TAS-102

• CAT Number: I013698
• CAS Number: 733030-01-8
• Molecular Formula: C₁₀H₁₁F₃N₂O₅ . ₁/₂C₉H₁₁ClN₄O₂ . ₁/₂HCl
• Molecular Weight: 435.76
• Purity: ≥95%
• Target: Nucleoside Antimetabolite/AnalogThymidylate Synthase
• Solubility: DMSO: 2.34 mg/mL (Need ultrasonic and warming)
• IUPAC Name: 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]-1H-pyrimidine-2,4-dione;1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)pyrimidine-2,4-dione;hydrochloride
• InChI: InChI=1S/2C10H11F3N2O5.C9H11ClN4O2.ClH/c2*11-10(12,13)4-2-15(9(19)14-8(4)18)7-1-5(17)6(3-16)20-7;10-7-5(12-9(16)13-8(7)15)4-14-3-1-2-6(14)11;/h2*2,5-7,16-17H,1,3H2,(H,14,18,19);11H,1-4H2,(H2,12,13,15,16);1H/t2*5-,6+,7+;;/m00../s1
• InChIKey: KTHXRTQHERFOMN-GIZOTSQLSA-N
• SMILES: C1CC(=N)N(C1)CC2=C(C(=O)NC(=O)N2)Cl.C1C(C(OC1N2C=C(C(=O)NC2=O)C(F)(F)F)CO)O.C1C(C(OC1N2C=C(C(=O)NC2=O)C(F)(F)F)CO)O.Cl

TAS-102 (Cat No.:I013698) is a combination drug that is taken orally and consists of two components: trifluridine, a thymidine nucleic acid analog, and tipiracil hydrochloride, a thymidine phosphatase inhibitor. This drug has been approved for the treatment of metastatic colorectal cancer that has not responded to standard therapies. The combination of trifluridine and tipiracil hydrochloride works by inhibiting DNA replication and promoting DNA damage, leading to the death of cancer cells. TAS-102 offers a new treatment option for patients with metastatic colorectal cancer.

Reference

[1]. Uboha N, et al. TAS-102: a novel antimetabolite for the 21st century. Future Oncol. 2016 Jan;12(2):153-63.[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 Mar;35(3):1437-45.[3]. Yamashita F, et al. Exposure-dependent incorporation of trifluridine into DNA of tumors and white blood cells in tumor-bearing mouse. Cancer Chemother Pharmacol. 2015 Aug;76(2):325-33.