Cat. No.: HY-10254

Mirdametinib

(Synonyms: PD0325901; PD325901)

159 Cited Publications

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Based on 159 publication(s) in Google Scholar

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.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté: 99.95%
CAS No.: 391210-10-9
Formule: C₁₆H₁₄F₃IN₂O₄
Masse moléculaire:482.19

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4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Mirdametinib Chemical Structure

CAS No.: 391210-10-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (159)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
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Activité biologique

Description

IC₅₀ & Target^[1]^[2]

MEK1

1 nM (Ki)

MEK2

1 nM (Ki)

MEK

0.33 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform MEK :

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-375	GI₅₀	1.28 nM Compound: 5; PD-325901	Antiproliferative activity against human A-375 cells harboring BRAF V600E mutant assessed as cell growth inhibition incubated for 72 hrs in the absence of UV irradiation by CellTiter-Glo luminescent assay Antiproliferative activity against human A-375 cells harboring BRAF V600E mutant assessed as cell growth inhibition incubated for 72 hrs in the absence of UV irradiation by CellTiter-Glo luminescent assay	[PMID: 36924668]
A-375	GI₅₀	1.37 nM Compound: 5; PD-325901	Antiproliferative activity against human A-375 cells harboring BRAF V600E mutant assessed as cell growth inhibition preincubated with compound for 1 hrs followed by UV irradiation for 1 min and measured 72 hrs post compound treatment by CellTiter-Glo lumi Antiproliferative activity against human A-375 cells harboring BRAF V600E mutant assessed as cell growth inhibition preincubated with compound for 1 hrs followed by UV irradiation for 1 min and measured 72 hrs post compound treatment by CellTiter-Glo lumi	[PMID: 36924668]
A-375	GI₅₀	1.49 nM Compound: 5; PD-325901	Antiproliferative activity against human A-375 cells harboring BRAF V600E mutant assessed as cell growth inhibition preincubated with compound for 1 hrs followed by UV irradiation for 5 mins and measured 72 hrs post compound treatment by CellTiter-Glo lum Antiproliferative activity against human A-375 cells harboring BRAF V600E mutant assessed as cell growth inhibition preincubated with compound for 1 hrs followed by UV irradiation for 5 mins and measured 72 hrs post compound treatment by CellTiter-Glo lum	[PMID: 36924668]
A-375	GI₅₀	1.59 nM Compound: 5; PD-325901	Antiproliferative activity against human A-375 cells harboring BRAF V600E mutant assessed as cell growth inhibition preincubated with compound for 1 hrs followed by UV irradiation for 3 mins and measured 72 hrs post compound treatment by CellTiter-Glo lum Antiproliferative activity against human A-375 cells harboring BRAF V600E mutant assessed as cell growth inhibition preincubated with compound for 1 hrs followed by UV irradiation for 3 mins and measured 72 hrs post compound treatment by CellTiter-Glo lum	[PMID: 36924668]
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	166 nM Compound: PD325901	Antiproliferative activity against human A549 cells Antiproliferative activity against human A549 cells	[PMID: 23474388]
A549	IC₅₀	166 nM Compound: PD325901	Antiproliferative activity against human A549 cells harboring K-Ras mutation Antiproliferative activity against human A549 cells harboring K-Ras mutation	[PMID: 26611920]
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]
A549	CC₅₀	>100 μM Compound: PD-0325901	Cytotoxicity against human A549 cells Cytotoxicity against human A549 cells	[PMID: 33539089]
A549	GI₅₀	10.6 nM Compound: 5; PD-325901	Antiproliferative activity against human A549 cells harboring KRas G13S mutant assessed as cell growth inhibition preincubated with compound for 1 hrs followed by UV irradiation for 5 mins and measured 72 hrs post compound treatment by CellTiter-Glo lumin Antiproliferative activity against human A549 cells harboring KRas G13S mutant assessed as cell growth inhibition preincubated with compound for 1 hrs followed by UV irradiation for 5 mins and measured 72 hrs post compound treatment by CellTiter-Glo lumin	[PMID: 36924668]
A549	GI₅₀	4.94 nM Compound: 5; PD-325901	Antiproliferative activity against human A549 cells harboring KRAS G13S mutant assessed as cell growth inhibition incubated for 72 hrs in the absence of UV irradiation by CellTiter-Glo luminescent assay Antiproliferative activity against human A549 cells harboring KRAS G13S mutant assessed as cell growth inhibition incubated for 72 hrs in the absence of UV irradiation by CellTiter-Glo luminescent assay	[PMID: 36924668]
COLO 205	IC₅₀	5 nM Compound: PD325901	Antiproliferative activity against human COLO205 cells harboring BRAF mutation Antiproliferative activity against human COLO205 cells harboring BRAF mutation	[PMID: 26611920]
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	194 nM Compound: PD325901	Antiproliferative activity against human HCT116 cells expressing KRAS G13D mutant Antiproliferative activity against human HCT116 cells expressing KRAS G13D mutant	[PMID: 23474388]
HCT-116	IC₅₀	185 nM Compound: PD325901	Antiproliferative activity against human HCT116 cells harboring K-Ras G13D mutation Antiproliferative activity against human HCT116 cells harboring K-Ras G13D mutation	[PMID: 26611920]
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]
HCT-116	GI₅₀	44.7 nM Compound: 5; PD-325901	Antiproliferative activity against human HCT-116 cells harboring KRAS G13D mutant assessed as cell growth inhibition incubated for 72 hrs in the absence of UV irradiation by CellTiter-Glo luminescent assay Antiproliferative activity against human HCT-116 cells harboring KRAS G13D mutant assessed as cell growth inhibition incubated for 72 hrs in the absence of UV irradiation by CellTiter-Glo luminescent assay	[PMID: 36924668]
HCT-116	GI₅₀	52.5 nM Compound: 5; PD-325901	Antiproliferative activity against human HCT-116 cells harboring KRAS G13D mutant assessed as cell growth inhibition preincubated with compound for 1 hrs followed by UV irradiation for 5 mins and measured 72 hrs post compound treatment by CellTiter-Glo lu Antiproliferative activity against human HCT-116 cells harboring KRAS G13D mutant assessed as cell growth inhibition preincubated with compound for 1 hrs followed by UV irradiation for 5 mins and measured 72 hrs post compound treatment by CellTiter-Glo lu	[PMID: 36924668]
HEK-293T	GI₅₀	>10000 nM Compound: 5; PD-325901	Cytotoxicity against HEK293T cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Glo luminescent assay Cytotoxicity against HEK293T cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 36924668]
HepG2	IC₅₀	5 nM Compound: PD325901	Antiproliferative activity against human HepG2 cells harboring N-Ras mutation Antiproliferative activity against human HepG2 cells harboring N-Ras mutation	[PMID: 26611920]
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]
LoVo	IC₅₀	128 nM Compound: PD325901	Antiproliferative activity against human LoVo cells Antiproliferative activity against human LoVo cells	[PMID: 23474388]
MCF7	IC₅₀	9550 nM Compound: PD325901	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 cells	[PMID: 26611920]
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]
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]
MIA PaCa-2	IC₅₀	17 nM Compound: PD325901	Antiproliferative activity against human MIAPaCa2 cells Antiproliferative activity against human MIAPaCa2 cells	[PMID: 23474388]
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.

Essai clinique

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

Chemical Information

CAS No. 391210-10-9
Appearance Solid
Masse moléculaire 482.19
Formule C₁₆H₁₄F₃IN₂O₄
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
Synonyms

PD0325901; PD325901
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (159)

All 2D/3D Cell Culture and DifferentiationIFWBCell Proliferation/Viability Assay

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Journal Impact Factor

Signal Transduct Target Ther

Tet methylcytosine dioxygenase 2 (TET2) deficiency elicits EGFR-TKI (tyrosine kinase inhibitors) resistance in non-small cell lung cancer. [Abstract]

2024 Mar 9;9(1):65. PMID: 38461173
Nature

Clinical functional proteomics of intercellular signalling in pancreatic cancer. [Abstract]

2025 Jan;637(8046):726-735. PMID: 39537929
Nature

Human blastoids model blastocyst development and implantation. [Abstract]

2022 Jan;601(7894):600-605. PMID: 34856602

Mirdametinib purchased from MedChemExpress. Usage Cited in: Nature. 2022 Jan;601(7894):600-605. [Abstract]

Upon exposure to lysophosphatidic acid (LPA) (a Hippo pathway inhibitor), A83-01 (an inhibitor of TGFβ family receptors) and PD0325901 (an ERK inhibitor) in a chemically defined medium containing the STAT activator leukaemia inhibitory factor (LIF) and Y-27632 (a ROCK inhibitor) (10 µM, 7 days),blastocyst-like structures formed efficiently from naive PSCs.

Mirdametinib purchased from MedChemExpress. Usage Cited in: Nature. 2022 Jan;601(7894):600-605. [Abstract]

Upon exposure to lysophosphatidic acid (LPA) (a Hippo pathway inhibitor), A83-01 (an inhibitor of TGFβ family receptors) and PD0325901 (an ERK inhibitor) in a chemically defined medium containing the STAT activator leukaemia inhibitory factor (LIF) and Y-27632 (a ROCK inhibitor) (10 µM, 7 days), blastocyst-like structures formed efficiently from naive PSCs. trophectoderm (TE) cell analogues (identified as GATA2+GATA3+CDX2+TROP2+) formed, proliferated, and established adherens junctions (marked by CDH1), apical-basal polarity (indicated by aPKC) and tight junctions (marked by ZO-1).
Cell

RNA Pol II inhibition activates cell death independently from the loss of transcription. [Abstract]

2025 Oct 30;188(22):6301-6316.e29. PMID: 40818455
Cell

mTOR activity paces human blastocyst stage developmental progression. [Abstract]

2024 Nov 14;187(23):6566-6583.e22. PMID: 39332412
Nat Methods

Challenging the Astral mass analyzer to quantify up to 5,300 proteins per single cell at unseen accuracy to uncover cellular heterogeneity. [Abstract]

2025 Mar;22(3):510-519. PMID: 39820751
Nat Immunol

Type A cholesterol-dependent cytolysins translocate to the trans-Golgi network for NLRP3 inflammasome activation. [Abstract]

2025 Oct;26(10):1673-1685. PMID: 40913097

Mirdametinib purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2025 Oct;26(10):1673-1685. [Abstract]

Representative immunofluorescence images in HeLa cells stably expressing NLRP3-GFP pre-treated with DMSO (solvent control), 20 μM U0126 or 20 μM Mirdametinib for 30 min before addition of rPFO or not (Mock) for 80 min. The results showed that significantly enhanced rPFO-induced TGN remodeling and NLRP3 recruitment in HeLa NLRP3-GFP. Scale bar, 10 μm.
Nat Biomed Eng

TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]

2018 Aug;2(8):578-588. PMID: 31015631
Cell Stem Cell

An inducible model of human post-implantation development derived from primed and naive stem cells. [Abstract]

2025 Oct 2;32(10):1509-1527.e9. PMID: 40885193
Cell Stem Cell

Modeling early gastrulation in human blastoids with DNA methylation patterns of natural blastocysts. [Abstract]

2025 Mar 6;32(3):409-425.e8. PMID: 39814012
Cell Stem Cell

Epiblast inducers capture mouse trophectoderm stem cells in vitro and pattern blastoids for implantation in utero. [Abstract]

2022 Jul 7;29(7):1102-1118.e8. PMID: 35803228
Nat Protoc

Putting mammalian early embryonic cells into dormancy. [Abstract]

2026 Jan 26. PMID: 41588252
Nat Protoc

Generating human blastoids modeling blastocyst-stage embryos and implantation. [Abstract]

2023 May;18(5):1584-1620. PMID: 36792779
Nat Commun

Klf5-adjacent super-enhancer functions as a 3D genome structure-dependent transcriptional driver to safeguard ESC identity. [Abstract]

2025 Jul 1;16(1):5540. PMID: 40592854
Nat Commun

Semi-automated IT-scATAC-seq profiles cell-specific chromatin accessibility in differentiation and peripheral blood populations. [Abstract]

2025 Mar 17;16(1):2635. PMID: 40097444
Nat Commun

An actin bracket-induced elastoplastic transition determines epithelial folding irreversibility. [Abstract]

2024 Dec 12;15(1):10476. PMID: 39668169
Nat Commun

The scaffolding function of LSD1 controls DNA methylation in mouse ESCs. [Abstract]

2024 Sep 5;15(1):7758. PMID: 39237615
Nat Commun

IL6 supports long-term expansion of hepatocytes in vitro. [Abstract]

2022 Nov 29;13(1):7345. PMID: 36446858

Mirdametinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Nov 29;13(1):7345. [Abstract]

Cell numbers of hepatocytes cultured in IL6-HCM and a number of pathway modulators, including Crytotanshinone and BP-1-102 (JAK/STAT3 inhibitor), MK2206 and GSK2141795 (PI3K/AKT inhibitor), PD0325901 (MARK/ERK1/2 inhibitor), and TGFβ1 for 14 days.The results showed that PD0325901 (PD) could inhibit IL6-induced hepatocyte proliferation.
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
Adv Sci (Weinh)

2026 Apr 22:e22570. PMID: 42018132
Adv Sci (Weinh)

Dynamics of the Mammalian Placental Metabolome in Placentogenesis and Embryonic Development. [Abstract]

2026 Jan 28:e07928. PMID: 41603190
Neuro Oncol

Preclinical assessment of MEK1/2 inhibitors for neurofibromatosis type 2-associated schwannomas reveals differences in efficacy and drug resistance development. [Abstract]

2019 Mar 18;21(4):486-497. PMID: 30615146
Chem Eng J

2026 Mar 19.
Chem Eng J

2024 Sep 1.
Nucleic Acids Res

Enhancer architecture-dependent multilayered transcriptional regulation orchestrates RA signaling-induced early lineage differentiation of ESCs. [Abstract]

2021 Nov 18;49(20):11575-11595. PMID: 34723340
Biomaterials

A fluorescent chemical probe CDy9 selectively stains and enables the isolation of live naïve mouse embryonic stem cells. [Abstract]

2018 Oct;180:12-23. PMID: 30014963
J Exp Clin Cancer Res

Dual CDK and MEK Inhibition potentiates CD8+ T cell-mediated antitumor immunity by inducing pyroptotic cell death in high-mutational head and neck cancer. [Abstract]

2025 Nov 6;44(1):300. PMID: 41194215
J Exp Clin Cancer Res

Supervillin promotes epithelial-mesenchymal transition and metastasis of hepatocellular carcinoma in hypoxia via activation of the RhoA/ROCK-ERK/p38 pathway. [Abstract]

2018 Jun 28;37(1):128. PMID: 29954442

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.
J Exp Clin Cancer Res

FAK-ERK activation in cell/matrix adhesion induced by the loss of apolipoprotein E stimulates the malignant progression of ovarian cancer. [Abstract]

2018 Feb 20;37(1):32. PMID: 29458390
Redox Biol

The protective role of GPX4 in naïve ESCs is highlighted by induced ferroptosis resistance through GPX4 expression. [Abstract]

2025 Apr:81:103539. PMID: 40010136
J Hazard Mater

Triazole fungicides exert neural differentiation alteration through H3K27me3 modifications: In vitro and in silico study. [Abstract]

2023 Oct 5:459:132225. PMID: 37557044
Alzheimers Dement

2026 Apr;22(4):e71378. PMID: 42043780
Clin Cancer Res

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

2020 Apr 15;26(8):2011-2021. PMID: 31937620
Clin Cancer Res

Upregulation of IGF1R by mutant RAS in leukemia and potentiation of RAS signaling inhibitors by small-molecule inhibition of IGF1R. [Abstract]

2014 Nov 1;20(21):5483-95. PMID: 25186968
Nat Struct Mol Biol

Interactions between the genome and the nuclear lamina are multivalent and cooperative. [Abstract]

2025 Sep 1. PMID: 40890525
Cancer Lett

Zoledronic acid enhances the efficacy of the MEK inhibitor trametinib in KRAS mutant cancers. [Abstract]

2019 Feb 1:442:202-212. PMID: 30429107
Environ Int

Bisphenol A impairs developmental potential of mouse blastoids through oxidative stress. [Abstract]

2025 Sep 28:204:109820. PMID: 41033068
Cell Death Dis

Genome-wide screening in the haploid system reveals Slc25a43 as a target gene of oxidative toxicity. [Abstract]

2022 Mar 30;13(3):284. PMID: 35354792
Cell Death Dis

Activation of G protein coupled estrogen receptor prevents chemotherapy-induced intestinal mucositis by inhibiting the DNA damage in crypt cell in an extracellular signal-regulated kinase 1- and 2- dependent manner. [Abstract]

2021 Oct 30;12(11):1034. PMID: 34718327
Sci China Life Sci

Maternal transcription factor OTX2 directly induces SETD1A and promotes embryonic genome activation in human pre-implantation embryos. [Abstract]

2025 Apr 22. PMID: 40285911
Genome Biol

IT-scC&T-seq streamlines scalable, parallel profiling of protein-DNA interactions in single cells. [Abstract]

2025 Jul 7;26(1):196. PMID: 40624534
Proc Natl Acad Sci U S A

SR9009 has REV-ERB-independent effects on cell proliferation and metabolism. [Abstract]

2019 Jun 18;116(25):12147-12152. PMID: 31127047
Dev Cell

Identifying cross-lineage dependencies of cell-type-specific regulators in mouse gastruloids. [Abstract]

2025 Jul 21;60(14):2007-2022.e7. PMID: 40101716
Cell Syst

Receptor-Driven ERK Pulses Reconfigure MAPK Signaling and Enable Persistence of Drug-Adapted BRAF-Mutant Melanoma Cells. [Abstract]

2020 Nov 18;11(5):478-494.e9. PMID: 33113355
Cell Syst

A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]

2018 Apr 25;6(4):424-443.e7. PMID: 29655704
Stem Cell Res Ther

Generation of equine induced pluripotent stem cells from cells of embryonic, perinatal and adult tissues. [Abstract]

2025 Oct 8;16(1):547. PMID: 41063189
Stem Cell Res Ther

Human platelet lysate enhances small lipid droplet accumulation of human MSCs through MAPK phosphorylation. [Abstract]

2024 Dec 18;15(1):473. PMID: 39696689
Aging Cell

2026 Jan 20;25(2):e70352.
Blood Adv

Melanocortin/MC5R axis regulates the proliferation of hematopoietic stem cells in mice after ionizing radiation injury. [Abstract]

2023 Jul 11;7(13):3199-3212. PMID: 36920787
Cell Death Discov

Gadd45g initiates embryonic stem cell differentiation and inhibits breast cell carcinogenesis. [Abstract]

2021 Oct 2;7(1):271. PMID: 34601500
Cell Rep

PRC1 and PRC2 proximal interactome in mouse embryonic stem cells. [Abstract]

2025 Mar 5;44(3):115362. PMID: 40053453
Sci Data

High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]

2024 Sep 19;11(1):1024. PMID: 39300112
Cell Rep

Rif1 and Hmgn3 regulate the conversion of murine trophoblast stem cells. [Abstract]

2022 Mar 29;38(13):110570. PMID: 35354046
Sci Signal

The APC/C adaptor Cdh1 stabilizes STING to potentiate innate immune activation in renal cell carcinoma. [Abstract]

2026 Jun 23;19(943):eaef1474. PMID: 42335217
Lwt-Food Sci Technol

11 Oct 2021.
Sci Signal

TSHZ2 is an EGF-regulated tumor suppressor that binds to the cytokinesis regulator PRC1 and inhibits metastasis. [Abstract]

2021 Jun 22;14(688):eabe6156. PMID: 34158398
Comput Biol Med

Identification of inflammation-related biomarkers and therapeutic targets for neurogenic bladder fibrosis via multi-omics analysis. [Abstract]

2025 Jul 5;196(Pt A):110721. PMID: 40618693
EMBO Rep

ZFP207 sustains pluripotency by coordinating OCT4 stability, alternative splicing and RNA export. [Abstract]

2022 Feb 3;23(3):e53191. PMID: 35037361
JCI Insight

FXR shapes an immunosuppressive microenvironment in PD-L1lo/- non-small cell lung cancer by upregulating HVEM. [Abstract]

2025 Sep 23;10(18):e190716. PMID: 40985894
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
J Invest Dermatol

Botulinum neurotoxin type A1 alleviates bleomycin-induced skin fibrosis by inhibiting phosphatidylinositol 3-kinase-protein kinase B (PI3K-Akt) pathway and associated cell cycle and proliferation. [Abstract]

2026 Jan 23:S0022-202X(26)00030-8. PMID: 41581589
J Invest Dermatol

Combined Cyclin-Dependent Kinase Inhibition Overcomes MAPK/Extracellular Signal-Regulated Kinase Kinase Inhibitor Resistance in Plexiform Neurofibroma of Neurofibromatosis Type I. [Abstract]

2022 Mar;142(3 Pt A):613-623.e7. PMID: 34534577
Cell Prolif

BCL2 is a major regulator of haploidy maintenance in murine embryonic stem cells. [Abstract]

2023 Dec;56(12):e13498. PMID: 37144356
Cell Prolif

Genome-scale screening in a rat haploid system identifies Thop1 as a modulator of pluripotency exit. [Abstract]

2022 Apr;55(4):e13209. PMID: 35274380
Mol Cancer Ther

ASCL1 Restrains ERK1/2 to Promote Survival of a Subset of Neuroendocrine Lung Cancers. [Abstract]

2024 Dec 3;23(12):1789-1800. PMID: 39295275
Stem Cell Reports

An acidic residue within the OCT4 dimerization interface of SOX17 is necessary and sufficient to overcome its pluripotency-inducing activity. [Abstract]

2025 Jan 23:102398. PMID: 39919754
Glia

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

2019 Jul;67(7):1320-1332. PMID: 30815939
Int J Mol Sci

The Rab18/Ras/ERK/FosB/MMP3 Signaling Pathway Mediates Cell Migration Regulation by 2'3'-cGAMP. [Abstract]

2025 Jun 16;26(12):5758. PMID: 40565221
Int J Mol Sci

Inhibition of NAMPT by PAK4 Inhibitors. [Abstract]

2024 Sep 21;25(18):10138. PMID: 39337621
Stem Cells Transl Med

High-throughput screening in postimplantation haploid epiblast stem cells reveals Hs3st3b1 as a modulator for reprogramming. [Abstract]

2021 May;10(5):743-755. PMID: 33511777
Cell Regen

A single-cell hematopoietic microenvironmental atlas reveals progressive maturation of bone marrow vascular niche. [Abstract]

2025 Dec 4;14(1):50. PMID: 41339619
Bioorg Chem

PD0325901, an ERK inhibitor, attenuates RANKL-induced osteoclast formation and mitigates cartilage inflammation by inhibiting the NF-κB and MAPK pathways. [Abstract]

2023 Mar:132:106321. PMID: 36642020
Eur J Pharm Sci

Velvet antler polypeptide-loaded polyvinyl alcohol-sodium alginate hydrogels promote the differentiation of neural progenitor cells in 3D towards oligodendrocytes in vitro. [Abstract]

2021 Dec 1:167:106003. PMID: 34517106
Int Immunopharmacol

Z-guggulsterone induces PD-L1 upregulation partly mediated by FXR, Akt and Erk1/2 signaling pathways in non-small cell lung cancer. [Abstract]

2021 Apr:93:107395. PMID: 33529916
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
Lung Cancer

KRASG12D/G13D-USP15 axis promotes TGF-β/SMAD signaling and glycolytic flux to accelerate NSCLC pathogenesis. [Abstract]

2025 Nov 19:211:108848. PMID: 41317688
Cancers (Basel)

Nuclear Membrane Protein SUN5 Is Highly Expressed and Promotes Proliferation and Migration in Colorectal Cancer by Regulating the ERK Pathway. [Abstract]

2022 Oct 31;14(21):5368. PMID: 36358787
Front Cell Dev Biol

Fast Dynamic in vivo Monitoring of Erk Activity at Single Cell Resolution in DREKA Zebrafish. [Abstract]

2018 Sep 25:6:111. PMID: 30320107
iScience

Network characterization linc1393 in the maintenance of pluripotency provides the principles for lncRNA targets prediction. [Abstract]

2023 Jul 26;26(8):107469. PMID: 37588167
Transl Oncol

CKAP4-mediated activation of FOXM1 via phosphorylation pathways regulates malignant behavior of glioblastoma cells. [Abstract]

2023 Mar:29:101628. PMID: 36701930
Sci Rep

Enhancement of melanoma aggressiveness via p38-MAPK, HIF-1α pathways, and metabolic reprogramming induced by Candida albicans. [Abstract]

2025 Nov 17;15(1):40227. PMID: 41249785
J Biol Chem

An alternative model for type I interferon induction downstream of human TLR2. [Abstract]

2020 Oct 16;295(42):14325-14342. PMID: 32796029
J Biol Chem

Kinome-wide selectivity profiling of ATP-competitive mammalian target of rapamycin (mTOR) inhibitors and characterization of their binding kinetics. [Abstract]

2012 Mar 23;287(13):9742-52. PMID: 22223645
Brain Res Bull

FGF9 alters the Wallerian degeneration process by inhibiting Schwann cell transformation and accelerating macrophage infiltration. [Abstract]

2019 Oct:152:285-296. PMID: 31220553
J Cell Sci

Tbl1 promotes Wnt/β-catenin signaling-induced degradation of the Tcf7l1 protein in mouse ESCs. [Abstract]

2024 May 1;137(9):jcs261241. PMID: 38639717
Stem Cells

P21-activated kinase 4 Pak4 maintains embryonic stem cell pluripotency via Akt activation. [Abstract]

2022 Oct 21;40(10):892-905. PMID: 35896382
Exp Cell Res

Loss of splicing factor RBM25 promotes the collapse of murine hematopoiesis. [Abstract]

2026 Mar 10;458(1):114982. PMID: 41819468
Front Med

ASPH interacts with RUVBL2 to promote tumor metastasis in lung adenocarcinoma via MAPK and Notch signaling pathways. [Abstract]

2025 Dec 27. PMID: 41454078
Exp Cell Res

Oxymatrine boosts hematopoietic regeneration by modulating MAPK/ERK phosphorylation after irradiation-induced hematopoietic injury. [Abstract]

2023 Jun 15;427(2):113603. PMID: 37075826
Viruses

Combination Kinase Inhibitor Treatment Suppresses Rift Valley Fever Virus Replication. [Abstract]

2018 Apr 13;10(4). pii: E191. PMID: 29652799

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.

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.
Andrology

Expression of IL-33 in rodent testes and its role in Leydig cell steroidogenesis and aging. [Abstract]

2025 Jun 16. PMID: 40521800
Stem Cells Int

Screening Genes Promoting Exit from Naive Pluripotency Based on Genome-Scale CRISPR-Cas9 Knockout. [Abstract]

2020 Feb 3;2020:8483035. PMID: 32089710
Stem Cells Int

Establishment and Identification of a CiPSC Lineage Reprogrammed from FSP-tdTomato Mouse Embryonic Fibroblasts (MEFs). [Abstract]

2018 Dec 25:2018:5965727. PMID: 30675169
Front Neurosci

Extracellular Adenosine Triphosphate Binding to P2Y1 Receptors Prevents Glutamate-Induced Excitotoxicity: Involvement of Erk1/2 Signaling Pathway to Suppress Autophagy. [Abstract]

2022 Jun 7;16:901688. PMID: 35747207
Biol Reprod

Establishment and comparison of human term placenta-derived trophoblast cells. [Abstract]

2024 May 9;110(5):950-970. PMID: 38330185
Bioorg Med Chem

Daphnanes diterpenes from the latex of Hura crepitans L. and their PKCζ-dependent anti-proliferative activity on colorectal cancer cells. [Abstract]

2023 Jul 15:90:117366. PMID: 37329676
J Anim Sci

Ubiquitination plays an important role during the formation of chicken primordial germ cells. [Abstract]

2024 Jan 3:102:skae251. PMID: 39187982
Genes (Basel)

Influence and Optimization of Diverse Culture Systems on Chicken Embryonic Stem Cell Culture. [Abstract]

2024 Oct 30;15(11):1400. PMID: 39596599
Neuroscience

DCPIB Attenuates Ischemia-Reperfusion Injury by Regulating Microglial M1/M2 Polarization and Oxidative Stress. [Abstract]

2024 May 9:S0306-4522(24)00196-9. PMID: 38734301
Animals (Basel)

The Effect of Inhibiting the Wingless/Integrated (WNT) Signaling Pathway on the Early Embryonic Disc Cell Culture in Chickens. [Abstract]

2024 May 4;14(9):1382. PMID: 38731386
Animals (Basel)

Glycolysis Combined with Core Pluripotency Factors to Promote the Formation of Chicken Induced Pluripotent Stem Cells. [Abstract]

2021 Feb 6;11(2):425. PMID: 33562170
Platelets

EloA promotes HEL polyploidization upon PMA stimulation through enhanced ERK1/2 activity. [Abstract]

2022 Jul 4;33(5):755-763. PMID: 34697988
Fundam Clin Pharmacol

Urolithin C increases glucose-induced ERK activation which contributes to insulin secretion. [Abstract]

2020 Oct;34(5):571-580. PMID: 32083757
Toxicon

Deoxynivalenol-induced anorexia is mediated by brain-gut peptides through CaSR-TRPM5 signaling axis. [Abstract]

2026 Jan:269:108660. PMID: 41241198
Gene

Immune-related glycosylation genes based classification predicts prognosis and therapy options of osteosarcoma. [Abstract]

2025 Jan 15:933:148985. PMID: 39369757
PeerJ

A novel dual MEK/PDK1 inhibitor 9za retards the cell cycle at G0/G1 phase and induces mitochondrial apoptosis in non-small cell lung cancer cells. [Abstract]

2020 Oct 2;8:e9981. PMID: 33072436
Virology

EGR1 upregulation following Venezuelan equine encephalitis virus infection is regulated by ERK and PERK pathways contributing to cell death. [Abstract]

2020 Jan 2;539:121-128. PMID: 31733451
FEBS Open Bio

Establishment and optimization of the two-step induction system for generating primordial germ cell-like cells from chicken embryonic stem cells. [Abstract]

2025 Sep 10. PMID: 40926636
FEBS Open Bio

Activation of ERK-Drp1 signaling promotes hypoxia-induced Aβ accumulation by upregulating mitochondrial fission and BACE1 activity. [Abstract]

2021 Oct;11(10):2740-2755. PMID: 34403210
Biochem Biophys Res Commun

COL8A1 enhances the invasion/metastasis in MDA-MB-231 cells via the induction of IL1B and MMP1 expression. [Abstract]

2023 Jan 29:642:145-153. PMID: 36577251
Biochem Biophys Res Commun

SEPHS1 is dispensable for pluripotency maintenance but indispensable for cardiac differentiation in mouse embryonic stem cells. [Abstract]

2022 Jan 29:590:125-131. PMID: 34974300
Biochem Biophys Res Commun

β-catenin stimulates Tcf7l1 degradation through recruitment of casein kinase 2 in mouse embryonic stem cells. [Abstract]

2020 Apr 2;524(2):280-287. PMID: 31987502

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.
Epilepsy Res

Inhibition of MEK-ERK signaling reduces seizures in two mouse models of tuberous sclerosis complex. [Abstract]

2022 Mar:181:106890. PMID: 35219048
STAR Protoc

Protocol for capturing trophectoderm stem cells reflecting the blastocyst stage. [Abstract]

2023 Mar 16;4(2):102151. PMID: 36930647
STAR Protoc

Protocol to generate induced trophoblast stem cells from embryonic stem cells in mice. [Abstract]

2023 Feb 3;4(1):102092. PMID: 36853659
STAR Protoc

Rapid generation of murine haploid-induced trophoblast stem cells via a Tet-on system. [Abstract]

2021 Nov 5;2(4):100881. PMID: 34806042
bioRxiv

Large RNA polymerase II condensates are promoter-centric assemblies associated with early stages of transcription at all expressed genes. [Abstract]

2026 May 25:2026.05.25.727590. PMID: 42244752
bioRxiv

2026 May 4.
bioRxiv

2026 Mar 13.
bioRxiv

2026 Mar 17.
bioRxiv

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medRxiv

2026 Mar 7.
Res Sq

2026 Mar 4.
bioRxiv

2026 Jan 17.
bioRxiv

2026 Jan 9.
Res Sq

Age-Driven Lipid Remodeling Activates Lysosome-Mediated Plasma Membrane Repair. [Abstract]

2026 Jan 20:rs.3.rs-8607320. PMID: 41646411
bioRxiv

2025 Dec 24.
bioRxiv

Hidden-driver inference reveals synergistic brain-penetrant therapies for medulloblastoma. [Abstract]

2025 Nov 20:2025.11.20.689490. PMID: 41332625
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2025 Oct 14:2025.10.12.681919. PMID: 41279276
bioRxiv

Noncanonical amino acid incorporation enables minimally disruptive labeling of stress granule and TDP-43 proteinopathy. [Abstract]

2025 Oct 17:2025.10.17.683020. PMID: 41279779
bioRxiv

2025 Sep 5.
SSRN

2025 May 27.
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Shigella OspF blocks rapid p38-dependent priming of the NAIP-NLRC4 inflammasome. [Abstract]

2025 Feb 2:2025.02.01.636075. PMID: 39975412
Patent

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Pol II degradation activates cell death independently from the loss of transcription. [Abstract]

2024 Dec 10:2024.12.09.627542. PMID: 39713309
bioRxiv

A direct interaction between the Chd1 CHCT domain and Rtf1 controls Chd1 distribution and nucleosome positioning on active genes. [Abstract]

2024 Dec 6:2024.12.06.627179. PMID: 39677735
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2024 Aug 31:2024.08.29.610385. PMID: 39257748
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2023 Jun 22.
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2023 May 5.
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October 21st, 2022.
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2022 Feb.
Oncotarget

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

2020 Nov 3;11(44):3921-3932. PMID: 33216841
bioRxiv

2019 Sep.
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Chem Biol

Discovery of potent and selective covalent inhibitors of JNK. [Abstract]

2012 Jan 27;19(1):140-54. PMID: 22284361

Solvant et solubilité

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.

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

2.0739 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

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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 2.08 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.

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.

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:

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

Protocole

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.

MedChemExpress (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.

MedChemExpress (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.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (281 KB)
SDS (788 KB)
- English - EN (788 KB)
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- Italian - IT (788 KB)
- Korean - KR (788 KB)
- Portuguese - PT (788 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)
Instruction de manipulation (2659 KB)

Références

[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]

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

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

Keywords

Mirdametinib

159 Cited Publications

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Mirdametinib

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Publications Citing Use of MedChemExpress (MCE) Mirdametinib

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Chemical Information

Publications (159)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Mirdametinib Related Classifications

HY-10254 Related Classifications