Quality Level
SMILES string
FC1=C2C(NC(C(N[C@H]3C[C@@H](N4C[C@H](CC4)N(C)S(C)(=O)=O)CCC3)=O)=C2)=C(C=C1)C.[0.75H2O]
assay
≥94% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Biochem/physiol Actions
Potent and selective SETD2 inhibitor with anti-cancer efficacy.
EPZ-719 is a potent and selective SETD2 inhibitor (Ki/IC50 = 3.3/8 nM), being > 8000-fold more selective towards SETD2 over 14 other histone methyltransferases, including the mono/di-H3K36 methylases SMYD2 and WHSC1/MMSET/NSD2. EPZ-719 downregulates cellular H3K36 trimethylation level (IC50 = 23 nM, A549 cells) and shows potent anti-proliferative activity against multiple myeloma cell lines (IC50 in 14 days = 25 nM/KMS34, 11 nM/KMS211) and good pharmacokinetic properties in mice.
EPZ-719 is a potent and selective SETD2 inhibitor (Ki/IC50 = 3.3/8 nM), being > 8000-fold more selective towards SETD2 over 14 other histone methyltransferases, including the mono/di-H3K36 methylases SMYD2 and WHSC1/MMSET/NSD2. EPZ-719 downregulates cellular H3K36 trimethylation level (IC50 = 23 nM, A549 cells) and shows potent anti-proliferative activity against multiple myeloma cell lines (IC50 in 14 days = 25 nM/KMS34, 11 nM/KMS211) and good pharmacokinetic properties in mice.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
John W Lampe et al.
ACS medicinal chemistry letters, 12(10), 1539-1545 (2021-10-22)
SET domain-containing protein 2 (SETD2), a histone methyltransferase, has been identified as a target of interest in certain hematological malignancies, including multiple myeloma. This account details the discovery of EPZ-719, a novel and potent SETD2 inhibitor with a high selectivity
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