Mirdametinib (Synonyms: PD0325901; PD325901)

Name: Mirdametinib
Brand: MedChemExpress
SKU: HY-10254
Rating: 5.0 (104 reviews)

Cat. No.: HY-10254 Purity: 99.95%: FAQs
Data Sheet SDS COA Handling Instructions

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Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC₅₀ of 0.33 nM. Mirdametinib exhibits a K_i^app of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts.

For research use only. We do not sell to patients.

Mirdametinib Chemical Structure

CAS No. : 391210-10-9

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
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10 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 104 publication(s) in Google Scholar

Other Forms of Mirdametinib:

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100 Publications Citing Use of MCE Mirdametinib

: Mirdametinib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2020 Apr 2;524(2):280-287. [Abstract]; Western blot analysis of Tcf7l1 protein levels in mESCs pre-treated with D4476 or DMAT and then treated with CHIR or PD03 for 24 h.

: Mirdametinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 28;37(1):128. [Abstract]; MHCC-97H cells are transfected with control or supervillin-specific siRNA for 48 h, exposed to hypoxia for 16 h, and lysates are assayed for the relative amounts of GTP-loaded (activated) Rac1, Cdc42, and RhoA. Cells that have been transfected with control RNAi are treated with a PD0325901 or SB239063 before assaying for GTP-Rac1, Cdc42, and RhoA levels.

: Mirdametinib purchased from MedChemExpress. Usage Cited in: Viruses. 2018 Apr 13;10(4). pii: E191. [Abstract]; H2.35 cells are serum starved for 72 h and then were pre-treated with either DMSO or BI-D1870 (p90 IN, 10 µM). Cells are infected with MP12 (MOI 5) for one hour, followed by removal of viral inoculum, and addition of growth medium containing DMSO or p90 IN (10 µM). At 18 hpi, cell lysates are collected for western blot analysis.

: Mirdametinib purchased from MedChemExpress. Usage Cited in: Viruses. 2018 Apr 13;10(4). pii: E191. [Abstract]; H2.35 cells are serum starved for 72 h and then are pre-treated with either DMSO or 10 µM PD0325901 (ERK IN). Cells are infected with MP12 (MOI 5) for one hour, followed by removal of viral inoculum, and addition of growth medium containing DMSO or 10 µM ERK IN. At 18 hpi, cell lysates are collected for western blot analysis.

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Protocol
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References
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Description

IC₅₀ & Target^[1]^[2]

MEK1

1 nM (Ki)

MEK2

1 nM (Ki)

MEK

0.33 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	13 nM Compound: PD325901	Antiproliferative activity against human A375 cells expressing BRAF V600E mutant after 72 hrs by Cell titer-glo assay Antiproliferative activity against human A375 cells expressing BRAF V600E mutant after 72 hrs by Cell titer-glo assay	[PMID: 23474388]
A-431	IC₅₀	< 0.014 μM Compound: PD-0325901	Inhibition of MEK/ERK signaling pathway in TNFalpha-stimulated human A431 cells transfected with COT siRNA assessed as reduction in ERK1/2 phosphorylation incubated for 60 mins followed by stimulation with TNFalpha for 10 mins by Western blot analysis Inhibition of MEK/ERK signaling pathway in TNFalpha-stimulated human A431 cells transfected with COT siRNA assessed as reduction in ERK1/2 phosphorylation incubated for 60 mins followed by stimulation with TNFalpha for 10 mins by Western blot analysis	[PMID: 27502541]
A-431	IC₅₀	0.038 μM Compound: PD-0325901	Inhibition of MEK/ERK signaling pathway in EGF-stimulated human A431 cells transfected with COT siRNA assessed as reduction in ERK1/2 phosphorylation incubated for 60 mins followed by stimulation with EGF for 10 mins by Western blot analysis Inhibition of MEK/ERK signaling pathway in EGF-stimulated human A431 cells transfected with COT siRNA assessed as reduction in ERK1/2 phosphorylation incubated for 60 mins followed by stimulation with EGF for 10 mins by Western blot analysis	[PMID: 27502541]
A549	IC₅₀	0.06 μM Compound: PD0325901	Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay	[PMID: 32305784]
COLO 205	GI₅₀	0.2 nM Compound: 4; PD0325901	Antiproliferative activity against human COLO205 cells assessed as reduction in cell growth after 3 days by WST8 assay Antiproliferative activity against human COLO205 cells assessed as reduction in cell growth after 3 days by WST8 assay	[PMID: 31730343]
HCT-116	IC₅₀	0.09 μM Compound: PD0325901	Antiproliferative activity against human HCT116 cells harboring KRAS G13D mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay Antiproliferative activity against human HCT116 cells harboring KRAS G13D mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay	[PMID: 32305784]
HL-60	IC₅₀	0.0013 μM Compound: PD0325901	Antiproliferative activity against human HL60 cells harboring NRAS K61L mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay Antiproliferative activity against human HL60 cells harboring NRAS K61L mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay	[PMID: 32305784]
HT-29	GI₅₀	3.1 nM Compound: 4; PD0325901	Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth after 3 days by MTT assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth after 3 days by MTT assay	[PMID: 31730343]
MDA-MB-231	IC₅₀	0.082 μM Compound: PD0325901	Antiproliferative activity against human MDA-MB-231 cells harboring KRAS G13D/BRAF G464V mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay Antiproliferative activity against human MDA-MB-231 cells harboring KRAS G13D/BRAF G464V mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay	[PMID: 32305784]
MDA-MB-231	GI₅₀	1 μM Compound: PD-0325901	Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
Sf21	IC₅₀	> 25 μM Compound: PD-0325901	Inhibition of human COT (66 to 395 residues) expressed in Sf21 cells using 5-Fluo-Ahx-AGAGSGQLIDSNleANSFVGTR-NH2 as substrate after 60 mins by caliper microfluidic mobility shift assay Inhibition of human COT (66 to 395 residues) expressed in Sf21 cells using 5-Fluo-Ahx-AGAGSGQLIDSNleANSFVGTR-NH2 as substrate after 60 mins by caliper microfluidic mobility shift assay	[PMID: 27502541]
SK-MEL-28	GI₅₀	2.9 nM Compound: 4; PD0325901	Antiproliferative activity against human SK-MEL-28 cells assessed as reduction in cell growth after 3 days by MTT assay Antiproliferative activity against human SK-MEL-28 cells assessed as reduction in cell growth after 3 days by MTT assay	[PMID: 31730343]
SU-DHL-1	GI₅₀	350 nM Compound: 1; PD0325901	Antiproliferative activity against human SU-DHL-1 cells incubated for 3 days by WST8 assay Antiproliferative activity against human SU-DHL-1 cells incubated for 3 days by WST8 assay	[PMID: 33284613]
UACC-257	GI₅₀	0.2 nM Compound: 4; PD0325901	Antiproliferative activity against human UACC257 cells assessed as reduction in cell growth after 3 days by MTT assay Antiproliferative activity against human UACC257 cells assessed as reduction in cell growth after 3 days by MTT assay	[PMID: 31730343]

In Vitro

Mirdametinib (PD325901; 0.0064, 0.032, 0.16, 0.8, 4, 20, 100 nM; for 2 days) inhibits the growth of Papillary thyroid carcinomas (PTC) cell lines (TPC-1 cells and K2 cells) with GC₅₀ of 11 nM and 6.3 nM, respectively^[3].
Mirdametinib (100 nmol/L; for 4 days) induces apoptosis in K2 cells (top) or TPC-1 cells^[3].
Mirdametinib (0.1, 1, 10, 100, 1000 nM; for 1 hour) suppresses the expression of p-ERK1/2 in K2 cells (top) or TPC-1 cells^[3].
Mirdametinib prevents the growth of melanoma cell lines. Mirdametinib significantly prevents the the growth of PTC cells harboring a BRAF mutation at very low concentration (10 nM)^[3].

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

In Vivo

Mirdametinib (25 mg/kg, p.o.) inhibits phosphorylation of ERK by more than 50% at 24 hours post-dosing. Mirdametinib (25 mg/kg/day; po) produces a 70% incidence of complete tumor responses (C26 model)^[2].
Mirdametinib (20-25 mg/kg/day; oral gavage; for 3 weeks (5 consecutive days/week)) suppresses tumor growth completely in mice inoculated with PTC cells carrying a BRAF mutation (K2) and significantly decreased tumor growth in mice inoculated with PTC cells carrying the RET/PTC1 rearrangement (TPC-1) in athymic Ncr-nu/nu mice at ages 6 to 8 weeks^[3].

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

Clinical Trial

Molecular Weight

482.19

Formula

C₁₆H₁₄F₃IN₂O₄

CAS No.

391210-10-9

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(C(F)=C1NC2=CC=C(I)C=C2F)F)NOC[C@H](O)CO

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : ≥ 56 mg/mL (116.14 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	2.0739 mL	10.3694 mL	20.7387 mL
5 mM	0.4148 mL	2.0739 mL	4.1477 mL
10 mM	0.2074 mL	1.0369 mL	2.0739 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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: ≥ 2.08 mg/mL (4.31 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.31 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.31 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:

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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.

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (281 KB) SDS (644 KB)

COA (249 KB) HNMR (191 KB) LCMS (315 KB) Elemental Analysis Report (107 KB)

Handling Instructions (2659 KB)

References

[1]. Barrett SD, et al. The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6501-4. [Content Brief]

[2]. Judith S. Sebolt-Leopold, et al. The biological profile of PD 0325901: A second generation analog of CI-1040 with improved pharmaceutical potential

[3]. Henderson YC, et al. MEK inhibitor PD0325901 significantly reduces the growth of papillary thyroid carcinoma cells in vitro and in vivo. Mol Cancer Ther. 2010 Jul;9(7):1968-76. [Content Brief]

Kinase Assay ^[1]	Incorporation of ³²P into myelin basic protein (MBP) is assayed in the presence of a glutathione S-transferase fusion protein containing p44MAP kinase (GST-MAPK) and a glutathione S-transferase protein containing p45MEK (GST-MEK). The assay solution contained 20 mM HEPES, pH 7.4, 10 mM MgCl₂, 1 mM MnCl₂, 1 mM EGTA, 50 mM [gamma-³²P]ATP, 10 mg GST-MEK, 0.5 mg GST-MAPK and 40 mg MBP in a final volume of 100 mL. Reactions are stopped after 20 minutes by addition of trichloroacetic acid and filtered through a GF/C filter mat. ³²P retained on the filter mat is determined using a 1205 Betaplate. PD0325901 is assessed at various dose ranges in order to determine dose response curves. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[2]	PTC cells (1×10⁴) are seeded in 24-well plates with 1 mL of medium for 4 days in a 37°C incubator. MEK inhibitor PD0325901 at varying concentrations is added to the cells in triplicate on day 0. MTT dissolved in 0.8% NaCl solution at 5 mg/mL is added to each well (0.2 mL) on day 2 to test GC₅₀ or every day for cell growth curves. The cells are incubated at 37°C for 3 hours with MTT. The liquid is then aspirated from the wells and discarded. Stained cells are dissolved in 0.5 mL of DMSO and their absorption at 570 nm is measured using a Synergy HT multidetection microplate reader. For GC₅₀, cell growth is calculated as 100×(T−T₀)/(C−T₀), where T is the optical density of the wells treated with inhibitors after a 48-hour period, T₀ is the optical density at time zero, and C is the control optical density with DMSO only. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice (10-14 per group) are anesthetized s.c. with a cocktail. K2 and TPC-1 cells stably infected with a retrovirus expressing luciferase (5×10⁵ cells in 5 μL RPMI1640 medium) are inoculated into the thyroid gland, and the mice are monitored weekly for tumor growth by Xenogen using Living Image 3.0 software. One week after inoculation, PD0325901 is dissolved in 80 mM citric buffer (pH 7) by sonication and given to mice daily by oral gavage (20-25 mg/kg) for 3 weeks (5 consecutive days/week). Mice are sacrificed only due to tumor burden or loss of 20% of body weight. Tumor sizes are measured with calipers and tumor volume (V) is calculated by the formula (V=length×width×depth). Control mice are given 80 mM citric buffer (pH 7) alone. All in vivo experiments are done at least twice. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Barrett SD, et al. The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6501-4. [Content Brief] [2]. Judith S. Sebolt-Leopold, et al. The biological profile of PD 0325901: A second generation analog of CI-1040 with improved pharmaceutical potential [3]. Henderson YC, et al. MEK inhibitor PD0325901 significantly reduces the growth of papillary thyroid carcinoma cells in vitro and in vivo. Mol Cancer Ther. 2010 Jul;9(7):1968-76. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0739 mL	10.3694 mL	20.7387 mL	51.8468 mL
	5 mM	0.4148 mL	2.0739 mL	4.1477 mL	10.3694 mL
	10 mM	0.2074 mL	1.0369 mL	2.0739 mL	5.1847 mL
	15 mM	0.1383 mL	0.6913 mL	1.3826 mL	3.4565 mL
	20 mM	0.1037 mL	0.5185 mL	1.0369 mL	2.5923 mL
	25 mM	0.0830 mL	0.4148 mL	0.8295 mL	2.0739 mL
	30 mM	0.0691 mL	0.3456 mL	0.6913 mL	1.7282 mL
	40 mM	0.0518 mL	0.2592 mL	0.5185 mL	1.2962 mL
	50 mM	0.0415 mL	0.2074 mL	0.4148 mL	1.0369 mL
	60 mM	0.0346 mL	0.1728 mL	0.3456 mL	0.8641 mL
	80 mM	0.0259 mL	0.1296 mL	0.2592 mL	0.6481 mL
	100 mM	0.0207 mL	0.1037 mL	0.2074 mL	0.5185 mL

Mirdametinib Related Classifications

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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:

Mirdametinib391210-10-9PD0325901 PD325901PD 0325901PD-0325901PD325901PD 325901PD-325901MEKAutophagyApoptosisMitogen-activated protein kinase kinaseMAPKKMAP2KInhibitorinhibitorinhibit

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Mirdametinib (Synonyms: PD0325901; PD325901)

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Other Forms of Mirdametinib:

Mirdametinib Related Antibodies

100 Publications Citing Use of MCE Mirdametinib

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Complete Stock Solution Preparation Table

Mirdametinib Related Classifications

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