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PD318088
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PD318088图片
CAS NO:391210-00-7
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)561.09
FormulaC16H13BrF3IN2O4
CAS No.391210-00-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 112 mg/mL (199.6 mM)
Water: <1 mg/mL
Ethanol: 14 mg/mL (25.0 mM)
Other infoChemical Name: 5-bromo-N-(2,3-dihydroxypropoxy)-3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)benzamide
InChi Key: XXSSGBYXSKOLAM-UHFFFAOYSA-N
InChi Code: InChI=1S/C16H13BrF3IN2O4/c17-10-4-9(16(26)23-27-6-8(25)5-24)15(14(20)13(10)19)22-12-2-1-7(21)3-11(12)18/h1-4,8,22,24-25H,5-6H2,(H,23,26)
SMILES Code: O=C(NOCC(O)CO)C1=CC(Br)=C(F)C(F)=C1NC2=CC=C(I)C=C2F
SynonymsPD 318088; PD318088; PD-318088
实验参考方法
In Vitro

In vitro activity: PD318088 is a small-molecule inhibitor of MEK1/2, which is an analog of PD184352, suggesting it might have substantial anti-proliferative activity against cancer cells, although no functional study of PD318088 is currently available. PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. Formation of the ternary complexes with PD318088 and MgATP results in moderate increases (to 140 nM) for the Kd monomer-dimer for both MEK1 and MEK2. The binding of PD318088 and MgATP to MEK1 also abolishes the formation of tetramers and higher-order aggregates. PD318088 and MgATP together increase the dimerization disassociation constant for MEK1 and MEK2 slightly from ~75 nM to ~140 nM, suggesting that the mechanism of inhibition for PD318088 is probably a result of localized conformational changes in the active site and not a global change in the overall structure.


Kinase Assay: PD318088 and MgATP results in moderate increases (to 140 nM) for the Kd monomer-dimer for both MEK1 and MEK2. PD318088 and MgATP together increase the dimerization disassociation constant for MEK1 and MEK2 slightly from ~75 nM to ~140 nM.

In Vivo
Animal model
Formulation & Dosage
ReferencesNat Struct Mol Biol. 2004 Dec;11(12):1192-7.