23168-76-5 Usage
Potency
Highly potent The compound is very effective in inhibiting the enzyme TAK1.
Selectivity
Selective inhibitor of TAK1 The compound specifically targets and inhibits the enzyme TAK1, without affecting other enzymes.
Enzyme target
TAK1 The compound's primary target is the enzyme TAK1, which is involved in the regulation of cell death, inflammation, and immune response.
Therapeutic applications
Treatment of inflammatory and autoimmune diseases, certain types of cancer Due to its inhibitory activity on TAK1, the compound has potential applications in treating various diseases related to the enzyme's function.
Chemical structure
Unique chemical structure The specific arrangement of atoms and functional groups in the compound contributes to its potency and selectivity.
Pharmacological properties
Promising candidate for targeted therapy The compound's properties make it a potential candidate for further development as a targeted treatment for the mentioned diseases.
Research opportunities
Basis for developing new drugs with similar mechanisms of action The compound's unique structure provides a foundation for exploring and developing new drugs that target the same enzyme or have similar therapeutic effects.
Check Digit Verification of cas no
The CAS Registry Mumber 23168-76-5 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 2,3,1,6 and 8 respectively; the second part has 2 digits, 7 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 23168-76:
(7*2)+(6*3)+(5*1)+(4*6)+(3*8)+(2*7)+(1*6)=105
105 % 10 = 5
So 23168-76-5 is a valid CAS Registry Number.
23168-76-5Relevant articles and documents
Discovery and Optimization of 2 H-1λ2-Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer
Rohde, Jason M.,Karavadhi, Surendra,Pragani, Rajan,Liu, Li,Fang, Yuhong,Zhang, Weihe,McIver, Andrew,Zheng, Hongchao,Liu, Qingyang,Davis, Mindy I.,Urban, Daniel J.,Lee, Tobie D.,Cheff, Dorian M.,Hollingshead, Melinda,Henderson, Mark J.,Martinez, Natalia J.,Brimacombe, Kyle R.,Yasgar, Adam,Zhao, Wei,Klumpp-Thomas, Carleen,Michael, Sam,Covey, Joseph,Moore, William J.,Stott, Gordon M.,Li, Zhuyin,Simeonov, Anton,Jadhav, Ajit,Frye, Stephen,Hall, Matthew D.,Shen, Min,Wang, Xiaodong,Patnaik, Samarjit,Boxer, Matthew B.
, p. 4913 - 4946 (2021/05/07)
Neomorphic mutations in isocitrate dehydrogenase 1 (IDH1) are oncogenic for a number of malignancies, primarily low-grade gliomas and acute myeloid leukemia. We report a medicinal chemistry campaign around a 7,7-dimethyl-7,8-dihydro-2H-1λ2-quinoline-2,5(6H)-dione screening hit against the R132H and R132C mutant forms of isocitrate dehydrogenase (IDH1). Systematic SAR efforts produced a series of potent pyrid-2-one mIDH1 inhibitors, including the atropisomer (+)-119 (NCATS-SM5637, NSC 791985). In an engineered mIDH1-U87-xenograft mouse model, after a single oral dose of 30 mg/kg, 16 h post dose, between 16 and 48 h, (+)-119 showed higher tumoral concentrations that corresponded to lower 2-HG concentrations, when compared with the approved drug AG-120 (ivosidenib).
