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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Purity: ≥98%
PD318088 (PD-318088), an analog of PD184352, is a novel, potent and non-ATP competitive (allosteric) MEK1/2 inhibitor with potential anticancer activity. Against different cancer cells, PD318088 exhibits strong anti-proliferative activity.
Targets |
MEK1; MEK2
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ln Vitro |
PD318088 is a small-molecule MEK1/2 inhibitor, an analog of PD184352, suggesting it might have significant anti-proliferative activity against cancer cells, even though there isn't a functional study of PD318088 available at this time. In an area of the MEK1 active site close to the ATP-binding site, PD318088 and ATP bind simultaneously. The Kd monomer-dimer for both MEK1 and MEK2 is moderately increased (to 140 nM) by the ternary complexes formed with PD318088 and MgATP. Tetramers and higher-order aggregates cannot form when PD318088 and MgATP are bound to MEK1. Together, PD318088 and MgATP slightly raise the dimerization disassociation constant for MEK1 and MEK2 from ~75 nM to ~140, indicating that the mechanism of PD318088 inhibition is likely the result of localized conformational changes in the active site rather than a general change in the structure. [1]
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ln Vivo |
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Enzyme Assay |
PD318088 and MgATP, the Kd monomer-dimer for MEK1 and MEK2 increases moderately (to 140 nM). The dimerization disassociation constant for MEK1 and MEK2 increases slightly from ~75 nM to ~140 nM when PD318088 and MgATP are combined.
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Animal Protocol |
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References |
Molecular Formula |
C16H13BRF3IN2O4
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Molecular Weight |
561.09
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Exact Mass |
559.91
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Elemental Analysis |
C, 34.25; H, 2.34; Br, 14.24; F, 10.16; I, 22.62; N, 4.99; O, 11.41
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CAS # |
391210-00-7
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Related CAS # |
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Appearance |
Solid powder
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SMILES |
C1=CC(=C(C=C1I)F)NC2=C(C(=C(C=C2C(=O)NOCC(CO)O)Br)F)F
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InChi Key |
XXSSGBYXSKOLAM-UHFFFAOYSA-N
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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)
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Chemical Name |
5-bromo-N-(2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodoanilino)benzamide
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (4.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (4.90 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.75 mg/mL (4.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.7822 mL | 8.9112 mL | 17.8225 mL | |
5 mM | 0.3564 mL | 1.7822 mL | 3.5645 mL | |
10 mM | 0.1782 mL | 0.8911 mL | 1.7822 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.