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PD184161

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Catalog No. T21635Cas No. 212631-67-9

PD184161 is a novel, orally-active MEK inhibitor. PD184161 inhibited MEK activity (IC50 = 10-100 nM) in a time- and concentration-dependent manner[1].

PD184161

PD184161

🥰Excellent
Purity: 99.09%
Catalog No. T21635Cas No. 212631-67-9
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 SizePriceAvailabilityQuantity
1 mg$32In Stock
2 mg$44In Stock
5 mg$72In Stock
10 mg$128In Stock
25 mg$287In Stock
50 mg$478In Stock
100 mg$688In Stock
200 mg$987In Stock
500 mg$1,480In Stock
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Purity:99.09%
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight557.56
FormulaC17H13BrClF2IN2O2
Cas No.212631-67-9
SmilesFc1c(F)c(Nc2ccc(I)cc2Cl)c(cc1Br)C(=O)NOCC1CC1
Relative Density.1.922 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM1.7935 mL8.9676 mL17.9353 mL89.6764 mL
5 mM0.3587 mL1.7935 mL3.5871 mL17.9353 mL
10 mM0.1794 mL0.8968 mL1.7935 mL8.9676 mL
20 mM0.0897 mL0.4484 mL0.8968 mL4.4838 mL
50 mM0.0359 mL0.1794 mL0.3587 mL1.7935 mL

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