RDEA119 (BAY 869766) 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.
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.
RDEA119 is a highly potent and selective inhibitor of mitogen activated ERK kinase (MEK), a key component of the RAS/RAF/MEK/ERK pathway that is commonly defective in human tumors . Rdea119 has favorable properties, including oral dosing, excellent selectivity and low central nervous system (CNS) penetration.
In mouse xenograft studies, when rdea119 was dosed orally once daily for 14 days, there are significant inhibition and delay of tumor growth. We observed inhibition of pERK in tumors (the target of therapy) at significantly lower concentrations (EC50 = 73 nM), compared to those required to inhibit brain pERK (EC50 > 5,000 nM).
| Molecular Weight (WM): | 572.34 |
|---|---|
| Formula: | C19H20F3IN2O5S |
| CAS No.: | 923032-37-5 |
| Synonyms: |
BAY 869766
|
| Dissolve in (25°C): | |
| 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
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