1598383-40-4 Usage
Description
EPZ011969, also known as N-[(1,2-Dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-[ethyl[trans-4-[(2-methoxyethyl)methylamino]cyclohexyl]amino]-2-methyl-5-[3-(4-morpholinyl)-1-propyn-1-yl]-benzamide, is a potent inhibitor of EZH2 histone methyltransferase. It is an orally bioavailable compound that selectively targets EZH2, a key enzyme involved in the proliferation and aggressive growth of neoplastic cells. EPZ011969 has demonstrated significant tumor growth inhibition in preclinical studies, making it a promising candidate for cancer treatment.
Uses
Used in Cancer Treatment:
EPZ011969 is used as an inhibitor of EZH2 histone methyltransferase for the treatment of cancer. It selectively targets the enzyme EZH2, which is overexpressed in various types of cancer and plays a crucial role in the proliferation and aggressive growth of neoplastic cells. By inhibiting EZH2, EPZ011969 can potentially suppress tumor growth and improve patient outcomes.
Used in Biological Studies:
In addition to its therapeutic applications, EPZ011969 is also used in biological studies as a research tool to investigate the role of EZH2 in cancer development and progression. Its high selectivity for EZH2 over other lysine methyltransferases makes it an invaluable compound for understanding the molecular mechanisms underlying cancer and identifying potential therapeutic targets.
Used in Drug Development:
EPZ011969 serves as a lead compound in the development of novel EZH2 inhibitors for cancer treatment. Its potent activity and selectivity for EZH2 make it an attractive starting point for the design and optimization of new drugs targeting this enzyme. Researchers can use EPZ011969 to guide the synthesis of more effective and selective EZH2 inhibitors, potentially leading to the development of improved cancer therapies.
Used in Drug Delivery Systems:
To enhance the efficacy and bioavailability of EPZ011969, researchers are exploring various drug delivery systems, such as nanoparticles and liposomes, to improve its delivery to cancer cells. These systems can help overcome limitations associated with the compound's solubility, stability, and pharmacokinetic properties, ultimately leading to more effective cancer treatments.
Check Digit Verification of cas no
The CAS Registry Mumber 1598383-40-4 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,5,9,8,3,8 and 3 respectively; the second part has 2 digits, 4 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 1598383-40:
(9*1)+(8*5)+(7*9)+(6*8)+(5*3)+(4*8)+(3*3)+(2*4)+(1*0)=224
224 % 10 = 4
So 1598383-40-4 is a valid CAS Registry Number.
1598383-40-4Relevant articles and documents
EPZ011989, A potent, orally-available EZH2 inhibitor with robust in vivo activity
Campbell, John E.,Kuntz, Kevin W.,Knutson, Sarah K.,Warholic, Natalie M.,Keilhack, Heike,Wigle, Tim J.,Raimondi, Alejandra,Klaus, Christine R.,Rioux, Nathalie,Yokoi, Akira,Kawano, Satoshi,Minoshima, Yukinori,Choi, Hyeong-Wook,Porter Scott, Margaret,Waters, Nigel J.,Smith, Jesse J.,Chesworth, Richard,Moyer, Mikel P.,Copeland, Robert A.
, p. 491 - 495 (2015/05/27)
Inhibitors of the protein methyltransferase Enhancer of Zeste Homolog 2 (EZH2) may have significant therapeutic potential for the treatment of B cell lymphomas and other cancer indications. The ability of the scientific community to explore fully the spectrum of EZH2-associated pathobiology has been hampered by the lack of in vivo-active tool compounds for this enzyme. Here we report the discovery and characterization of EPZ011989, a potent, selective, orally bioavailable inhibitor of EZH2 with useful pharmacokinetic properties. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma. Hence, this compound represents a powerful tool for the expanded exploration of EZH2 activity in biology.
