173529-46-9 Usage
Description
HMN-214 is an orally bioavailable prodrug form of HMN-176, an indirect inhibitor of polo-like kinase (PLK) activity that inhibits the proliferation of a variety of cancer cells. It is characterized by its ability to decrease the expression of multidrug resistance gene 1 (MDR1) in certain cell lines and tumor models, as well as its effectiveness in reducing tumor volume across different mouse xenograft models without causing significant adverse effects on nerve conduction.
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 articles and documents
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.
