Home Cart Sign in  
Chemical Structure| 212631-79-3 Chemical Structure| 212631-79-3

Structure of CI-1040
CAS No.: 212631-79-3

Chemical Structure| 212631-79-3

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

CI-1040 (PD 184352) is an orally active, highly specific, small-molecule inhibitor of MEK, with an IC50 of 17 nM for MEK1.

Synonyms: PD 184352

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

Product Details of CI-1040

CAS No. :212631-79-3
Formula : C17H14ClF2IN2O2
M.W : 478.66
SMILES Code : O=C(C1=CC=C(C(F)=C1NC2=CC=C(I)C=C2Cl)F)NOCC3CC3
Synonyms :
PD 184352
MDL No. :MFCD02683961
InChI Key :GFMMXOIFOQCCGU-UHFFFAOYSA-N
Pubchem ID :6918454

Safety of CI-1040

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of CI-1040

MAPK

Isoform Comparison

Biological Activity

Target
  • MEK2

    MEK2, IC50:17 nM

  • MEK1

    MEK1, IC50:17 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
WZR4+ cells 1 μM 72 h CI-1040 partially restores sensitivity of WZR4+ cells to the combination of WZ4002 and BMS536924 PMC3994895
PFR3+ cells 1 μM 72 h CI-1040 partially restores sensitivity of PFR3+ cells to the combination of PF299804 and BMS536924 PMC3994895
MDAH2774 cells 5 µM 72 h To evaluate the inhibitory effect of CI-1040 on cell proliferation. Results showed that CI-1040 significantly inhibited the proliferation of MDAH2774 cells. PMC2607229
ES2 cells 5 µM 6 h To evaluate the inhibitory effect of CI-1040 on ERK1/2 activity. Results showed that CI-1040 significantly inhibited ERK1/2 activity in ES2 cells within 6 h. PMC2607229
C26 mouse colon carcinoma cells 2 μM 6 months C26/CI-1040r cells are approximately 100-fold more resistant than the parental line to CI-1040 inhibition in soft agar and are less sensitive to the induction of apoptosis that normally occurs in response to CI-1040 treatment PMC1501146
K1 0.5 µM 48 h CI-1040 treatment increased the proportion of G1-phase cells, but did not reach statistical significance. PMC2857444
SW1736 0.5 µM 48 h CI-1040 treatment significantly reduced the fraction of S-phase cells and increased the proportion of G1-phase cells. PMC2857444
Cardiac HSA primary cells 7.6 ±5.6 µM 72 h To test the role of MEK signaling in HSA growth and proliferation, results showed that CI-1040 reduced cell viability PMC3769440
Cutaneous HSA primary cells 3.3 ±1.1 µM 72 h To test the role of MEK signaling in HSA growth and proliferation, results showed that CI-1040 reduced cell viability PMC3769440
Visceral HSA primary cells 2.7 ±1.5 µM 72 h To test the role of MEK signaling in HSA growth and proliferation, results showed that CI-1040 reduced cell viability PMC3769440
SUM185 cells 1 μM 2 h Inhibition of MEK1 with CI-1040 restored radiosensitization with 45% fewer surviving colonies when combined with radiation PMC2799330
SUM102 cells 1 μM 2 h Inhibition of MEK1 with CI-1040 resulted in 95% inhibition of surviving colonies when combined with radiation PMC2799330

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice ELT3 cell xenograft model Oral 150 mg/kg Twice daily for 7 weeks CI-1040 significantly reduced the levels of circulating ELT3 cells in the blood of E2-treated animals and completely blocked E2-induced lung metastasis. PMC2637277
Nude mice Nude mouse tumor model Intraperitoneal injection 150 mg/kg Once daily for 3 weeks To evaluate the inhibitory effect of CI-1040 on tumor growth in vivo. Results showed that CI-1040 significantly inhibited tumor growth in KRAS mutant MDAH2774 cells but had no significant effect on wild-type SKOV3 cells. PMC2607229
BALB/c mice C26 tumor model Oral gavage 300 mg/kg Once daily for 28 days C26/PD0325901r tumors exhibited significant resistance to CI-1040 treatment, while the growth of parental tumors was significantly delayed PMC1501146
Nude mice Cutaneous HSA xenograft model Oral 48 mg/kg Twice daily for 42 days To test the effect of MEK inhibitor CI-1040 on the growth of HSA xenografts, results showed that CI-1040 significantly inhibited tumor growth PMC3769440

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00034827 Colorectal Neoplasms|Breast Ne... More >>oplasms|Carcinoma, Non-Small-Cell Lung|Pancreatic Neoplasms Less << PHASE2 COMPLETED 2025-05-03 Pfizer Investigational Site, B... More >>irmingham, Alabama, 35205, United States|Pfizer Investigational Site, Birmingham, Alabama, 35233, United States|Pfizer Investigational Site, Blendora, California, 91740, United States|Pfizer Investigational Site, Glendale, California, 91204, United States|Pfizer Investigational Site, Huntington Beach, California, 92648, United States|Pfizer Investigational Site, Long Beach, California, 90813, United States|Pfizer Investigational Site, Los Alamitos, California, 90720, United States|Pfizer Investigational Site, Los Angeles, California, 90048, United States|Pfizer Investigational Site, Los Angeles, California, 90095, United States|Pfizer Investigational Site, Mission Hills, California, 91345, United States|Pfizer Investigational Site, Northridge, California, 91328, United States|Pfizer Investigational Site, Oxnard, California, 93030, United States|Pfizer Investigational Site, Pasadena, California, 91105, United States|Pfizer Investigational Site, Pomona, California, 91767, United States|Pfizer Investigational Site, Rancho Cucamonga, California, 91730, United States|Pfizer Investigational Site, Redondo Beach, California, 90277, United States|Pfizer Investigational Site, Santa Monica, California, 90404, United States|Pfizer Investigational Site, Torrance, California, 90505, United States|Pfizer Investigational Site, Ventura, California, 93003, United States|Pfizer Investigational Site, West Covina, California, 91790, United States|Pfizer Investigational Site, Atlanta, Georgia, 30342, United States|Pfizer Investigational Site, Decatur, Georgia, 30033, United States|Pfizer Investigational Site, Macon, Georgia, 30342, United States|Pfizer Investigational Site, Crestview Hills, Kentucky, 41017, United States|Pfizer Investigational Site, Detroit, Michigan, 48201, United States|Pfizer Investigational Site, Rochester, Minnesota, 55905, United States|Pfizer Investigational Site, Cincinnait, Ohio, 45236, United States|Pfizer Investigational Site, Cincinnati, Ohio, 45219, United States|Pfizer Investigational Site, Cincinnati, Ohio, 45230, United States|Pfizer Investigational Site, Cincinnati, Ohio, 45242, United States Less <<
NCT00033384 Breast Cancer|Colorectal Cance... More >>r|Lung Cancer|Pancreatic Cancer Less << PHASE2 COMPLETED 2025-11-03 University of Alabama at Birmi... More >>ngham Comprehensive Cancer Center, Birmingham, Alabama, 35294-3300, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.45mL

2.09mL

1.04mL

20.89mL

4.18mL

2.09mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

Historical Records

Categories