[CAS NO. 183204-72-0] Tipiracilhydrochloride

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PRODUCTS SPECIFICATIONS [183204-72-0]

Catalog

HY-A0063

Brand

MCE

CAS

183204-72-0

DESCRIPTION [183204-72-0]

Overview

MDL	MFCD01571384
Molecular Weight	279.12
Molecular Formula	C9H12Cl2N4O2
SMILES	[H]Cl.O=C1C(Cl)=C(CN2C(CCC2)=N)NC(N1)=O

For research use only. We do not sell to patients.

4 Publications Citing Use of MCE

Summary

Tipiracil (hydrochloride) is a thymidine phosphorylase inhibitor (TPI), used for cancer research.

In Vitro

Tipiracil has antiangiogenic effect, and inhibits proliferation of endothelial cells ^[1] . Tipiracil is a potent inhibitor of thymidine phosphorylase, which is the enzyme that degrades FTD ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT05198934	Amgen	Colorectal Cancer (CRC)	April 19, 2022	Phase 3
NCT04294264	Rutgers, The State University of New Jersey\|National Cancer Institute (NCI)	Metastatic Colorectal Carcinoma\|Recurrent Colon Carcinoma\|Refractory Colorectal Carcinoma\|Stage IV Colon Cancer AJCC v7\|Stage IVA Colon Cancer AJCC v7\|Stage IVB Colon Cancer AJCC v7	February 12, 2019	Phase 2
NCT04104139	OHSU Knight Cancer Institute\|Oregon Health and Science University\|Taiho Pharmaceutical Co., Ltd.	Rectal Adenocarcinoma\|Stage IIA Rectal Cancer AJCC v8\|Stage IIB Rectal Cancer AJCC v8\|Stage III Rectal Cancer AJCC v8\|Stage IIIA Rectal Cancer AJCC v8\|Stage IIIB Rectal Cancer AJCC v8\|Stage IIIC Rectal Cancer AJCC v8	December 11, 2019	Phase 1
NCT03317119	City of Hope Medical Center\|National Cancer Institute (NCI)	Metastatic Colon Carcinoma\|Metastatic Colorectal Carcinoma\|Metastatic Rectal Carcinoma\|RAS Family Gene Mutation\|Stage III Colon Cancer AJCC v7\|Stage III Colorectal Cancer AJCC v7\|Stage III Rectal Cancer AJCC v7\|Stage IIIA Colon Cancer AJCC v7\|Stage IIIA Colorectal Cancer AJCC v7\|Stage IIIA Rectal Cancer AJCC v7\|Stage IIIB Colon Cancer AJCC v7\|Stage IIIB Colorectal Cancer AJCC v7\|Stage IIIB Rectal Cancer AJCC v7\|Stage IIIC Colon Cancer AJCC v7\|Stage IIIC Colorectal Cancer AJCC v7\|Stage IIIC Rectal Cancer AJCC v7\|Stage IV Colon Cancer AJCC v7\|Stage IV Colorectal Cancer AJCC v7\|Stage IV Rectal Cancer AJCC v7\|Stage IVA Colon Cancer AJCC v7\|Stage IVA Colorectal Cancer AJCC v7\|Stage IVA Rectal Cancer AJCC v7\|Stage IVB Colon Cancer AJCC v7\|Stage IVB Colorectal Cancer AJCC v7\|Stage IVB Rectal Cancer AJCC v7	April 11, 2018	Phase 1
NCT05356897	Academic and Community Cancer Research United\|National Cancer Institute (NCI)	Metastatic Colon Adenocarcinoma\|Metastatic Colorectal Adenocarcinoma\|Metastatic Rectal Adenocarcinoma\|Stage IV Colon Cancer AJCC v8\|Stage IV Colorectal Cancer AJCC v8\|Stage IV Rectal Cancer AJCC v8	November 30, 2022	Phase 2
NCT04109924	Roswell Park Cancer Institute\|National Comprehensive Cancer Network	Advanced Colorectal Carcinoma\|Metastatic Colon Adenocarcinoma\|Metastatic Rectal Adenocarcinoma\|Recurrent Colon Adenocarcinoma\|Recurrent Colorectal Adenocarcinoma\|Recurrent Rectal Adenocarcinoma\|Stage III Colon Cancer AJCC v8\|Stage III Colorectal Cancer AJCC v8\|Stage III Rectal Cancer AJCC v8\|Stage IIIA Colon Cancer AJCC v8\|Stage IIIA Colorectal Cancer AJCC v8\|Stage IIIB Colorectal Cancer AJCC v8\|Stage IIIB Rectal Cancer AJCC v8\|Stage IIIC Colon Cancer AJCC v8\|Stage IIIC Colorectal Cancer AJCC v8\|Stage IV Colon Cancer AJCC v8\|Stage IVA Colorectal Cancer AJCC v8\|Stage IVA Rectal Cancer AJCC v8\|Stage IVB Colon Cancer AJCC v8\|Stage IVB Colorectal Cancer AJCC v8\|Stage IVB Rectal Cancer AJCC v8\|Stage IVC Colon Cancer AJCC v8\|Stage IVC Colorectal Cancer AJCC v8\|Stage IVC Rectal Cancer AJCC v8\|Unresectable Colon Adenocarcinoma\|Unresectable Colorectal Carcinoma\|Unresectable Rectal Adenocarcinoma	December 27, 2019	Phase 2
NCT05468892	University of Campania Luigi Vanvitelli	Metastatic Colon Cancer	October 29, 2019	Phase 2
NCT03844620	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Refractory Colorectal Carcinoma\|Stage III Colorectal Cancer AJCC v8\|Stage IIIA Colorectal Cancer AJCC v8\|Stage IIIB Colorectal Cancer AJCC v8\|Stage IIIC Colorectal Cancer AJCC v8\|Stage IV Colorectal Cancer AJCC v8\|Stage IVA Colorectal Cancer AJCC v8\|Stage IVB Colorectal Cancer AJCC v8\|Stage IVC Colorectal Cancer AJCC v8	January 29, 2019	Phase 2
NCT03974594	Chia Tai Tianqing Pharmaceutical Group Co., Ltd.	Colorectal Cancer	May 21, 2019	Phase 1
NCT04097028	Roswell Park Cancer Institute\|National Comprehensive Cancer Network	Clinical Stage IIA Esophageal Adenocarcinoma AJCC v8\|Clinical Stage IIA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Clinical Stage III Esophageal Adenocarcinoma AJCC v8\|Clinical Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8\|Clinical Stage IVA Esophageal Adenocarcinoma AJCC v8\|Clinical Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IIB Esophageal Adenocarcinoma AJCC v8\|Pathologic Stage IIB Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage III Esophageal Adenocarcinoma AJCC v8\|Pathologic Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IIIA Esophageal Adenocarcinoma AJCC v8\|Pathologic Stage IIIA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IIIB Esophageal Adenocarcinoma AJCC v8\|Pathologic Stage IIIB Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IVA Esophageal Adenocarcinoma AJCC v8\|Pathologic Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8	December 20, 2019	Phase 2
NCT05130060	Mayo Clinic\|National Cancer Institute (NCI)	Metastatic Colon Adenocarcinoma\|Metastatic Colorectal Adenocarcinoma\|Metastatic Colorectal Carcinoma\|Metastatic Microsatellite Stable Colon Carcinoma\|Metastatic Microsatellite Stable Colorectal Carcinoma\|Metastatic Rectal Adenocarcinoma\|Microsatellite Stable Rectal Carcinoma\|Stage IV Colorectal Cancer AJCC v8\|Stage IVA Colorectal Cancer AJCC v8\|Stage IVB Colorectal Cancer AJCC v8\|Stage IVC Colorectal Cancer AJCC v8	January 10, 2022	Phase 1
NCT04660760	Academic and Community Cancer Research United\|National Cancer Institute (NCI)	Clinical Stage III Gastric Cancer AJCC v8\|Clinical Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8\|Clinical Stage IV Gastric Cancer AJCC v8\|Clinical Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8\|Clinical Stage IVA Gastric Cancer AJCC v8\|Clinical Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Clinical Stage IVB Gastric Cancer AJCC v8\|Clinical Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC v8\|Locally Advanced Unresectable Gastric Adenocarcinoma\|Locally Advanced Unresectable Gastroesophageal Junction Adenocarcinoma\|Metastatic Gastric Adenocarcinoma\|Metastatic Gastroesophageal Junction Adenocarcinoma\|Pathologic Stage III Gastric Cancer AJCC v8\|Pathologic Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IIIA Gastric Cancer AJCC v8\|Pathologic Stage IIIA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IIIB Gastric Cancer AJCC v8\|Pathologic Stage IIIB Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IIIC Gastric Cancer AJCC v8\|Pathologic Stage IV Gastric Cancer AJCC v8\|Pathologic Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC v8\|Postneoadjuvant Therapy Stage III Gastric Cancer AJCC v8\|Postneoadjuvant Therapy Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8\|Postneoadjuvant Therapy Stage IIIA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Postneoadjuvant Therapy Stage IIIB Gastroesophageal Junction Adenocarcinoma AJCC v8\|Postneoadjuvant Therapy Stage IV Gastric Cancer AJCC v8\|Postneoadjuvant Therapy Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8\|Postneoadjuvant Therapy Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Postneoadjuvant Therapy Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC v8	June 16, 2021	Phase 2
NCT04854434	Karyopharm Therapeutics Inc	Metastatic Colorectal Cancer	June 29, 2021	Phase 2
NCT03368963	Emory University\|Taiho Oncology, Inc.\|Ipsen	Colorectal Adenocarcinoma\|Gastric Adenocarcinoma\|Metastatic Pancreatic Adenocarcinoma\|Non-Resectable Cholangiocarcinoma\|Stage IV Colorectal Cancer\|Stage IV Gastric Cancer\|Stage IV Pancreatic Cancer\|Stage IVA Colorectal Cancer\|Stage IVB Colorectal Cancer\|Stage III Colorectal Cancer\|Stage III Gastric Cancer\|Stage III Pancreatic Cancer\|Unresectable Digestive System Adenocarcinoma\|Unresectable Pancreatic Carcinoma	January 30, 2018	Phase 1\|Phase 2
NCT04457297	National Cancer Center Hospital East\|Alpha-A, Inc.	Colorectal Neoplasms\|Trifluridine and Tipiracil\|Circulating Tumor DNA	July 8, 2020	Phase 3
NCT04511039	Roswell Park Cancer Institute\|Pfizer	Advanced Malignant Solid Neoplasm\|Clinical Stage III Gastroesophageal Junction Adenocarcinoma\|Clinical Stage IV Gastroesophageal Junction Adenocarcinoma\|Clinical Stage IVA Gastroesophageal Junction Adenocarcinoma\|Clinical Stage IVB Gastroesophageal Junction Adenocarcinoma A\|Locally Advanced Colorectal Carcinoma\|Locally Advanced Gastroesophageal Junction Adenocarcinoma\|Metastatic Colorectal Adenocarcinoma\|Metastatic Gastroesophageal Junction Adenocarcinoma\|Pathologic Stage III Gastroesophageal Junction Adenocarcinoma\|Pathologic Stage IIIA Gastroesophageal Junction Adenocarcinoma\|Pathologic Stage IIIB Gastroesophageal Junction Adenocarcinoma\|Pathologic Stage IV Gastroesophageal Junction Adenocarcinoma\|Pathologic Stage IVA Gastroesophageal Junction Adenocarcinoma\|Pathologic Stage IVB Gastroesophageal Junction Adenocarcinoma\|Postneoadjuvant Therapy Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8\|Postneoadjuvant Therapy Stage IIIA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Postneoadjuvant Therapy Stage IIIB Gastroesophageal Junction Adenocarcinoma AJCC v8\|Postneoadjuvant Therapy Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8\|Postneoadjuvant Therapy Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Postneoadjuvant Therapy Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC v8\|Stage III Colorectal Cancer AJCC v8\|Stage IIIA Colorectal Cancer AJCC v8\|Stage IIIB Colorectal Cancer AJCC v8\|Stage IIIC Colorectal Cancer AJCC v8\|Stage IV Colorectal Cancer AJCC v8\|Stage IVA Colorectal Cancer AJCC v8\|Stage IVB Colorectal Cancer AJCC v8\|Stage IVC Colorectal Cancer AJCC v8	May 28, 2021	Phase 1
NCT04072445	Mayo Clinic\|National Cancer Institute (NCI)\|National Comprehensive Cancer Network	Advanced Bile Duct Carcinoma\|Advanced Gallbladder Carcinoma\|Refractory Bile Duct Carcinoma\|Refractory Gallbladder Carcinoma\|Stage III Distal Bile Duct Cancer AJCC v8\|Stage III Gallbladder Cancer AJCC v8\|Stage III Intrahepatic Bile Duct Cancer AJCC v8\|Stage IIIA Distal Bile Duct Cancer AJCC v8\|Stage IIIA Gallbladder Cancer AJCC v8\|Stage IIIA Intrahepatic Bile Duct Cancer AJCC v8\|Stage IIIB Distal Bile Duct Cancer AJCC v8\|Stage IIIB Gallbladder Cancer AJCC v8\|Stage IIIB Intrahepatic Bile Duct Cancer AJCC v8\|Stage IV Distal Bile Duct Cancer AJCC v8\|Stage IV Gallbladder Cancer AJCC v8\|Stage IV Intrahepatic Bile Duct Cancer AJCC v8\|Stage IVA Gallbladder Cancer AJCC v8\|Stage IVB Gallbladder Cancer AJCC v8	October 18, 2019	Phase 2
NCT03992456	Academic and Community Cancer Research United\|National Cancer Institute (NCI)	Metastatic Colon Adenocarcinoma\|Metastatic Colorectal Carcinoma\|Metastatic Rectal Adenocarcinoma\|Stage III Colon Cancer AJCC v8\|Stage III Colorectal Cancer AJCC v8\|Stage III Rectal Cancer AJCC v8\|Stage IIIA Colon Cancer AJCC v8\|Stage IIIA Colorectal Cancer AJCC v8\|Stage IIIA Rectal Cancer AJCC v8\|Stage IIIB Colon Cancer AJCC v8\|Stage IIIB Colorectal Cancer AJCC v8\|Stage IIIB Rectal Cancer AJCC v8\|Stage IIIC Colon Cancer AJCC v8\|Stage IIIC Colorectal Cancer AJCC v8\|Stage IIIC Rectal Cancer AJCC v8\|Stage IV Colon Cancer AJCC v8\|Stage IV Colorectal Cancer AJCC v8\|Stage IV Rectal Cancer AJCC v8\|Stage IVA Colon Cancer AJCC v8\|Stage IVA Colorectal Cancer AJCC v8\|Stage IVA Rectal Cancer AJCC v8\|Stage IVB Colon Cancer AJCC v8\|Stage IVB Colorectal Cancer AJCC v8\|Stage IVB Rectal Cancer AJCC v8\|Stage IVC Colon Cancer AJCC v8\|Stage IVC Colorectal Cancer AJCC v8\|Stage IVC Rectal Cancer AJCC v8\|Unresectable Colon Adenocarcinoma\|Unresectable Colorectal Carcinoma\|Unresectable Rectal Adenocarcinoma	April 24, 2020	Phase 2
NCT03981614	Academic and Community Cancer Research United\|National Cancer Institute (NCI)	Metastatic Colorectal Carcinoma\|Stage IV Colorectal Cancer AJCC v8\|Stage IVA Colorectal Cancer AJCC v8\|Stage IVB Colorectal Cancer AJCC v8\|Stage IVC Colorectal Cancer AJCC v8\|Unresectable Carcinoma	October 29, 2019	Phase 2
NCT05155124	Wuhan Union Hospital, China	Colorectal Neoplasms Malignant	September 2022	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

In Vitro:

H ₂ O : 50 mg/mL ( 179.13 mM ; Need ultrasonic)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

DMF : < 1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.5827 mL	17.9134 mL	35.8269 mL
5 mM	0.7165 mL	3.5827 mL	7.1654 mL
10 mM	0.3583 mL	1.7913 mL	3.5827 mL

* Please refer to the solubility information to select the appropriate solvent.

References

Synonyms

2,4(1H,3H)-Pyrimidinedione, 5-chloro-6-[(2-imino-1-pyrrolidinyl)methyl]-, hydrochloride (1:1)

2,4(1H,3H)-Pyrimidinedione, 5-chloro-6-[(2-imino-1-pyrrolidinyl)methyl]-, monohydrochloride

TPI hydrochloride

TAS 1-462

Tipiracil hydrochloride

5-Chloro-6-[(2-iminopyrrolidin-1-yl)methyl]pyrimidine-2,4(1H,3H)-dione hydrochloride