HMN-214
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50:HMN-176对几种肿瘤细胞系表现出强烈的细胞毒性,平均IC50为118 nmol/L。
Polo样激酶(PLK)是高度保守的丝氨酸/苏氨酸激酶,可以作为有丝分裂的调节酶。HMN-214是HMN-176的口服前药,是一种二苯乙烯衍生物,参与干扰polo样激酶1的亚细胞空间位置,polo样激酶1是调节关键的有丝分裂事件的丝氨酸/苏氨酸激酶。
体外实验:HMN-176具有强效的细胞毒性作用,平均IC50为118 nM。HNM-176的细胞毒性优于ADM、VP-16和CDDP,但不如紫杉酚和VCR。与参考药剂相比,HMN-176的log(IC50)变化较小。此外,与测试的其他试剂相比,通过判断其低耐药指数,HMN-176对具有药物耐受表型的肿瘤细胞具有更强的细胞毒性[1]。
体内:PK研究表明,HNM-214是HMN-176的一个可接受的口服前体药物。体内分析HMN-214的时间依赖性发现,重复给药5天可诱发有效的抗肿瘤活性,与细胞计数研究中HMN-176依赖性的细胞毒性预期结果一致。HMN-214对人肿瘤异种移植物的抗肿瘤活性与临床可用试剂效果相当或更有效,包括顺铂、阿霉素、长春新碱和UFT,无严重毒性如神经毒性[1]。
临床试验:I期临床药代动力学研究表明,重复给药没有HMN-176及其代谢产物的积累。在29例患者中,有7例病情稳定,严重的乳腺癌患者达到6个月的病情稳定期。在一例大肠癌患者中有短暂的癌胚抗原下降[2]。
参考文献:
[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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 424.47 |
Cas No. | 173529-46-9 |
Formula | C22H20N2O5S |
Solubility | ≥21.2 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
Chemical Name | N-(4-methoxyphenyl)sulfonyl-N-[2-[(E)-2-(1-oxidopyridin-1-ium-4-yl)ethenyl]phenyl]acetamide |
SDF | Download SDF |
Canonical SMILES | CC(=O)N(C1=CC=CC=C1C=CC2=CC=[N+](C=C2)[O-])S(=O)(=O)C3=CC=C(C=C3)OC |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Description | HMN-214是HMN-176的前体药物,是强效和广谱的抗肿瘤试剂。 | |||||
靶点 | PLK1 | |||||
IC50 |
质量控制和MSDS
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