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Chemical Structure| 1380288-87-8 Chemical Structure| 1380288-87-8

Structure of Pinometostat
CAS No.: 1380288-87-8

Chemical Structure| 1380288-87-8

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Pinometostat (EPZ-5676) is an extremely potent inhibitor of DOT1L histone methyltransferase, exhibiting a Ki of 80 pM.

Synonyms: EPZ-5676

4.5 *For Research Use Only !

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Product Citations

Product Citations

Liu, Zhiwei ; Liu, Yingluo ; Qian, Lili ; Jiang, Shangwen ; Gai, Xiameng ; Ye, Shu , et al.

Abstract: KRAS mutant cancer, characterized by the activation of a plethora of phosphorylation signaling pathways, remains a major challenge for cancer therapy. Despite recent advancements, a comprehensive profile of the proteome and phosphoproteome is lacking. This study provides a proteomic and phosphoproteomic landscape of 43 KRAS mutant cancer cell lines across different tissue origins. By integrating transcriptomics, proteomics, and phosphoproteomics, we identify three subsets with distinct biological, clinical, and therapeutic characteristics. The integrative analysis of phosphoproteome and drug sensitivity information facilitates the identification of a set of drug combinations with therapeutic potentials. Among them, we demonstrate that the combination of DOT1L and SHP2 inhibitors is an effective treatment specific for subset 2 of KRAS mutant cancers, corresponding to a set of TCGA clinical tumors with the poorest prognosis. Together, this study provides a resource to better understand KRAS mutant cancer heterogeneity and identify new therapeutic possibilities.

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Product Details of Pinometostat

CAS No. :1380288-87-8
Formula : C30H42N8O3
M.W : 562.71
SMILES Code : NC1=NC=NC2=C1N=CN2[C@H]3[C@H](O)[C@H](O)[C@@H](CN([C@@H]4C[C@H](CCC5=NC6=C(C=CC(C(C)(C)C)=C6)N5)C4)C(C)C)O3
Synonyms :
EPZ-5676
MDL No. :MFCD24849416
InChI Key :LXFOLMYKSYSZQS-XKHGBIBOSA-N
Pubchem ID :57345410

Safety of Pinometostat

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Pinometostat

epigenetics

Isoform Comparison

Biological Activity

Target
  • Histone Methyltransferase

    DOT1L, Ki:80 pM

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01684150 Acute Myeloid Leukemia|Acute L... More >>ymphoblastic Leukemia|Myelodysplastic Syndrome|Myeloproliferative Disorders Less << PHASE1 COMPLETED 2025-02-16 Mayo Clinic Scottsdale-Phoenix... More >>, Scottsdale, Arizona, 85259, United States|Northwestern University, Chicago, Illinois, 60611, United States|Memorial Sloan Kettering Cancer Center, New York, New York, 10065, United States|Duke University Health System, Durham, North Carolina, 27710, United States|Sarah Cannon Research Institute, Nashville, Tennessee, 37203, United States|UT MD Anderson Cancer, Houston, Texas, 77030, United States|Universit?tsklinikum Ulm, Ulm, 89081, Germany|Erasmus University Medical Center, Rotterdam, Netherlands Less <<
NCT02141828 Leukemia|Acute Myeloid Leukemi... More >>a|Acute Lymphocytic Leukemia|Acute Leukemias Less << PHASE1 COMPLETED 2025-06-16 Childrens Hospital Los Angeles... More >>, Los Angeles, California, 90027, United States|University of California San Francisco Medical Center-Parnassus, San Francisco, California, 94143, United States|Children's Hospital Colorado, Aurora, Colorado, 80045, United States|Emory Children's Healthcare of Atlanta, Atlanta, Georgia, 30322, United States|Johns Hopkins University, Baltimore, Maryland, 21287, United States|Dana Farber Cancer Institute, Boston, Massachusetts, 02215, United States|Memorial Sloan Kettering Cancer Center, New York, New York, 10065, United States|Cincinnati Children's Hospital Medical Center, Cincinnati, Ohio, 45229, United States|The Hospital for Sick Kids, Toronto, Ontario, Canada Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.78mL

0.36mL

0.18mL

8.89mL

1.78mL

0.89mL

17.77mL

3.55mL

1.78mL

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

References

 

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