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CI-1040

Cat. No. M1690

CI-1040 Structure

Synonym: PD184352

Size Price Availability Quantity
10mg USD 90 In stock
50mg USD 280 In stock
200mg USD 650 In stock
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Quality Control
Biological Activity

CI-1040 (PD184352) is a targeted signal transduction inhibitor of MEK with a ki value of 300nM in vitro. CI-1040 (PD184352) is an orally active, highly specific, small-molecule inhibitor of one of the key components of this pathway (MEK1/MEK2), and thereby effectively blocks the phosphorylation of ERK and continued signal transduction through this pathway.

Protocol
Cell Experiment
Cell lines CCl39 cells expressing FLAG-ERK5
Preparation method Cells were serum-starved for 16 h prior to the addition of PD184352, or an equivalent of DMSO vehicle control for 90 min. Single dishes of cells were then stimulated with 10% FBS for 15 min and immune-complex kinase assays performed with either myelin basic protein (MBP; ERK1) or GST-MEF2C (ERK5), as a substrate. PD184352 inhibited FBS-induced ERK1 activation with an IC50 below 1 μM, whereas even a dose of 20 μM PD184352 was insufficient to inhibit ERK5 activity, induced in the same manner and assayed from the same cell extracts as ERK1.
Concentrations 0~1µM
Incubation time 90min
Animal Experiment
Animal models DBA/2-pcy/pcy mice
Formulation DMSO
Dosages 400 mg/kg daily for the first week and then every third day for 6 additional weeks
Administration Oral administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 478.67
Formula C17H14ClF2IN2O2
CAS Number 212631-79-3
Purity 98.81%
Solubility DMSO
Storage at -20°C
References

Inhibition of MEK pathway in vestibular schwannoma cell culture.
Neff et al. Laryngoscope. 2012 Aug 10. PMID: 22886786.

The MEK inhibitor PD184352 enhances BMS-214662-induced apoptosis in CD34+ CML stem/progenitor cells.
Pellicano et al. Leukemia. 2011 Jul;25(7):1159-67. PMID: 21483442.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CI-1040, PD184352 supplier, MEK, inhibitors

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