PD 184352 (Synonyms: CI-1040)

Name: CI-1040
Brand: MedChemExpress
SKU: HY-50295
Rating: 5.0 (23 reviews)

製品番号: HY-50295 純度: 99.91%: Data Sheet SDS COA 取扱説明書
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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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CAS 番号 : 212631-79-3

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 64	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 64	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$61	在庫あり	Estimated Time of Arrival: December 31
10 mg	$99	在庫あり	Estimated Time of Arrival: December 31
25 mg	$180	在庫あり	Estimated Time of Arrival: December 31
50 mg	$277	在庫あり	Estimated Time of Arrival: December 31
100 mg	$445	在庫あり	Estimated Time of Arrival: December 31
200 mg	$580	在庫あり	Estimated Time of Arrival: December 31
1 g	$1500	在庫あり	Estimated Time of Arrival: December 31
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カスタマーレビュー

Based on 23 publication(s) in Google Scholar

Other Forms of CI-1040:

CI-1040 hydrochloride お問い合わせ
CI-1040 (Standard) お問い合わせ

顧客検証

: 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.

: 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.

: 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.

MEK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

MEK1 MEK2 MEK5 MEK MAP2K4/MEK4 MAP2K7/MEK7

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純度とドキュメンテーション
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製品説明

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)

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	EC₅₀	100 1 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]
786-0	EC₅₀	100 1 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]
A549	CC₅₀	312 3 Compound: 55; PD184352, CI-1040	Cytotoxicity against human A549 cells Cytotoxicity against human A549 cells	[PMID: 33539089]
Caco-2	IC₅₀	> 1000 1 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]
Caco-2	IC₅₀	>1 3 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]
A375P	EC₅₀	0.24 3 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]
Colon 26	IC₅₀	53 1 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]
Colon 26	IC₅₀	53 1 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]
A549	CC₅₀	312 3 Compound: 55; PD184352, CI-1040	Cytotoxicity against human A549 cells Cytotoxicity against human A549 cells	[PMID: 33539089]
LoVo	IC₅₀	131 1 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]
786-0	EC₅₀	100 1 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]
COLO 205	EC₅₀	0.23 3 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]
LoVo	IC₅₀	131 1 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]
Caco-2	IC₅₀	> 1000 1 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]
Colon 26	IC₅₀	53 1 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 3 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 3 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 3 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 3 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 3 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 1 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 3 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 3 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 3 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 3 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]

体外実験

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.

体内実験

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.

臨床実験

分子量

478.66

分子式

C₁₇H₁₄ClF₂IN₂O₂

CAS 番号

212631-79-3

Appearance

Solid

Color

White to off-white

SMILES

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.91%

Select Batch:

データシート (278 KB) SDS (598 KB)

COA (251 KB) HNMR (282 KB) LCMS (95 KB)

取扱説明書 (2659 KB)

参考文献

[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]

細胞実験 ^[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) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[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) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[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]

Complete Stock Solution Preparation Table

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

CI-1040 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CI-1040212631-79-3PD 184352CI1040CI 1040PD184352PD-184352MEKApoptosisMitogen-activated protein kinase kinaseMAPKKMAP2KInhibitorinhibitorinhibit

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PD 184352 (Synonyms: CI-1040)

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MEK アイソフォーム固有の製品をすべて表示:

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参考文献

カスタマーレビュー

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

CI-1040 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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PD 184352 (Synonyms: CI-1040)

カスタマーレビュー

Other Forms of CI-1040:

PD 184352 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

MEK アイソフォーム固有の製品をすべて表示:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

PD 184352 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

CI-1040 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

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Request for HNMR Report

Request for HNMR Report