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[CAS NO. 733030-01-8] Trifluridine/tipiracilhydrochloridemixture
| Ships within | Stock | Price | Qty | Total |
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| Catalog: | HY-16478 |
| Brand: | MCE |
| CAS: | 733030-01-8 |
Overview
| MDL | MFCD30481309 |
|---|---|
| Molecular Weight | 435.76 |
| Molecular Formula | C10H11F3N2O5.1/2C9H11ClN4O2.1/2HCl |
| SMILES | O=C1N([C@H]2C[C@H](O)[C@@H](CO)O2)C=C(C(F)(F)F)C(N1)=O.O=C3N([C@H]4C[C@H](O)[C@@H](CO)O4)C=C(C(F)(F)F)C(N3)=O.O=C5NC(CN6CCCC6=N)=C(Cl)C(N5)=O.Cl |
1 Publications Citing Use of MCE
Summary
Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a potent and orally active nucleoside antitumor agent. The composition of Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a 1:0.5 mixture (on a molar basis) of alpha,alpha,alpha-tri-fluorothymidine (FTD) and thymidine phosphorylase inhibitor (TPI). Trifluridine/tipiracil hydrochloride mixture (TAS-102) shows the antitumor activity mainly via the inhibition of thymidylate synthase (TS) and incorporation into DNA [1] [2] .
In Vivo
Trifluridine/tipiracil hydrochloride mixture (150 mg/kg/day; p.o.; twice a day for 14 days) prevents body weight loss and reduces the relative tumor volume in colorectal cancer and gastric cancer mice models [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male nude mice bearing KM12C, KM12C/5-FU, DLD-1, DLD-1/5-FU, and SC-2 cells [2] |
| Dosage: | 150 mg/kg/day |
| Administration: | p.o.; twice a day for 14 days |
| Result: | Prevented body weight loss and reduced the relative tumor volume in colorectal cancer and gastric cancer mice models. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02500043 | Taiho Oncology, Inc. |
Refractory Metastatic Gastric Cancer
|
February 24, 2016 | Phase 3 |
| NCT01607957 | Taiho Oncology, Inc. |
Colorectal Cancer
|
June 17, 2012 | Phase 3 |
| NCT04042714 | Baylor Research Institute|Taiho Oncology, Inc. |
High-grade Extra Pulmonary Neuroendocrine Cancer
|
August 15, 2019 | Phase 2 |
| NCT03909724 | Amsterdam UMC, location VUmc |
Colorectal Cancer|Metastasis
|
October 1, 2019 | Phase 2|Phase 3 |
| NCT05064059 | Merck Sharp & Dohme LLC |
Colorectal Cancer
|
November 10, 2021 | Phase 3 |
| NCT03278106 | Mayo Clinic|National Cancer Institute (NCI) |
Cholangiocarcinoma|Stage III Gallbladder Cancer AJCC v7|Stage IIIA Gallbladder Cancer AJCC v7|Stage IIIB Gallbladder Cancer AJCC v7|Stage IV Gallbladder Cancer AJCC v7|Stage IVA Gallbladder Cancer AJCC v7|Stage IVB Gallbladder Cancer AJCC v7
|
October 20, 2017 | Phase 2 |
| NCT01955837 | Taiho Pharmaceutical Co., Ltd. |
Colorectal Cancer
|
September 2013 | Phase 3 |
| NCT02286492 | Taiho Oncology, Inc. |
Colorectal Cancer Metastatic
|
||
| NCT01874522 | Taiho Oncology, Inc. |
Advanced Solid Tumors (Excluding Breast Cancer)
|
July 2013 | Phase 1 |
| NCT05364489 | The First Affiliated Hospital of Zhengzhou University |
Advanced Colorectal Cancer
|
June 15, 2022 | Phase 2 |
| NCT05314101 | Fujian Cancer Hospital |
Immunotherapy|Colorectal Cancer
|
April 1, 2022 | Phase 2 |
| NCT02261532 | Taiho Pharmaceutical Co., Ltd. |
Advanced or Metastatic Solid Tumors
|
September 2014 | Phase 1 |
| NCT04776148 | Merck Sharp & Dohme LLC|Eisai Inc. |
Colorectal Neoplasms
|
March 29, 2021 | Phase 3 |
| NCT03686488 | H. Lee Moffitt Cancer Center and Research Institute |
Gastric Adenocarcinoma|Gastroesophageal Junction Adenocarcinoma|Gastric Cancer
|
December 20, 2018 | Phase 2 |
| NCT03305913 | AIO-Studien-gGmbH|Institut für Klinisch-Onkologische Forschung (IKF) am Krankenhaus Nordwest GmbH|Bayer |
Pretreated Metastatic Colorectal Cancer
|
July 31, 2017 | Phase 1 |
| NCT01904253 | Taiho Oncology, Inc.|Taiho Pharmaceutical Co., Ltd. |
Small Cell Lung Cancer (SCLC)
|
July 2013 | Phase 2 |
| NCT04920032 | University of California, Irvine|Taiho Pharmaceutical Co., Ltd.|Natera, Inc. |
Colon Adenocarcinoma|Colorectal Cancer
|
August 26, 2021 | Phase 1 |
| NCT04808791 | AHS Cancer Control Alberta |
Gastroesophageal Junction Adenocarcinoma|Advanced Gastric Carcinoma
|
August 31, 2021 | Phase 2 |
| NCT04074343 | University of California, Irvine|Taiho Pharmaceutical Co., Ltd. |
Gastric Adenocarcinoma|GastroEsophageal Cancer
|
August 26, 2019 | Phase 1 |
| NCT02848079 | Yale University |
Colorectal Neoplasms
|
October 31, 2016 | Phase 1|Phase 2 |
| NCT03297710 | Mayo Clinic|National Cancer Institute (NCI) |
Rectal Adenocarcinoma|Recurrent Rectal Carcinoma|Stage IV Rectal Cancer AJCC v7|Stage IVA Rectal Cancer AJCC v7|Stage IVB Rectal Cancer AJCC v7
|
December 11, 2017 | Phase 1 |
| NCT05004831 | Sun Yat-sen University |
Metastatic Colorectal Cancer
|
March 11, 2022 | Phase 2 |
| NCT03762161 | Rahul Parikh|Taiho Oncology, Inc.|University of Kansas Medical Center |
Bladder Cancer
|
January 3, 2019 | Phase 2 |
| NCT02943733 | University of Wisconsin, Madison|Taiho Pharmaceutical Co., Ltd. |
Neuroendocrine Tumors|Neoplasms|Cancer|Tumors
|
August 22, 2017 | Phase 1 |
| NCT05343013 | M.D. Anderson Cancer Center|Taiho |
Colorectal Cancer
|
June 6, 2022 | Phase 2 |
| NCT02654639 | Georgetown University |
Metastatic Colorectal Cancer
|
February 2016 | Phase 2 |
| NCT04923529 | The University of Hong Kong|Taiho Pharmaceutical Co., Ltd. |
Pancreas Cancer
|
March 1, 2021 | Phase 2 |
| NCT05600309 | Merck Sharp & Dohme LLC |
Colorectal Cancer
|
June 14, 2022 | Phase 3 |
| NCT02860546 | Taiho Oncology, Inc. |
Refractory Metastatic Colorectal Cancer
|
August 29, 2016 | Phase 2 |
| NCT01867879 | Taiho Oncology, Inc. |
Advanced Solid Tumors (Excluding Breast Cancer)
|
June 2013 | Phase 1 |
| NCT04868773 | University of California, Irvine |
Colorectal Cancer|Colorectal Carcinoma|Metastatic Cancer|CRC
|
July 16, 2021 | Phase 1 |
| NCT04683965 | The First Affiliated Hospital with Nanjing Medical University|Jiangsu Hansoh Pharmaceutical Co., Ltd. |
Colorectal Neoplasms
|
January 1, 2021 | Phase 2 |
| NCT05481463 | Sun Yat-sen University |
Pancreatic Neoplasms
|
August 2022 | Phase 2 |
| NCT02301117 | Taiho Oncology, Inc. |
Advanced Solid Tumors
|
January 2015 | Phase 1 |
| NCT04417699 | Providence Health & Services|Taiho Oncology |
Rectal Cancer
|
July 5, 2022 | Phase 2 |
| NCT04627961 | National University Hospital, Singapore |
Metastatic Nasopharyngeal Carcinoma|Recurrent Nasopharyngeal Carcinoma
|
August 26, 2020 | Phase 2 |
| NCT02920476 | University of Florida|Taiho Oncology, Inc. |
Squamous Cell Lung Carcinoma
|
July 19, 2017 | Phase 2 |
| NCT03974594 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. |
Colorectal Cancer
|
May 21, 2019 | Phase 1 |
| NCT02031055 | Taiho Oncology, Inc. |
Advanced Solid Tumors
|
February 2014 | Phase 1 |
| NCT05266820 | Fujian Cancer Hospital |
Metastatic Colorectal Cancer
|
October 1, 2021 | Phase 2 |
| NCT05029102 | Zhejiang University |
Gastric Cancer
|
September 1, 2021 | Phase 2 |
| NCT05328908 | Bristol-Myers Squibb |
Colorectal Neoplasms
|
April 28, 2022 | Phase 3 |
| NCT03520946 | Institut für Klinische Krebsforschung IKF GmbH at Krankenhaus Nordwest|Eli Lilly and Company|Trium Analysis Online GmbH |
Colorectal Cancer
|
January 24, 2019 | Phase 3 |
| NCT01916447 | Taiho Oncology, Inc. |
Advanced Gastrointestinal Tumors
|
September 2013 | Phase 1 |
| NCT02301104 | Taiho Oncology, Inc. |
Advanced Solid Tumors
|
January 2015 | Phase 1 |
| NCT04701476 | Teclison Ltd.|Merck Sharp & Dohme LLC |
Colorectal Cancer; Lung Cancer
|
May 20, 2021 | Phase 2 |
| NCT02613221 | Takeda |
Colorectal Cancer
|
December 7, 2015 | Phase 1|Phase 2 |
| NCT01896856 | Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Van Andel Research Institute|Astex Pharmaceuticals, Inc. |
Previously Treated Metastatic Colorectal Cancer
|
October 23, 2013 | Phase 1|Phase 2 |
| NCT03223779 | Massachusetts General Hospital|Taiho Oncology, Inc. |
Colorectal Cancer
|
October 13, 2017 | Phase 1|Phase 2 |
| NCT02921737 | University of Florida|Taiho Oncology, Inc. |
Pancreatic Cancer
|
November 9, 2017 | Phase 2 |
| NCT03717038 | Symphogen A+S |
Metastatic Colorectal Cancer|Colorectal Cancer Metastatic|Carcinoma
|
February 2019 | Phase 3 |
| NCT04517747 | Institut für Klinische Krebsforschung IKF GmbH at Krankenhaus Nordwest |
Gastric Adenocarcinoma|Metastatic Adenocarcinoma of the Gastroesophageal Junction
|
October 15, 2020 | Not Applicable |
| NCT01867866 | Taiho Oncology, Inc. |
Advanced Solid Tumors
|
May 2013 | Phase 1 |
| NCT02602327 | University of California, San Francisco|Sirtex Medical|Taiho Pharmaceutical Co., Ltd. |
Colon Cancer|Rectal Cancer|Liver Metastases
|
January 9, 2017 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 100 mg/mL ( 229.48 mM ; Need ultrasonic)
DMF : 20 mg/mL ( 45.90 mM ; Need ultrasonic)
DMSO : 2.34 mg/mL ( 5.37 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2948 mL | 11.4742 mL | 22.9484 mL |
| 5 mM | 0.4590 mL | 2.2948 mL | 4.5897 mL |
| 10 mM | 0.2295 mL | 1.1474 mL | 2.2948 mL |
-
1.
Add each solvent one by one: Saline
Solubility: 100 mg/mL (229.48 mM); Clear solution; Need ultrasonic
-
2.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (114.74 mM); Clear solution; Need ultrasonic
References
- [1] Emura T, et al. A novel antimetabolite, TAS-102 retains its effect on FU-related resistant cancer cells. Int J Mol Med. 2004;13(4):545-549.
- [2] Nukatsuka M, et al. Efficacy of combination chemotherapy using a novel oral chemotherapeutic agent, TAS-102, with irinotecan hydrochloride on human colorectal and gastric cancer xenografts. Anticancer Res. 2015;35(3):1437-1445.
- [3] Limagne E, Thibaudin M, Nuttin L, et al. Trifluridine/Tipiracil plus Oxaliplatin Improves PD-1 Blockade in Colorectal Cancer by Inducing Immunogenic Cell Death and Depleting Macrophages. Cancer Immunol Res. 2019;7(12):1958-1969.
- [4] Suzuki N, Nakagawa F, Takechi T. Trifluridine/tipiracil increases survival rates in peritoneal dissemination mouse models of human colorectal and gastric cancer [published correction appears in Oncol Lett. 2021 Jul;22(1):511]. Oncol Lett. 2017;14(1):639-6
Synonyms
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