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Pinometostat (EPZ5676) - ≥98%, high purity , CAS No.1380288-87-8, Inhibitor of DOT1 like histone lysine methyltransferase

  • Moligand™
  • ≥98%
Item Number
E125307
Grouped product items
SKUSizeAvailabilityPrice Qty
E125307-1mg
1mg
In stock
$16.90
E125307-5mg
5mg
In stock
$68.90
E125307-10mg
10mg
In stock
$98.90
E125307-25mg
25mg
In stock
$206.90
E125307-50mg
50mg
In stock
$355.90
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DOT1 like histone lysine methyltransferase Inhibitor

Basic Description

Synonymspinometostat|1380288-87-8|EPZ-5676|EPZ5676|Pinometostat, trans-|Pinometostat [INN]|Pinometostat anhydrous|Pinometostat(EPZ5676)|(2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)
Specifications & Purity≥98%
Storage TempStore at -20°C
Shipped InDry ice
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of DOT1 like histone lysine methyltransferase
Product Description

Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki of 80 pM in a cell-free assay, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor.

Associated Targets

DOT1L Tchem Histone-lysine N-methyltransferase, H3 lysine-79 specific 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

Pubchem Sid488201822
Pubchem Sid Urlhttps://pubchem.ncbi.nlm.nih.gov/substance/488201822
IUPAC Name (2R,3R,4S,5R)-2-(6-aminopurin-9-yl)-5-[[[3-[2-(6-tert-butyl-1H-benzimidazol-2-yl)ethyl]cyclobutyl]-propan-2-ylamino]methyl]oxolane-3,4-diol
INCHI InChI=1S/C30H42N8O3/c1-16(2)37(13-22-25(39)26(40)29(41-22)38-15-34-24-27(31)32-14-33-28(24)38)19-10-17(11-19)6-9-23-35-20-8-7-18(30(3,4)5)12-21(20)36-23/h7-8,12,14-17,19,22,25-26,29,39-40H,6,9-11,13H2,1-5H3,(H,35,36)(H2,31,32,33)/t17?,19?,22-,25-,26-,29-/m1/s1
InChi Key LXFOLMYKSYSZQS-XKHGBIBOSA-N
Canonical SMILES CC(C)N(CC1C(C(C(O1)N2C=NC3=C(N=CN=C32)N)O)O)C4CC(C4)CCC5=NC6=C(N5)C=C(C=C6)C(C)(C)C
Isomeric SMILES CC(C)N(C[C@@H]1[C@H]([C@H]([C@@H](O1)N2C=NC3=C(N=CN=C32)N)O)O)C4CC(C4)CCC5=NC6=C(N5)C=C(C=C6)C(C)(C)C
PubChem CID 57345410
Molecular Weight 562.71

Certificates

Certificate of Analysis(COA)

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10 results found

Lot NumberCertificate TypeDateItem
C23311055Certificate of AnalysisJan 16, 2023 E125307
C2331470Certificate of AnalysisJan 16, 2023 E125307
C2331521Certificate of AnalysisJan 16, 2023 E125307
C2331523Certificate of AnalysisJan 16, 2023 E125307
C2331548Certificate of AnalysisJan 16, 2023 E125307
C2331549Certificate of AnalysisJan 16, 2023 E125307
C2331550Certificate of AnalysisJan 16, 2023 E125307
C2331551Certificate of AnalysisJan 16, 2023 E125307
C2331552Certificate of AnalysisJan 16, 2023 E125307
C2331553Certificate of AnalysisJan 16, 2023 E125307

Chemical and Physical Properties

Solubility≥28.15 mg/mL in DMSO; insoluble in H2O; ≥50.3 mg/mL in EtOH with ultrasonic

Related Documents

 SDS

 Specification Sheet

References

1. Daigle SR, Olhava EJ, Therkelsen CA, Basavapathruni A, Jin L, Boriack-Sjodin PA, Allain CJ, Klaus CR, Raimondi A, Scott MP et al..  (2013)  Potent inhibition of DOT1L as treatment of MLL-fusion leukemia..  Blood,  122  (6): (1017-25).  [PMID:23801631]
2. Bernt KM, Zhu N, Sinha AU, Vempati S, Faber J, Krivtsov AV, Feng Z, Punt N, Daigle A, Bullinger L et al..  (2011)  MLL-rearranged leukemia is dependent on aberrant H3K79 methylation by DOT1L..  Cancer Cell,  20  (1): (66-78).  [PMID:21741597]
3. Muntean AG, Hess JL.  (2012)  The pathogenesis of mixed-lineage leukemia..  Annu Rev Pathol,  7  (3): (283-301).  [PMID:22017583]

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