.8 ± 1.0 μM.
BIX 02189 is a selective MEK5/ERK5 inhibitor with an IC50 of 59 nM.
PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor.
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]
| Molecular Weight (WM): | 461.23 |
|---|---|
| Formula: | C16H17FIN3O4 |
| CAS No.: | 869357-68-6 |
| Synonyms: |
N/A
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| 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 |
A collection of 864 bioactive compounds
A collection of 481 inhibitors
A collection of 194 kinase inhibitors
A collection of 85 tyrosine kinase inhibitors.
A collection of 426 FDA approved drugs
A collection of 139 natural products
A collection of 40 chemotherapeutic agents
A unique collection of 17 small molecule modulators
A unique collection of 47 small molecule inhibitors
A unique collection of 63 GPCR small molecules

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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