905973-89-9 Usage
Uses
Used in Anticancer Applications:
2,2-DIPHENYL-N-(2,2,2-TRICHLORO-1-[3-(4-FLUORO-3-NITROPHENYL)THIOUREIDO]ETHYL)ACETAMIDE is used as an anticancer agent for its ability to inhibit the ATM protein/kinase, which is involved in the DNA damage response pathway in cells. By suppressing ATM-mediated p21 expression required for survival in prematurely senescent breast, lung, and colon cancer cells, CGK733 results in cell death. Additionally, when used in combination with caffeine, it leads to a rapid decline in cyclin D1 protein levels and a reduction in retinoblastoma protein levels, inhibiting the proliferation of human cancer cell lines.
Used in Enhancing the Therapeutic Capacity of Genotoxic Anti-Cancer Regimens:
2,2-DIPHENYL-N-(2,2,2-TRICHLORO-1-[3-(4-FLUORO-3-NITROPHENYL)THIOUREIDO]ETHYL)ACETAMIDE is used as a strategy to increase the therapeutic capacity of certain genotoxic anti-cancer regimens by sensitizing cancer cells to these agents. Inhibiting the ATM and ATMand Rad3-related (ATR) kinases signaling pathway with CGK733 can activate cell cycle arrest, DNA repair, induction of premature senescence, and cell death, making cancer cells more susceptible to the effects of genotoxic agents.
Biological Activity
Originally defined as a selective inhibitor of ATR and ATM kinases that reverses senescence in human BJ and HMEC cells. Decreases p21 CIP1 levels in senescent with no effect on p53 and Bcl-2 family members.
Check Digit Verification of cas no
The CAS Registry Mumber 905973-89-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,0,5,9,7 and 3 respectively; the second part has 2 digits, 8 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 905973-89:
(8*9)+(7*0)+(6*5)+(5*9)+(4*7)+(3*3)+(2*8)+(1*9)=209
209 % 10 = 9
So 905973-89-9 is a valid CAS Registry Number.
InChI:InChI=1/C23H18Cl3FN4O3S/c24-23(25,26)21(30-22(35)28-16-11-12-17(27)18(13-16)31(33)34)29-20(32)19(14-7-3-1-4-8-14)15-9-5-2-6-10-15/h1-13,19,21H,(H,29,32)(H2,28,30,35)
905973-89-9Relevant academic research and scientific papers
ATM AND ATR INHIBITOR
-
Page/Page column 36, (2008/06/13)
The present invention relates to a urea compound of formula (1) and a pharmaceutically acceptable salt thereof having inhibitory activity of ATM and ATR. According to the present invention, the urea compound of formula (1) selectively binds to ATM and ATR, and thus specifically suppresses the function of ATM and ATR as protein kinase. Therefore, the urea compound according to the present invention can be used for controlling cell function and treating diseases, in connection with function abnormality in ATM and ATR
