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PD184352 (CI1040)

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PD184352 (CI1040)
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Cat #: V0448 CAS #: 212631-79-3 Purity ≥ 98%

Description: PD184352 (PD-184352; CI-1040), an analog of benzhydroxamate, is an orally bioactive, specific, allosteric/non-ATP competitive MEK1/2 inhibitor with potential anticancer activity.

References: Allen LF, et al. CI-1040 (PD184352), a targeted signal transduction inhibitor of MEK (MAPKK). Semin Oncol. 2003 Oct;30(5 Suppl 16):105-16.

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Molecular Weight (MW)478.67
Molecular FormulaC17H14ClF2IN2O2
CAS No.212631-79-3
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 96 mg/mL (200.6 mM)r
Water: <1 mg/mLr
Ethanol: 14 mg/mL (29.2 mM)
Solubility In Vivo30% PEG400+0.5% Tween80+5% propylene glycol, pH 9: 10 mg/mL
SMILES CodeO=C(NOCC1CC1)C2=CC=C(F)C(F)=C2NC3=CC=C(I)C=C3Cl
SynonymsPD 184352; CI-1040; CI1040; PD-184352; PD184352; CI 1040;
ProtocolIn VitroCI-1040 directly inhibits MEK1 with an IC50 of 17 nM. It has also been shown to have little activity against a panel of related kinases with IC50 values more than 2.5 orders of magnitude higher. Treatment of whole cells with CI-1040 completely inhibits the mitogen-stimulated phosphorylation of ERK. CI-1040 at a concentration of 1 μM is found to inhibit phosphorylation of ERK1 and ERK2 by 99% and 92%, respectively in MDA-MB-231 breast cancer cells.
In VivoThe systemic administration of the MEK inhibitor CI-1040 reduces adenoma formation to a third and significantly restores lung structure. The proliferation rate of lung cells of mice treated with CL-1040 is decreased without any obvious effects on differentiation of pneumocytes.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.0891 mL10.4456 mL20.8912 mL41.7824 mL
5mM0.4178 mL2.0891 mL4.1782 mL8.3565 mL
10mM0.2089 mL1.0446 mL2.0891 mL4.1782 mL
20mM0.1045 mL0.5223 mL1.0446 mL2.0891 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid 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 master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (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.