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Chemical Structure| 391210-10-9 Chemical Structure| 391210-10-9

Structure of Mirdametinib
CAS No.: 391210-10-9

Chemical Structure| 391210-10-9

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PD0325901 is selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM.

Synonyms: PD0325901; PD325901

4.5 *For Research Use Only !

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Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

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Product Details of Mirdametinib

CAS No. :391210-10-9
Formula : C16H14F3IN2O4
M.W : 482.19
SMILES Code : O=C(C1=CC=C(C(F)=C1NC2=CC=C(I)C=C2F)F)NOC[C@H](O)CO
Synonyms :
PD0325901; PD325901
MDL No. :MFCD08435926
InChI Key :SUDAHWBOROXANE-SECBINFHSA-N
Pubchem ID :9826528

Safety of Mirdametinib

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301-H373-H410
Precautionary Statements:P273-P301+P310
Class:6.1
UN#:2811
Packing Group:

Related Pathways of Mirdametinib

MAPK

Isoform Comparison

Biological Activity

Target
  • MEK

    MEK, IC50:0.33 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
WU-225 10 µM 2 h Evaluate the inhibitory effect of Mirdametinib on WU-225 microtissues, results showed that Mirdametinib significantly inhibited the growth of WU-225 microtissues. PMC10628938
JH-2-079-c 10 µM 2 h Evaluate the inhibitory effect of Mirdametinib on JH-2-079-c microtissues, results showed that Mirdametinib significantly inhibited the growth of JH-2-079-c microtissues. PMC10628938
JH-2-002 10 µM 2 h Evaluate the inhibitory effect of Mirdametinib on JH-2-002 microtissues, results showed that Mirdametinib significantly inhibited the growth of JH-2-002 microtissues. PMC10628938
MN-2 10 µM 2 h Evaluate the inhibitory effect of Mirdametinib on MN-2 microtissues, results showed that Mirdametinib significantly inhibited the growth of MN-2 microtissues. PMC10628938
K562-R cells 0.5 μM 3 h Mirdametinib significantly increased ATO-induced cell death in TKI-resistant primary blasts derived from patients with CML or ALL. PMC10400427
Ba/F3p210T315I cells 0.5 μM 3 h The combination of Mirdametinib and ATO synergistically induced apoptosis in all tested cell lines, regardless of their sensitivity to TKIs. PMC10400427
JHH-136 10 nM 72 h To evaluate the effect of Mirdametinib combined with radiation, results showed that combined therapy significantly inhibited cell growth and sphere formation in NF1-deficient neurospheres. PMC11374499
HSR-GBM1 10 nM 72 h To evaluate the effect of Mirdametinib combined with radiation, results showed that combined therapy significantly inhibited cell growth and sphere formation in NF1-deficient neurospheres. PMC11374499
Calu-6 3 µM BGB-283 significantly enhanced the antiproliferative activity of PD-0325901, with a 59-fold decrease in EC50. PMC7400788

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice NRG mice Oral 1.5 mg/kg Daily for 5-6 weeks Evaluate the inhibitory effect of Mirdametinib on MPNST tumor growth in NRG mice, results showed that Mirdametinib significantly inhibited tumor growth. PMC10628938
Mice BCR::ABL1-T315I-induced leukemia model Oral 10 mg/kg Continued for 3 weeks The combination of Mirdametinib and ATO significantly prolonged the survival of mice bearing BCR::ABL1-T315I-induced leukemia and reduced tumor cell infiltration. PMC10400427
Mice BTBR mice Intraperitoneal injection 1 mg/kg, 10 mg/kg, 25 mg/kg Once daily for 11 days To evaluate the effects of Mirdametinib on core symptoms of autism. Results showed that Mirdametinib dose-dependently reduced social deficits, vocalization abnormalities, and repetitive behaviors in BTBR mice, and reversed abnormal EEG signals. PMC10149189
NSG mice Heterotopic xenograft models Oral gavage 1.5 mg/kg Twice daily for 4 weeks To evaluate the effect of Mirdametinib combined with radiation, results showed that combined therapy significantly inhibited tumor growth in NF1-deficient heterotopic xenograft models. PMC11374499
Mice Calu-6 NSCLC xenograft model Oral 25 mg/kg Twice daily for 28 days The combination of BGB-283 and selumetinib showed enhanced antitumor efficacy in suppressing tumor growth and resulted in partial and complete tumor regression. PMC7400788

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03170206 Lung Cancer Phase 1 Phase 2 Recruiting March 31, 2024 United States, Massachusetts ... More >> Dana Farber Cancer Institute Recruiting Boston, Massachusetts, United States, 02215 Contact: Geoffrey Shapiro, MD, PhD    617-632-4942       Principal Investigator: Geoffrey Shapiro, MD          Massachusetts General Hospital Not yet recruiting Boston, Massachusetts, United States, 02215 Contact: Rebecca Heist, MD    617-726-1838       Principal Investigator: Rebecca Heist, MD Less <<
NCT02510001 Solid Tumor C... More >>olorectal Cancer Less << Phase 1 Active, not recruiting September 2019 United Kingdom ... More >> Oxford University Hospital NHS Trust Oxford, United Kingdom, OX3 7LE Less <<
NCT01347866 - Terminated(Refer to Detailed D... More >>escription for documentaion of Termination Statement.) Less << - -
NCT01347866 Advanced Cancer Phase 1 Terminated(Refer to Detailed D... More >>escription for documentaion of Termination Statement.) Less << - United States, California ... More >> Ronald Reagan UCLA Medical Center Los Angeles, California, United States, 90095-6984 Ronald Reagan UCLA Medical Center Los Angeles, California, United States, 90095 UCLA Medical Center Los Angeles, California, United States, 90095 UCLA Oncology Center Los Angeles, California, United States, 90095 Santa Monica - UCLA Medical Center and Orthopaedic Hospital Santa Monica, California, United States, 90404 UCLA Santa Monica Hematology Oncology Santa Monica, California, United States, 90404 United States, Colorado Anschutz Cancer Pavilion Aurora, Colorado, United States, 80045 University of Colorado Denver (CTRC) Aurora, Colorado, United States, 80045 University of Colorado Hospital Anschutz Inpatient Pavilion Aurora, Colorado, United States, 80045 University of Colorado Hospital Aurora, Colorado, United States, 80045 United States, South Carolina Medical University of South Carolina, Hollings Cancer Center Charleston, South Carolina, United States, 29425 Medical University of South Carolina Charleston, South Carolina, United States, 29425 MUSC, Investigational Drug Services Charleston, South Carolina, United States, 29425 MUSC Health East Cooper Mount Pleasant, South Carolina, United States, 29464 MUSC Specialty Care-North North Charleston, South Carolina, United States, 29406 Canada, Ontario Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Italy Ospedale San Raffaele Milano, Italy, 20132 Spain Hospital General Vall d'Hebron Barcelona, Spain, 08035 Less <<
NCT00147550 Melanoma Colo... More >>nic Neoplasms Breast Neoplasms Less << Phase 1 Phase 2 Terminated(See termination rea... More >>son in detailed description.) Less << - United States, Alabama ... More >> Pfizer Investigational Site Birmingham, Alabama, United States, 35233-2115 Pfizer Investigational Site Birmingham, Alabama, United States, 35233 Pfizer Investigational Site Birmingham, Alabama, United States, 35294 United States, California Pfizer Investigational Site La Jolla, California, United States, 92037 Pfizer Investigational Site La Jolla, California, United States, 92093 Pfizer Investigational Site La Mesa, California, United States, 91942 Pfizer Investigational Site Los Angeles, California, United States, 90025 Pfizer Investigational Site San Diego, California, United States, 92103 Pfizer Investigational Site San Diego, California, United States, 92123 Pfizer Investigational Site Santa Monica, California, United States, 90404 United States, Florida Pfizer Investigational Site Tampa, Florida, United States, 33612 United States, Michigan Pfizer Investigational Site Detroit, Michigan, United States, 48201 Pfizer Investigational Site Detroit, Michigan, United States, 48202 United States, Minnesota Pfizer Investigational Site Rochester, Minnesota, United States, 55905 United States, New York Pfizer Investigational Site New York, New York, United States, 10021 Pfizer Investigational Site New York, New York, United States, 10022 United States, Ohio Pfizer Investigational Site Cleveland, Ohio, United States, 44106 Less <<
NCT00174369 Carcinoma, Non-Small-Cell Lung Phase 2 Terminated(Terminated [See Det... More >>ailed Description for Termination Reason.]) Less << - United States, California ... More >> Pfizer Investigational Site Greenbrae, California, United States, 94904 Pfizer Investigational Site La Jolla, California, United States, 92093 Pfizer Investigational Site LaJolla, California, United States, 92037 Pfizer Investigational Site San Diego, California, United States, 92103 Pfizer Investigational Site San Mateo, California, United States, 94402 United States, Florida Pfizer Investigational Site Tampa, Florida, United States, 33612 United States, Michigan Pfizer Investigational Site Ann Arbor, Michigan, United States, 48106-0995 Pfizer Investigational Site Detroit, Michigan, United States, 48201 Pfizer Investigational Site Farmington Hills, Michigan, United States, 48334 United States, Minnesota Pfizer Investigational Site Coon Rapids, Minnesota, United States, 55433 Pfizer Investigational Site Fridley, Minnesota, United States, 55432 Pfizer Investigational Site Robbinsdale, Minnesota, United States, 55422 United States, New York Pfizer Investigational Site New York, New York, United States, 11725 United States, Pennsylvania Pfizer Investigational Site Philadelphia, Pennsylvania, United States, 19111 Less <<
NCT02297802 - - - United States, California ... More >> Sharp Healthcare San Diego, California, United States, 92123 Less <<
NCT02039336 Colorectal Cancer Phase 1 Phase 2 Recruiting December 2019 Netherlands ... More >> The Netherlands Cancer Institute Recruiting Amsterdam, Netherlands, 1066CX Contact: F opdam, MD, PhD    +31 20 512 2446    f.opdam@nki.nl    Erasmus Medical Center Cancer Institute Recruiting Rotterdam, Netherlands, 3015CE University Medical Center Utrecht Recruiting Utrecht, Netherlands, 3584CX Less <<
NCT02096471 Neurofibromatosis Type 1 and G... More >>rowing or Symptomatic, Inoperable PN Less << Phase 2 Active, not recruiting December 2018 United States, California ... More >> Children's Hospital Los Angeles Los Angeles, California, United States, 90027 United States, District of Columbia Children's National Medical Center Washington, District of Columbia, United States, 20010 United States, Illinois University of Chicago Chicago, Illinois, United States, 60637 United States, Indiana Indiana Unversity Indianapolis, Indiana, United States, 46202 United States, Maryland National Cancer Institute (NCI) Bethesda, Maryland, United States, 20892 United States, Massachusetts Children's Hospital Boston Boston, Massachusetts, United States, 02115 United States, Missouri Washington University - St. Louis Saint Louis, Missouri, United States, 63110 United States, New York New York University Medical Center New York, New York, United States, 10016 United States, Ohio Cincinnati Children's Hospital Medical Center Cincinnati, Ohio, United States, 45229 United States, Pennsylvania Children's Hospital of Philadelphia Philadelphia, Pennsylvania, United States, 19096 United States, Utah University of Utah Salt Lake City, Utah, United States, 84132 Less <<
NCT02022982 KRAS Mutant Non-Small Cell Lun... More >>g Cancer Solid Tumors Less << Phase 1 Phase 2 Active, not recruiting December 2020 United States, Massachusetts ... More >> Dana Farber Cancer Institute Boston, Massachusetts, United States, 02115 Less <<
NCT06153173 Langerhans Cell Histiocytosis ... More >>(LCH)|Juvenile Xanthogranuloma (JXG)|Rosai-Dorfman Disease (RDD)|Histiocytic Disorders Less << PHASE2 RECRUITING 2025-03-31 Cincinnati Children's Hospital... More >> Medical Center, Cincinnati, Ohio, 45229, United States Less <<
NCT06159166 NF1|Cutaneous Neurofibroma|Mon... More >>otherapy Less << PHASE1|PHASE2 RECRUITING 2028-11-15 Johns Hopkins Hospital, Baltim... More >>ore, Maryland, 21287, United States Less <<
NCT06666348 Pediatric Low-grade Glioma PHASE1|PHASE2 NOT_YET_RECRUITING 1935-01-01 -
NCT04923126 Low-Grade Glioma|Recurrent Low... More >>-Grade Glioma|Progressive Low-Grade Glioma Less << PHASE1|PHASE2 RECRUITING 1931-06-01 St. Jude Children's Research H... More >>ospital, Memphis, Tennessee, 38105, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.07mL

0.41mL

0.21mL

10.37mL

2.07mL

1.04mL

20.74mL

4.15mL

2.07mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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