Art. -Nr.: HY-50295

CI-1040

(Synonyms: PD 184352)

23 Cited Publications

Kundenbewertung

Based on 23 publication(s) in Google Scholar

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

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Reinheit: 99.91%
CAS. Nr.: 212631-79-3
Formel: C₁₇H₁₄ClF₂IN₂O₂
Molecular Weight:478.66

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

CI-1040 Chemical Structure

CAS. Nr.: 212631-79-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (23)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

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

IC₅₀ & Target^[1]

MEK1

17 nM (IC₅₀)

Alle MEK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	EC₅₀	100 nM Compound: CI-1040	Inhibition of CK2 in human 786-0 cells assessed as decrease in Akt1 phosphorylation at Ser129 after 24 hrs by Western blot analysis Inhibition of CK2 in human 786-0 cells assessed as decrease in Akt1 phosphorylation at Ser129 after 24 hrs by Western blot analysis	[PMID: 30689946]
A375P	EC₅₀	0.24 μM Compound: Chemical probe: CI-1040	Antiproliferative activity against human A375P cells expressing B-Raf V600E mutant assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay Antiproliferative activity against human A375P cells expressing B-Raf V600E mutant assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay	[PMID: 17145850]
A549	CC₅₀	312 μM Compound: 55; PD184352, CI-1040	Cytotoxicity against human A549 cells Cytotoxicity against human A549 cells	[PMID: 33539089]
Caco-2	IC₅₀	>1000 nM Compound: 1	Inhibitory concentration against CaCo cell proliferation, was determined using Cellular proliferation assays Inhibitory concentration against CaCo cell proliferation, was determined using Cellular proliferation assays	[PMID: 12941327]
COLO 205	EC₅₀	0.23 μM Compound: Chemical probe: CI-1040	Antiproliferative activity against human COLO 205 cells expressing B-Raf V600E mutant assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay Antiproliferative activity against human COLO 205 cells expressing B-Raf V600E mutant assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay	[PMID: 17145850]
Colon 26	IC₅₀	53 nM Compound: PD-184352, CI-1040	Inhibition of MEK in mouse Colon 26 cells by Western blot Inhibition of MEK in mouse Colon 26 cells by Western blot	[PMID: 18951019]
HCT-116	EC₅₀	2.2 μM Compound: Chemical probe: CI-1040	Antiproliferative activity against human HCT-116 cells expressing K-Ras G13D mutant assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay Antiproliferative activity against human HCT-116 cells expressing K-Ras G13D mutant assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay	[PMID: 17145850]
HFF	EC₅₀	4.9 μM Compound: Chemical probe: CI-1040	Cytotoxicity against human HFF cells assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay Cytotoxicity against human HFF cells assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay	[PMID: 17145850]
HMEC	EC₅₀	0.58 μM Compound: Chemical probe: CI-1040	Cytotoxicity against human HMEC cells assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay Cytotoxicity against human HMEC cells assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay	[PMID: 17145850]
HT-1080	EC₅₀	1.6 μM Compound: Chemical probe: CI-1040	Antiproliferative activity against human HT-1080 cells expressing N-Ras Q61K mutant assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay Antiproliferative activity against human HT-1080 cells expressing N-Ras Q61K mutant assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay	[PMID: 17145850]
HT-29	EC₅₀	0.36 μM Compound: Chemical probe: CI-1040	Antiproliferative activity against human HT-29 cells expressing B-Raf V600E mutant assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay Antiproliferative activity against human HT-29 cells expressing B-Raf V600E mutant assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay	[PMID: 17145850]
LoVo	IC₅₀	131 nM Compound: 1	Inhibitory concentration against LoVo cell proliferation, was determined using Cellular proliferation assays Inhibitory concentration against LoVo cell proliferation, was determined using Cellular proliferation assays	[PMID: 12941327]
Malme-3M	EC₅₀	0.44 μM Compound: Chemical probe: CI-1040	Antiproliferative activity against human Malme-3M cells expressing B-Raf V600E mutant assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay Antiproliferative activity against human Malme-3M cells expressing B-Raf V600E mutant assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay	[PMID: 17145850]
PrEC	EC₅₀	0.49 μM Compound: Chemical probe: CI-1040	Cytotoxicity against human PrEC cells assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay Cytotoxicity against human PrEC cells assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay	[PMID: 17145850]
SK-MEL-2	EC₅₀	0.36 μM Compound: Chemical probe: CI-1040	Antiproliferative activity against human SK-MEL-2 cells expressing N-Ras Q61R mutant assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay Antiproliferative activity against human SK-MEL-2 cells expressing N-Ras Q61R mutant assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay	[PMID: 17145850]
SK-MEL-28	EC₅₀	0.22 μM Compound: Chemical probe: CI-1040	Antiproliferative activity against human SK-MEL-28 cells expressing B-Raf V600E mutant assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay Antiproliferative activity against human SK-MEL-28 cells expressing B-Raf V600E mutant assessed as decrease in cell growth incubated for 72 hrs by CellTiter-Glo based luminescence assay	[PMID: 17145850]

In Vitro

CI-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^[1].
CI-1040 induces apoptosis and inhibits proliferation in U-937 cells in a dose and time-dependent manner. CI-1040 induces a significant increase in PUMA mRNA and protein levels^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The 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^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 212631-79-3
Appearance Solid
Molecular Weight 478.66
Formel C₁₇H₁₄ClF₂IN₂O₂
Color White to off-white
SMILES

O=C(C1=CC=C(C(F)=C1NC2=CC=C(I)C=C2Cl)F)NOCC3CC3
Synonyms

PD 184352
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (23)

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Journal Impact Factor

Nat Methods

Reconstruction of dynamic mammary mini gland in vitro for normal physiology and oncogenesis. [Abstract]

2023 Dec;20(12):2021-2033. PMID: 37919421
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Clin Cancer Res

Gene Expression Signatures Identify Novel Therapeutics for Metastatic Pancreatic Neuroendocrine Tumors. [Abstract]

2020 Apr 15;26(8):2011-2021. PMID: 31937620
Int J Biol Macromol

Isolation, structural characterization and immunoregulatory activity of a novel acidic polysaccharide from Ganoderma sinense. [Abstract]

2026 Mar 3:151196. PMID: 41786176
Int J Biol Macromol

Cordyceps militaris polysaccharide converts immunosuppressive macrophages into M1-like phenotype and activates T lymphocytes by inhibiting the PD-L1/PD-1 axis between TAMs and T lymphocytes. [Abstract]

2020 May 1;150:261-280. PMID: 32044366
Int J Biol Macromol

Polysaccharide isolated from Sarcodon aspratus induces RAW264.7 activity via TLR4-mediated NF-κB and MAPK signaling pathways. [Abstract]

2018 Dec;120(Pt A):1039-1047. PMID: 30171950
Oncogenesis

A novel small-molecule inhibitor of trefoil factor 3 (TFF3) potentiates MEK1/2 inhibition in lung adenocarcinoma. [Abstract]

2019 Nov 4;8(11):65. PMID: 31685806

CI-1040 purchased from MedChemExpress. Usage Cited in: Oncogenesis. 2019 Nov 4;8(11):65. [Abstract]

Western blot analysis of p-ERK and ERK protein levels in cell lysates of H1975 treated with AMPC, CI-1040 for 24 h. The levels of the total ERK was used as an input control.
Cancer Cell Int

Construction of a prognostic model with histone modification-related genes and identification of potential drugs in pancreatic cancer. [Abstract]

2021 Jun 5;21(1):291. PMID: 34090418
Biochem Pharmacol

PD184352 exerts anti-inflammatory and antioxidant effects by promoting activation of the Nrf2/HO-1 axis. [Abstract]

2023 May:211:115542. PMID: 37028460

CI-1040 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2023 May:211:115542. [Abstract]

CI-1040 (PD 184352; 10, 20, 40 nM; 48 h) significantly inhibits the expression of iNOS and COX2 in a dose-dependent manner in ATDC5 cells.
Life Sci

A novel exosome-like nanovesicles from Cordyceps militaris potentiate immunomodulatory and anti-tumor effect by reprogramming macrophages. [Abstract]

2024 Dec 1:358:123163. PMID: 39442867
Glia

Inhibition of MAPK/ERK pathway promotes oligodendrocytes generation and recovery of demyelinating diseases. [Abstract]

2019 Jul;67(7):1320-1332. PMID: 30815939
Biol Direct

Nuclear respiratory factor 1 drives hepatocellular carcinoma progression by activating LPCAT1-ERK1/2-CREB axis. [Abstract]

2023 Oct 24;18(1):67. PMID: 37875967
Brain Commun

Spike-induced cytoarchitectonic changes in epileptic human cortex are reduced via MAP2K inhibition. [Abstract]

2024 Apr 29;6(3):fcae152. PMID: 38741662
J Virol

Targeting Cell Cycle Facilitates E1A-Independent Adenoviral Replication. [Abstract]

2023 Jun 29;97(6):e0037023. PMID: 37219458
Curr Oncol

Direct Targeting of the Raf-MEK-ERK Signaling Cascade Inhibits Neuroblastoma Growth. [Abstract]

2022 Sep 10;29(9):6508-6522. PMID: 36135081
Neurotox Res

Lithium Chloride Facilitates Autophagy Following Spinal Cord Injury via ERK-dependent Pathway. [Abstract]

2017 Nov;32(4):535-543. PMID: 28593525

CI-1040 purchased from MedChemExpress. Usage Cited in: Neurotox Res. 2017 Nov;32(4):535-543. [Abstract]

Lithium promotes autophagy flux by activating MEK/ERK pathway in cells. Original Western blot showing LC3-II and p62 abundance following treatment with lithium in the presence of PD184352 and SCH772984 in neurons. Arithmetic means±SEM (n=5) showing LC3-II abundance following treatment with lithium in the presence of PD184352 and SCH772984 in neurons.
Biochim Biophys Acta Gen Subj

Human milk derived peptide AOPDM1 attenuates obesity by restricting adipogenic differentiation through MAPK signalling. [Abstract]

2021 Mar;1865(3):129836. PMID: 33370564
bioRxiv

2025 Jun 24.
McGill University

2023 Dec.
Research Square Preprint

2023 Aug 25.
Research Square Print

Nov 2nd, 2022
Oncotarget

MEK is a promising target in the basal subtype of bladder cancer. [Abstract]

2020 Nov 3;11(44):3921-3932. PMID: 33216841
ACS Comb Sci

Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]

2019 Dec 9;21(12):805-816. PMID: 31689077

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (208.92 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0892 mL

10.4458 mL

20.8917 mL

5 mM

0.4178 mL

2.0892 mL

4.1783 mL

10 mM

0.2089 mL

1.0446 mL

2.0892 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.22 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.35 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[2]

The MEK inhibitor CI-1040 is dissolved in DMSO as 10 mM stock solutions and used in cell culture at final concentration 50 mg/mL. U-937 cells are pretreated for 24 hrs with 5 and 20 uM CI- 1040, then transfected with wt-p53 siRNA or PUMA siRNA for 48 hrs. Then 20 mL of MTT solution are added to each well and incubated further for 2 hours. Upon termination, the supernatant is aspirated and the MTT formazan formed by metabolically viable cells is dissolved in 100 mL of isopropanol. The plates are mixed for 30 minutes on a gyratory shaker, and absorbance is measured at 595 nm using a plate reader^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[3]

Mice: The lung cancer mouse model is generated by targeting constitutively active C-Raf kinase to the lung. BAY 43-9006 or CI-1040 is daily intraperitoneal injected at a dose of 100 mg/kg from 4 months of age over a period of 21 days. Lungs were isolated and analyzed at the end of the treatment period^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (598 KB)
- English - EN (598 KB)
- Français - FR (598 KB)
- Deutsch - DE (598 KB)
- Norwegian - NO (598 KB)
- Español - ES (598 KB)
- Swedish - SV (598 KB)
- Italian - IT (598 KB)
- Portuguese - PT (598 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. 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. [Content Brief]

[2]. Wei CR, et al. MEK inhibitor CI-1040 induces apoptosis in acute myeloid leukemia cells in vitro. Eur Rev Med Pharmacol Sci. 2016 May;20(10):1961-8. [Content Brief]

[3]. Kramer BW, et al. Use of mitogenic cascade blockers for treatment of C-Raf induced lung adenoma in vivo: CI-1040strongly reduces growth and improves lung structure. BMC Cancer. 2004 Jun 1;4:24. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0892 mL	10.4458 mL	20.8917 mL	52.2291 mL
	5 mM	0.4178 mL	2.0892 mL	4.1783 mL	10.4458 mL
	10 mM	0.2089 mL	1.0446 mL	2.0892 mL	5.2229 mL
	15 mM	0.1393 mL	0.6964 mL	1.3928 mL	3.4819 mL
	20 mM	0.1045 mL	0.5223 mL	1.0446 mL	2.6115 mL
	25 mM	0.0836 mL	0.4178 mL	0.8357 mL	2.0892 mL
	30 mM	0.0696 mL	0.3482 mL	0.6964 mL	1.7410 mL
	40 mM	0.0522 mL	0.2611 mL	0.5223 mL	1.3057 mL
	50 mM	0.0418 mL	0.2089 mL	0.4178 mL	1.0446 mL
	60 mM	0.0348 mL	0.1741 mL	0.3482 mL	0.8705 mL
	80 mM	0.0261 mL	0.1306 mL	0.2611 mL	0.6529 mL
	100 mM	0.0209 mL	0.1045 mL	0.2089 mL	0.5223 mL

Keywords

CI-1040

23 Cited Publications

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CI-1040

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Publications Citing Use of MedChemExpress (MCE) CI-1040

Alle MEK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (23)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CI-1040 Related Classifications

Art. -Nr.: HY-50295