HMN-214
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MedKoo CAT#: 201490

CAS#: 173529-46-9

Description: HMN-214 is potent PLK inhibitor, HMN-214 is an oral prodrug of HMN-176, a stilbene derivative that interferes with the subcellular spatial location of polo-like kinase-1, a serine/threonine kinase that regulates critical mitotic events.

Chemical Structure

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HMN-214
CAS# 173529-46-9
Instruction

Theoretical Analysis

MedKoo Cat#: 201490
Name: HMN-214
CAS#: 173529-46-9
Chemical Formula: C22H20N2O5S
Exact Mass: 424.11
Molecular Weight: 424.470
Elemental Analysis: C, 62.25; H, 4.75; N, 6.60; O, 18.85; S, 7.55

Price and Availability

Size Price Availability Quantity
25mg USD 250
50mg USD 450
100mg USD 750 2 Weeks
200mg USD 1250 2 Weeks
500mg USD 2650 2 Weeks
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Synonym: HMN214; HMN 214; HMN-214

IUPAC/Chemical Name: (E)-4-(2-(N-((4-methoxyphenyl)sulfonyl)acetamido)styryl)pyridine 1-oxide

InChi Key: OCKHRKSTDPOHEN-BQYQJAHWSA-N

InChi Code: InChI=1S/C22H20N2O5S/c1-17(25)24(30(27,28)21-11-9-20(29-2)10-12-21)22-6-4-3-5-19(22)8-7-18-13-15-23(26)16-14-18/h3-16H,1-2H3/b8-7+

SMILES Code: CC(N(C1=CC=CC=C1/C=C/C2=CC=[N+]([O-])C=C2)S(=O)(C3=CC=C(OC)C=C3)=O)=O

Appearance: Solid powder

Purity: >98%

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Phase I trials of HMN-214: Thirty-three patients were enrolled onto four dosing cohorts of HMN-214 from 3 to 9.9 mg/m2/d using a continuous 21-day dosing schedule every 28 days, with pharmacokinetic sampling during cycle 1. RESULTS:  A severe myalgia/bone pain syndrome and hyperglycemia were dose-limiting toxicities at 9.9 mg/m2/d. A dose reduction and separate enrollment by pretreatment status (lightly versus heavily pretreated) was undertaken, with one dose-limiting toxicity (grade 3 bone pain) at 8 mg/m2/d. The maximum tolerated dose was defined as 8 mg/m2/d for both treatment cohorts. Dose-proportional increases were observed in AUC but not Cmax. There was no accumulation of HMN-176, the metabolite of HMN-214, with repeated dosing. Seven of 29 patients had stable disease as best tumor response, including 6-month stable disease in a heavily pretreated breast cancer patient. A transient decline in carcinoembryonic antigen in a patient with colorectal cancer was noted. CONCLUSIONS: The maximum tolerated dose and recommended phase II dose of HMN-214 when administered on this schedule was 8 mg/m2/d regardless of pretreatment status. Further development of HMN-214 will focus on patient populations for which high expression of polo-like kinase-1 is seen (i.e., prostate and pancreatic cancer patients). (source: Clin Cancer Res. 2006 Sep 1;12(17):5182-9.).    

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 424.47 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1. Schoffski, Patrick. Polo-like kinase (PLK) inhibitors in preclinical and early clinical development in oncology. Oncologist (2009), 14(6), 559-570. CODEN: OCOLF6 ISSN:1083-7159. CAN 152:421294 AN 2009:879296

2. Low, Jonathan; Chakravartty, Arunava; Blosser, Wayne; Dowless, Michele; Chalfant, Christopher; Bragger, Patty; Stancato, Louis. Phenotypic fingerprinting of small molecule cell cycle kinase inhibitors for drug discovery. Current Chemical Genomics (2009), 3 13-21. CODEN: CCGUAQ ISSN:1875-3973. CAN 152:254294 AN 2009:623851

3. Xiang, Youbin; Jaspersen, Sue; Florens, Laurence; Smith, Sarah Kendall; Hawley, R. Scott. Inhibition of Polo kinase by Matrimony protein maintains G2 arrest in the meiotic cell cycle. U.S. Pat. Appl. Publ. (2009), 41 pp. CODEN: USXXCO US 2009123934 A1 20090514 CAN 150:533852 AN 2009:587922

4. Hu, Laixing; Li, Zhou-rong; Wang, Yue-ming; Jiang, Jian-dong; Boykin, David W. Structure-activity relationships of novel pyridinyl and pyrimidinyl carbazole sulfonamides as antiproliferative agents. Abstracts, 58th Southeast Regional Meeting of the American Chemical Society, Augusta, GA, United States, November 1-4 (2006), SRM06-194. CODEN: 69INUY AN 2006:1190723

5. Palazzo, Robert E. Marine invertebrate gametes and embryos as an assay system for therapeutic screening. U.S. Pat. Appl. Publ. (2006), 12pp. CODEN: USXXCO US 2006240402 A1 20061026 CAN 145:432189 AN 2006:1123520

6. Garland, Linda L.; Taylor, Charles; Pilkington, Deborah L.; Cohen, Jan L.; Von Hoff, Daniel D. 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. Clinical Cancer Research (2006), 12(17), 5182-5189. CODEN: CCREF4 ISSN:1078-0432. CAN 146:454294 AN 2006:899334

7. Medina-Gundrum, Leticia; Cerna, Cesario; Gomez, Lionel; Izbicka, Elzbieta. Investigation of HMN-176 anticancer activity in human tumor specimens in vitro and the effects of HMN-176 on differential gene expression. Investigational New Drugs (2005), 23(1), 3-9. CODEN: INNDDK ISSN:0167-6997. CAN 142:290700 AN 2004:930695

8. Tanaka, Hideki; Ohshima, Nobuko; Ikenoya, Mami; Komori, Kinuyo; Katoh, Fumitaka; Hidaka, Hiroyoshi. HMN-176, an Active Metabolite of the Synthetic Antitumor Agent HMN-214, Restores Chemosensitivity to Multidrug-Resistant Cells by Targeting the Transcription Factor NF-Y. Cancer Research (2003), 63(20), 6942-6947. CODEN: CNREA8 ISSN:0008-5472. CAN 140:174617 AN 2003:845423

9. Takagi, Manabu; Honmura, Takuya; Watanabe, Shuuji; Yamaguchi, Reiko; Nogawa, Masaki; Nishimura, Ikumi; Katoh, Fumitaka; Matsuda, Masato; Hidaka, Hiroyoshi. 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. Investigational New Drugs (2003), 21(4), 387-399. CODEN: INNDDK ISSN:0167-6997. CAN 141:16960 AN 2003:833144

10. Bayes M; Rabasseda X; Prous J R Gateways to clinical trials. Methods and findings in experimental and clinical pharmacology (2004), 26(8), 639-63. Journal code: 7909595. ISSN:0379-0355. PubMed ID 15605126 AN 2004629312