1. MAPK/ERK Pathway
  2. MEK
  3. Mirdametinib

Mirdametinib (PD0325901) (GMP) is Mirdametinib (HY-10254) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Mirdametinib is an orally active, selective and non-ATP-competitive MEK inhibitor.

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Mirdametinib

Mirdametinib Chemical Structure

CAS No. : 391210-10-9

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Description

Mirdametinib (PD0325901) (GMP) is Mirdametinib (HY-10254) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Mirdametinib is an orally active, selective and non-ATP-competitive MEK inhibitor[1][2][3].

Cellular Effect
Cell Line Type Value Description References
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 luminescent assay
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 luminescent assay
[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 luminescent assay
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 luminescent assay
[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 luminescent assay
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 luminescent assay
[PMID: 36924668]
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
0.038 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]
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]
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 luminescent assay
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 luminescent assay
[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]
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 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]
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]
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]
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 luminescent assay
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 luminescent assay
[PMID: 36924668]
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 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
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]
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]
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]
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]
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]
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]
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]
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 (250 nM; 7 d) induces differentiation of cardiac PCs into vascular smooth muscle cell (VSMC)-like cells[1].
Mirdametinib (10 μM; 4 d) induces oligodendrocyte precursor cells (OPC) to oligodendrocytes (OL) differentiation[2].
Mirdametinib enhances embryonic stem cells (ESC) self-renewal capacity both by key regulatory genes and ES cell-specific miRNA, which in turn influences ESC self-renewal and cellular differentiation[3].

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

Molecular Weight

482.19

Formula

C16H14F3IN2O4

CAS No.
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

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Product Name:
Mirdametinib
Cat. No.:
HY-10254G
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