Tipiracil hydrochloride
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.
Tipiracil hydrochloride是一种胸苷磷酸化酶（TP）抑制剂。
胸苷磷酸化酶（TP）是嘧啶核苷补救途径的关键酶。TP催化胸苷可逆磷酸化，从而合成胸腺嘧啶和2-脱氧-D-核糖-1-磷酸。
Tipiracil（TPI）和Trifluridine（FTD）是TAS-102的活性成分，分子比为1: 0.5。TAS-102作为一个新型的口服核苷类抗肿瘤药物，正处于临床试验阶段。与单独静脉注射FTD不同， TPI和FTD联合使用时采取口服给药方式[1]。当口服给予FTD时，FTD在肠内和肝脏中迅速降解成无活性形式（首过效应）[2]，但与TPI合用时，TPI有助于保持足够的FTD血浆浓度[3]。因此，TPI加强了FTD的抗肿瘤活性，FTD对TPI的最佳分子比是1：0.5[3]。
参考文献：
1. Tsukihara H1, Nakagawa F2, Sakamoto K et al. Efficacy of combination chemotherapy using a novel oral chemotherapeutic agent, TAS-102, together with bevacizumab, cetuximab, or panitumumab on human colorectal cancer xenografts. Oncol Rep. 2015 May;33(5):2135-42.
2. Dexter DL, Wolberg WH, Ansfield FJ, Helson L and Heidelberger C: The clinical pharmacology of 5-trifluoro-methyl-2'-deoxyuridine. Cancer Res 32: 247-253, 1972.
3. Fukushima M, Suzuki N, Emura T et al. Structure and activity of specific inhibitors of thymidine phosphorylase to potentiate the function of antitumor 2'-deoxyribonucleosides. biochem Pharmacol 59: 1227-1236, 2000.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 279.12 |
| Cas No. | 183204-72-0 |
| Formula | C9H12Cl2N4O2 |
| Synonyms | Tipiracil |
| Solubility | insoluble in DMSO; insoluble in EtOH; ≥13.25 mg/mL in H2O |
| Chemical Name | 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione;hydrochloride |
| SDF | Download SDF |
| Canonical SMILES | C1CC(=N)N(C1)CC2=C(C(=O)NC(=O)N2)Cl.Cl |
| 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。 |
| 动物实验 [1]: | |
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动物模型 |
携带结直肠癌和胃癌异种移植肿瘤的裸鼠模型 |
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给药剂量 |
每日150 mg/kg（Trifluridine和Tipiracil Hydrochloride联合用药）；口服给药；每日2次，持续14天 |
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实验结果 |
在结直肠癌（HCT116和SW-48细胞）和胃癌（SC-2和MKN74细胞）小鼠中，联合使用TAS-102（由Trifluridine和Tipiracil Hydrochloride组成）和Oxaliplatin在肿瘤生长抑制活性和RTV5方面显著优于单一治疗。在体内，TAS-102单一治疗能作用于MKN74/5FU细胞。TAS-102与Oxaliplatin联合用药显著增强其抗肿瘤活性。与单一治疗相比，上述联合用药不会导致显著的体重下降或毒性。 |
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其它注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。 |
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References: [1]. Tsukihara H, Nakagawa F, Sakamoto K et al. Efficacy of combination chemotherapy using a novel oral chemotherapeutic agent, TAS-102, together with bevacizumab, cetuximab, or panitumumab on human colorectal cancer xenografts. Oncol Rep. 2015 May;33(5):2135-42. |
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| Description | Tipiracil hydrochloride是一种胸苷磷酸化酶抑制剂。 | |||||
| 靶点 | thymidine phosphorylase | |||||
| IC50 | ||||||
质量控制和MSDS
- 批次:
化学结构
