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CI-1040

Catalog No. T2443 CAS 212631-79-3

Synonyms: PD 184352

CI-1040 (PD 184352) (PD184352) is an ATP non-competitive MEK1/2 inhibitor (IC50: 17 nM).

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CI-1040, CAS 212631-79-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 48.00
10 mg	In stock	$ 77.00
25 mg	In stock	$ 150.00
50 mg	In stock	$ 231.00
100 mg	In stock	$ 385.00
200 mg	In stock	$ 482.00
1 mL * 10 mM (in DMSO)	In stock	$ 53.00

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Purity: 99.1%

Biological Description

Chemical Properties

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Description	CI-1040 (PD 184352) (PD184352) is an ATP non-competitive MEK1/2 inhibitor (IC50: 17 nM).
Targets&IC50	MEK2:17 nM (cell free), MEK1:17 nM (cell free)
In vitro	PD 184352 (CI-1040) also substantially reduced steady-state levels of phosphorylated MAPK (pMAPK) in a diverse panel of tumor lines grown in the presence of serum. Treatment of colon 26 cells for 1 hour with 1 μM PD 184352 produced a reduction of pMAPK levels of more than 75%. Treatment of colon 26 cells with 10 μM PD 184352 did not inhibit the phosphorylation of Jun kinase, p38 kinase or AKT [1]. The IC50 for inhibition of MKK1 by PD 184352 was 0.3 μM, 15-fold higher than the concentration required to inhibit the EGF-induced activation of ERK2 in Swiss 3T3 cells. The activation of MKK1 in cells was inhibited by 50% at 2 nM PD 184352 [2]. CI-1040 induced apoptosis and inhibited proliferation in U-937 cells in a dose and time-dependent manner. CI-1040 induced a significant increase in PUMA mRNA and protein levels. Knockdown of PUMA by PUMA siRNA transfection inhibited CI-1040-induced apoptosis and proliferation inhibition in U-937 cells [3].
In vivo	The tumors were excised at 1 hour and 6 hours after treatment with PD 184352 (150 mg/kg, i.p. or p.o.). Treatment with PD 184352 completely suppressed MAPK phosphorylation by either route of administration for at least 6 hours. MAPK phosphorylation returned at 12 hours after dosing and attained control levels by 24 hours [1]. In vivo, the systemic administration of the MEK inhibitor CI-1040 reduced adenoma formation to a third and significantly restored lung structure. The proliferation rate of lung cells of mice treated with CL-1040 was decreased without any obvious effects on the differentiation of pneumocytes [4].
Kinase Assay	All protein kinase activities were linear with respect to time in every incubation. Assays were performed either manually for 10 min at 30 °C in 50 μl incubations using [γ-32P]ATP, or with a Biomek 2000 Laboratory Automation Workstation in a 96-well format for 40 min at ambient temperature in 25 μl incubations using [γ-33P]ATP. The concentrations of ATP and magnesium acetate were 0.1 mM and 10 mM respectively, unless stated otherwise. This concentration of ATP is 5–10-fold higher than the Km for ATP of most of the protein kinases studied in the present paper, but lower than the normal intracellular concentration, which is in the millimolar range. All assays were initiated with MgATP. Manual assays were terminated by spotting aliquots of each incubation on to phosphocellulose paper, followed by immersion in 50 mM phosphoric acid. Robotic assays were terminated by the addition of 5 μl of 0.5 M phosphoric acid before spotting aliquots on to P30 filter mats. All papers were then washed four times in 50 mM phosphoric acid to remove ATP, once in acetone (manual incubations) or methanol (robotic incubations), and then dried and counted for radioactivity [2].
Cell Research	Cells were planted seeded in T-75 cm2 flasks and treated the next day for 24 h with either DMSO or PD 184352. Single-cell suspensions were collected, and pellets were fixed in ice-cold ethanol (70%) for 30 min. After centrifugation of the samples, propidium iodide (50 μg/ml) and RNase (30 units/ml) were added to the pellets for 20 min at 37 °C. After filtration, samples were analyzed by flow cytometry [1].
Animal Research	Tumor fragments (approximately 3 mm^3 in size) were implanted subcutaneously into the right axillae of CD2F1 male mice (colon 26 studies) or female nude mice (HT-29 studies) 4–6 weeks old. Treatment was administered by gavage or intraperitoneally and was initiated either the day after tumor implantation (colon 26) or when tumors reached approximately 200 mg in size (HT-29). PD 184352 was prepared in a vehicle of 10% Cremophore EL, 10% ethanol and 80% water. Tumor size was evaluated periodically by caliper measurements, generally three times per week. Percent tumor growth inhibition was calculated as [(T–C)/number of days of treatment] × 100, with T and C being defined as the time required for treated and control tumors, respectively, to reach 750 mg (colon 26) or to reach twofold growth (HT-29) [1].

Synonyms	PD 184352
Molecular Weight	478.66
Formula	C17H14ClF2IN2O2
CAS No.	212631-79-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 12 mg/mL (25 mM)

DMSO: 47.9 mg/mL (100 mM)

References and Literature

1. Sebolt-Leopold JS, et al. Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo. Nat Med. 1999 Jul;5(7):810-6. 2. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. 3. 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. 4. 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.

Citations

1. Wu R, Pang S, Lv W, et al.Injectable pH‐Responsive CI1040 Delayed‐Release Hydrogel for the Treatment of Tendon Adhesion.Advanced Functional Materials.2024: 2314731.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Highly Selective Inhibitor Library Fluorochemical Library MAPK Inhibitor Library

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Keywords

CI-1040 212631-79-3 Apoptosis MAPK MEK Inhibitor MAP2K PD184352 MAPKK CI 1040 PD-184352 Mitogen-activated protein kinase kinase CI1040 PD 184352 inhibit inhibitor

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