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733030-01-8 (TAS-102)

1

Identification

TAS-102 TAS-102
Name TAS-102
Formula C20H28Cl2F3N7O6
MW 590.38
CAS No. 733030-01-8
EINECS
Smiles O=C1N([[email protected]]2C[[email protected]](O)[[email protected]@H](CO)O2)C=C(C(F)(F)F)C(N1)=O.O=C3NC(CN4CCCC4=N)=C(Cl)C(C3)=N.N.Cl
Synonyms 1-((2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-(trifluoromethyl)pyrimidine-2,4(1H,3H)-dione compound with 5-chloro-4-imino-6-((2-iminopyrrolidin-1-yl)methyl)-3,4-dihydropyridin-2(1H)-one and ammonia (1:1:1) hydrochloride
InChI InChI=1S/C10H13ClN4O.C10H11F3N2O5.ClH.H3N/c11-10-6(12)4-9(16)14-7(10)5-15-3-1-2-8(15)13;11-10(12,13)4-2-15(9(19)14-8(4)18)7-1-5(17)6(3-16)20-7;;/h12-13H,1-5H2,(H,14,16);2,5-7,16-17H,1,3H2,(H,14,18,19);1H;1H3/t;5-,6+,7+;;/m.0../s1
2

Introduction

TAS-102 is an orally administered combination of a thymidine-based nucleic acid analogue, trifluridine, and a thymidine phosphorylase inhibitor, tipiracil hydrochloride.

Background Information

TAS-102 is an orally bioavailable combination agent composed of the cytotoxic pyrimidine analog Trifluridine (5-trifluoro-2??-deoxythymidine or TFT) and a thymidine phosphorylase inhibitor (TPI) tipiracil hydrochloride, in a molar ratio of 1.0:0.5 (TFT:TPI), with potential antineoplastic activity, ......by AdooQ BioScience, LLC
TAS-102 is an orally bioavailable combination agent composed of the cytotoxic pyrimidine analog Trifluridine (5-trifluoro-2’-deoxythymidine or TFT) and a thymidine phosphorylase inhibitor (TPI) tipiracil hydrochloride, in a molar ratio of 1.0:0.5 (TFT:TPI ......by BOC Sciences
TAS-102 is a novel oral combination drug that consists of an antineoplastic thymidine-based nucleoside analog, trifluorothymidine, and a potent thymidine phosphorylase inhibitor, tipiracil, in a 1:0.5 molar ratio. ......by MedChemexpress Co., Ltd.
TAS-102 is an investigational drug candidate for metastatic colorectal cancer. It contains trifluridine (TFT) and Tipiracil hydrochloride (TTP) in a molar ratio of 1;0.5. Trifluridine is a nucleoside analog, and tipiracil hydrochloride is a thymidine phosphorylase inhibitor, which prevents rapid metabolism of trifluiridine, increasing the bioavailability of trifluiridine. After oral administration of TAS-102, TFT is phosphorylated to the active monophosphate form TF-TMP, which binds covalently to the active site of thymidylate synthase, thereby reducing the nucleotide pool levels required for DNA replication. Furthermore, the triphosphate form TF-TTP can be incorporated into DNA, which induces DNA fragmentation and leads to the inhibition of tumor growth. TPI exhibits a dual effect: 1) an anti-angiogenic effect mediated through the inhibition of thymidine phosphorylase, which plays an important role in nucleotide metabolism and a variety of development processes, including angiogenesis, 2) increased bioavailability of the normally short-lived antimetabolite TFT by preventing its degradation into the inactive form trifluorothymine (TF-Thy). The synergistic effect of the components in TAS-102 may demonstrate antitumor activity in 5-FU-resistant cancer cells. ......by MedKoo Biosciences, Inc.
TAS-102 is an orally administered combination of a thymidine-based nucleic acid analogue, trifluridine, and a thymidine phosphorylase inhibitor, tipiracil hydrochloride. ......by Selleck Chemicals LLC
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance: EBNumber:EB000018544

Storage condition

Solubility

DMSO: 2.34 mg/mL (Need ultrasonic and warming) by CHEMSCENE, LLC
DMSO: 2.34 mg/mL (Need ultrasonic and warming) by MedChemexpress Co., Ltd.
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Mechanism and Indication

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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
TAS-102 Takeda Colorectal Cancer 2015/11/1 Phase 1|Phase 2
TAS-102 Georgetown University Metastatic Colorectal Cancer 2016/2/1 Phase 2
TAS-102 Taiho Oncology, Inc. Refractory Metastatic Colorectal Cancer 2016/8/1 Phase 2
TAS-102 University of Florida|Taiho Oncology, Inc. Squamous Cell Lung Carcinoma 2017/6/30 Phase 2
TAS-102 University of Florida|Taiho Oncology, Inc. Pancreatic Cancer 2017/7/1 Phase 2
TAS-102 Taiho Oncology, Inc. Advanced Solid Tumors 2015/1/1 Phase 1
TAS-102 Taiho Oncology, Inc. Refractory Metastatic Gastric Cancer 2015/12/1 Phase 3
TAS-102 University of Wisconsin, Madison|National Cancer Institute (NCI)|Taiho Pharmaceutical Co., Ltd. Neuroendocrine Tumors|Neoplasms|Cancer|Tumors 2016/11/1 Phase 1
TAS-102 Taiho Oncology, Inc. Advanced Solid Tumors (Excluding Breast Cancer) 2013/7/1 Phase 1
TAS-102 Taiho Pharmaceutical Co., Ltd. Advanced or Metastatic Solid Tumors 2014/9/1 Phase 1
TAS-102 Taiho Oncology, Inc. Advanced Solid Tumors 2015/1/1 Phase 1
TAS-102 Taiho Oncology, Inc. Advanced Solid Tumors 2014/2/1 Phase 1
TAS-102 Taiho Oncology, Inc. Advanced Solid Tumors (Excluding Breast Cancer) 2013/6/1 Phase 1
TAS-102 Sidney Kimmel Comprehensive Cancer Center Previously Treated Metastatic Colorectal Cancer 2013/9/1 Phase 1|Phase 2
TAS-102 Taiho Oncology, Inc. Advanced Gastrointestinal Tumors 2013/9/1 Phase 1
TAS-102 Taiho Oncology, Inc. Colorectal Cancer 2012/6/1 Phase 3
TAS-102 Taiho Oncology, Inc. Advanced Solid Tumors 2013/6/1 Phase 1
TAS-102 Taiho Pharmaceutical Co., Ltd. Colorectal Cancer 2013/9/1 Phase 3
TAS-102 Taiho Oncology, Inc. Colorectal Cancer Metastatic
TAS-102 University of California, San Francisco Colon Cancer|Rectal Cancer|Liver Metastases 2016/10/1 Phase 1
TAS-102 Yale University Colorectal Neoplasms 2016/8/1 Phase 1|Phase 2
TAS-102 Taiho Oncology, Inc.|Taiho Pharmaceutical Co., Ltd. Small Cell Lung Cancer (SCLC) 2013/7/1 Phase 2
TAS-102 - Launched
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Safety Data of TAS-102

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
AdooQ BioScience, LLC USA
BOC Sciences
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD90();10mg/USD150() USA
MedChemexpress Co., Ltd. 5mg/USD90();10mg/USD150() USA
MedKoo Biosciences, Inc. USA
Selleck Chemicals LLC USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD90();10mg/USD150() China
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Related Products

Other Forms of 733030-01-8

Name CAS No Formula MW

Recommended Compounds in Thymidylate Synthase Nucleoside Antimetabolite/Analog

Name CAS No Formula MW
Trifluorothymidine 70-00-8 C10H11F3N2O5 296.2
Raltitrexed 112887-68-0 C21H22N4O6S 458.49
Tipiracil 183204-74-2 C9H11ClN4O2 242.66
TAS-102 733030-01-8 C10H11F3N2O5 . 1/2C9H11ClN4O2 . 1/2HCl 435.76
5-BrdU 59-14-3 C9H11BrN2O5 307.1
Vidarabine 5536-17-4 C10H13N5O4 267.24
Adenosine 58-61-7 C10H13N5O4 267.24
Carmofur 61422-45-5 C11H16FN3O3 257.26
Cytidine 65-46-3 C9H13N3O5 243.22
Merimepodib 198821-22-6 C23H24N4O6 452.46
Floxuridine 50-91-9 C9H11FN2O5 246.19
Dacarbazine 4342-03-4 C6H10N6O 182.18
Tipiracil (hydrochloride) 183204-72-0 C9H12Cl2N4O2 279.12
Orotic acid 65-86-1 C5H4N2O4 156.1
Nelarabine 121032-29-9 C11H15N5O5 297.27
6-Mercaptopurine 50-44-2 C5H4N4S 152.18
LY2334737 892128-60-8 C17H25F2N3O5 389.39
Cytarabine (hydrochloride) 69-74-9 C9H14ClN3O5 279.68
Cytarabine 147-94-4 C9H13N3O5 243.22
Gemcitabine (elaidate) 210829-30-4 C27H43F2N3O5 527.6442

Recommended Compounds in Same Indication

Name CAS No Formula MW
Regorafenib 755037-03-7 C21H15ClF4N4O3 482.82
Regorafenib (Hydrochloride) 835621-07-3 C21H16Cl2F4N4O3 519.28
Tivantinib 905854-02-6 C23H19N3O2 369.42
Fruquintinib 1194506-26-7 C21H19N3O5 393.39
Dovitinib 405169-16-6 C21H21FN6O 392.43
Sunitinib 557795-19-4 C22H27FN4O2 398.47
Brivanib (alaninate) 649735-63-7 C22H24FN5O4 441.46
Dasatinib (hydrochloride) 854001-07-3 C22H27Cl2N7O2S 524.47
RO4929097 847925-91-1 C22H20F5N3O3 469.4
5-Fluorouracil 51-21-8 C4H3FN2O2 130.08
Oxaliplatin 61825-94-3 C8H14N2O4Pt 397.29
Exatecan 171335-80-1 C24H22FN3O4 435.45
Exatecan (Mesylate) 169869-90-3 C25H26FN3O7S 531.55
Napabucasin 83280-65-3 C14H8O4 240.2109
Andrographolide 5508-58-7 C20H30O5 350.45
SU5416 204005-46-9 C15H14N2O 238.28
Cediranib 288383-20-0 C25H27FN4O3 450.51
BYL-719 1217486-61-7 C19H22F3N5O2S 441.47
Apatinib 1218779-75-9 C25H27N5O4S 493.58
AS703026 1236699-92-5 C15H15FIN3O3 431.2
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Route of Synthesis

12

References

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More Information

TAS-102

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