1432660-47-3 Usage
Description
AGI-6780 is a potent and selective small molecule inhibitor of the tumor-associated mutant IDH2 (Isocitrate Dehydrogenase-2) in leukemia cells. It is specifically designed to target the IDH2 R140Q mutant, with an IC50 of 23 nM, making it a valuable compound for IDH-related research.
Uses
Used in Oncology Research:
AGI-6780 is used as a research tool for studying the role of mutant IDH2 in leukemia and other cancer types. Its potent and selective inhibition of the IDH2 R140Q mutant allows researchers to investigate the underlying molecular mechanisms and potential therapeutic strategies for IDH2-driven malignancies.
Used in Drug Development:
AGI-6780 serves as a starting point for the development of novel therapeutics targeting IDH2 mutations in cancer. Its high specificity and potency make it a promising candidate for further optimization and evaluation in preclinical and clinical studies, with the potential to improve treatment options for patients with IDH2-mutated leukemia and other cancers.
Used in Diagnostic Applications:
AGI-6780 can be employed in the development of diagnostic tests to identify patients with IDH2 R140Q mutations. Accurate identification of these patients can help guide personalized treatment strategies and improve patient outcomes by providing targeted therapies.
Used in Combination Therapies:
AGI-6780 may be used in combination with other cancer treatments, such as chemotherapy or targeted therapies, to enhance the overall efficacy of treatment regimens. Its selective inhibition of the IDH2 R140Q mutant can potentially synergize with other treatments, leading to improved outcomes for patients with IDH2-mutated cancers.
In vitro
AGI-6780 potently reduce (R)-2-hydroxyglutarate (2HG) levels in cell lines ectopically overexpressing IDH2/R140Q with EC50 of 20 nM, with excellent selectivity against other dehydrogenases. AGI-6780 reverses the IDH2/R140Q-induced differentiation block in TF-1 cells, and induces blast differentiation in primary human IDH2/R140Q AML patient samples.
Biological Activity
agi-6780 is a potent and selective inhibitor of tumor-associated idh2/r140q mutation with ic50 value of 23 nm [1].agi-6780 could significantly reduce intracellular concentration of 2hg in the human glioblastoma tf1/r140q cells, as well as reverse idh2/r140q-mediated differentiation block in tf1 cells in the presence of epo. agi-6780 could restore klf1 and hemoglobin g1/2 expressions in the epo-induced tf1/r140q cells [1].
references
[1] wang f1, travins j, delabarre b, penard-lacronique v, schalm s, hansen e, straley k, kernytsky a, liu w, gliser c, yang h, gross s, artin e, saada v,mylonas e, quivoron c, popovici-muller j, saunders jo, salituro fg, yan s, murray s, wei w, gao y, dang l, dorsch m, agresta s, schenkein dp, biller sa, su sm, de botton s, yen ke. targeted inhibition of mutant idh2 in leukemia cells induces cellular differentiation. science. 2013 may 3;340(6132):622-6.
Check Digit Verification of cas no
The CAS Registry Mumber 1432660-47-3 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,3,2,6,6 and 0 respectively; the second part has 2 digits, 4 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 1432660-47:
(9*1)+(8*4)+(7*3)+(6*2)+(5*6)+(4*6)+(3*0)+(2*4)+(1*7)=143
143 % 10 = 3
So 1432660-47-3 is a valid CAS Registry Number.
1432660-47-3Relevant articles and documents
THERAPEUTIC COMPOUNDS AND COMPOSITIONS
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Page/Page column 138; 144, (2014/05/07)
Provided are aryl sulfonamide diarylurea derivative compounds that are inhibitors of mutant isocitrate dehydrogenase 1/2 (IDH 1/2), useful for treating cancer. Also provided are methods of treating cancer comprising administering to a subject in need thereof a compound described herein. Cancers that are treatable by the compounds of the invention are glioblastoma, myelodysplastic syndrome, myeloproliferative neoplasm, acute myelogenous leukemia, sarcoma, melanoma, non-small cell lung cancer, chondrosarcoma, and non-Hodgkin's lymphoma (NHL).
