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PD184161 is a novel, orally-active MEK inhibitor. PD184161 inhibited MEK activity (IC50 = 10-100 nM) in a time- and concentration-dependent manner[1].
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $32 | In Stock | |
2 mg | $44 | In Stock | |
5 mg | $72 | In Stock | |
10 mg | $128 | In Stock | |
25 mg | $287 | In Stock | |
50 mg | $478 | In Stock | |
100 mg | $688 | In Stock | |
200 mg | $987 | In Stock | |
500 mg | $1,480 | In Stock |
Description | PD184161 is a novel, orally-active MEK inhibitor. PD184161 inhibited MEK activity (IC50 = 10-100 nM) in a time- and concentration-dependent manner[1]. |
Targets&IC50 | MEK1/2:10-100 nM |
In vitro | PD184161 inhibited MEK activity (IC50 = 10-100 nM) in a time- and concentration-dependent manner more effectively than PD098059 or U0126. PD184161 inhibited cell proliferation and induced apoptosis at concentrations of > or = 1.0 microM in a time- and concentration-dependent manner[1]. |
In vivo | In vivo, tumor xenograft P-ERK levels were significantly reduced 3 to 12 hours after an oral dose of PD184161 (P < .05). Contrarily, tumor xenograft P-ERK levels following long-term (24 days) daily dosing of PD184161 were refractory to this signaling effect. PD184161 significantly suppressed tumor engraftment and initial growth (P < .0001); however, established tumors were not significantly affected. In conclusion, PD184161 has antitumor effects in HCC in vivo that appear to correlate with suppression of MEK activity [1]. |
Molecular Weight | 557.56 |
Formula | C17H13BrClF2IN2O2 |
Cas No. | 212631-67-9 |
Smiles | Fc1c(F)c(Nc2ccc(I)cc2Cl)c(cc1Br)C(=O)NOCC1CC1 |
Relative Density. | 1.922 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 55 mg/mL (98.64 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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