173529-46-9 Usage
Uses
Used in Pharmaceutical Industry:
HMN-214 is used as an anticancer agent for patients with advanced solid tumors. It functions as a prodrug of HMN-176, which interferes with the subcellular spatial location of polo-like kinase-1 (PLK1), a key enzyme involved in cell division and proliferation. By targeting PLK1, HMN-214 exhibits potential in treating various types of cancer.
Additionally, HMN-214 is used as a chemosensitizer to overcome multidrug resistance in cancer treatment. It decreases the expression of the multidrug resistance gene 1 (MDR1) in AB-A.1 cells and in tumors isolated from mice bearing multidrug-resistant KB-A1 xenografts, enhancing the effectiveness of conventional chemotherapy.
Used in Oncology Research:
HMN-214 is utilized as a research tool to study the role of polo-like kinase (PLK) in cancer cell proliferation and the development of multidrug resistance. Its ability to inhibit PLK activity and reduce MDR1 expression makes it a valuable compound for understanding the underlying mechanisms of cancer progression and resistance to treatment.
in vitro
hmn-176 showed potent cytotoxicity, with a mean ic50 of 118 nm. the cytotoxic effecacy of hnm-176 was superior to that of adm, vp-16 and cddp, but inferior to that of taxol and vcr. hmn-176 showed less vaiance in log(ic50) than did the reference agents. in addition, judging by its low resistance indices, hmn-176 was more cytotoxic toward the drug-resistant phenotypes of tumor cells than were the other agents tested [1].
in vivo
pk studies showed that hnm-214 was an acceptable oral prodrug of hmn-176. in the in vivo analysis of the schedule-dependency of hmn-214, the repeated administration for over 5 days elicited potent antitumor activity, as expected from the exposure-dependency of the cytotoxicity of hmn-176 and from the cytometric studies. the antitumor activity of hmn-214 against human tumor xenografts was equal or superior to that of clinically avaiable agents, including cis-platinum, adriamycin, vincristine and uft without severe toxicity such as neurotoxicity [1].
IC 50
hmn-176 showed potent cytotoxic activity against several tumor cell lines with an average ic50 of 118 nmol/l
references
[1] takagi m, honmura t, watanabe s, yamaguchi r, nogawa m, nishimura i, katoh f, matsuda m, hidaka h. in vivo antitumor activity of a novel sulfonamide, hmn-214, against human tumor xenografts in mice and the spectrum of cytotoxicity of its active metabolite, hmn-176. invest new drugs. 2003 nov;21(4):387-99.[2] garland ll, taylor c, pilkington dl, cohen jl, von hoff dd. a phase i pharmacokinetic study of hmn-214, a novel oral stilbene derivative with polo-like kinase-1-interacting properties, in patients with advanced solid tumors. clin cancer res. 2006 sep 1;12(17):5182-9.
Check Digit Verification of cas no
The CAS Registry Mumber 173529-46-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,7,3,5,2 and 9 respectively; the second part has 2 digits, 4 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 173529-46:
(8*1)+(7*7)+(6*3)+(5*5)+(4*2)+(3*9)+(2*4)+(1*6)=149
149 % 10 = 9
So 173529-46-9 is a valid CAS Registry Number.
173529-46-9Relevant academic research and scientific papers
Aminostilbazole derivative and medicine
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, (2008/06/13)
The invention relates to an aminostilbazole derivative of the following formula or a hydrate thereof, and a salt thereof. STR1 wherein R1 and R2 each represents hydrogen etc.; R3, R4, R13, and R14 each represents hydrogen, C1-3 acyl, halogen, hydroxy etc.; R5 represents hydrogen or hydroxy-substituted C1-3 alkyl etc.; R6 represents benzenesulfonyl substituted by C1-3 alkoxy etc.; ring Y represents phenyl etc.; ring Z represents 4-pyridyl, its oxide etc. The compound is useful or the treatment of various malignant tumors.
