SU 6668

• CAT Number: I002859
• CAS Number: 252916-29-3
• Molecular Formula: C₁₈H₁₈N₂O₃
• Molecular Weight: 310.35
• Purity: ≥95%
• Target: VEGFR
• Solubility: DMSO: ≥ 28 mg/mL
• Storage: 3 years -20℃ powder
• IC50: 8 nM (Ki) [1]
• IUPAC Name: 3-[2,4-dimethyl-5-[(Z)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid
• InChI: InChI=1S/C18H18N2O3/c1-10-12(7-8-17(21)22)11(2)19-16(10)9-14-13-5-3-4-6-15(13)20-18(14)23/h3-6,9,19H,7-8H2,1-2H3,(H,20,23)(H,21,22)/b14-9+
• InChIKey: NHFDRBXTEDBWCZ-NTEUORMPSA-N
• SMILES: CC1=C(NC(=C1CCC(=O)O)C)C=C2C3=CC=CC=C3NC2=O

TSU-68 (SU6668; Orantinib) (Cat.No:I002859) is a novel multiple receptor tyrosine kinase inhibitor with IC50 of 2.1 μM, 8 nM and 1.2 μM for VEGF-R1, PDGF-Rβ and FGF-R1, respectively; has greatest potency against PDGFR autophosphorylation.

Reference

1:Relaxing Effect of TSU-68, an Antiangiogenic Agent, on Mouse Airway Smooth Muscle. Tan H, Lei J, Xue L, Cai C, Liu QH, Shen J.Cell Physiol Biochem. 2017 Apr 27;41(6):2350-2362. doi: 10.1159/000475653. [Epub ahead of print] PMID: 28478457 Free Article2:Quality of life on TSU-68: Combination of docetaxel and TSU-68, an oral antiangiogenic agent, in patients with metastatic breast cancer previously treated with anthracycline. Sohn BS, Kim SB, Ahn JH, Jung KH, Kim J, Lee KS, Ro J, Im SA, Im YH, Song HS, Park HS, Chung HC.Asia Pac J Clin Oncol. 2017 Mar 16. doi: 10.1111/ajco.12681. [Epub ahead of print] PMID: 28303646 3:Circulating Plasma Biomarkers for TSU-68, an Oral Antiangiogenic Agent, in Patients with Metastatic Breast Cancer. Yoo C, Kim SB, Ro J, Im SA, Im YH, Kim JH, Ahn JH, Jung KH, Song HS, Kang SY, Park HS, Chung HC.Cancer Res Treat. 2016 Apr;48(2):499-507. doi: 10.4143/crt.2015.089. Epub 2015 Jul 14. PMID: 26194374 Free PMC Article4:TSU-68 ameliorates hepatocellular carcinoma growth by inhibiting microenvironmental platelet-derived growth factor signaling. Hara Y, Yamashita T, Oishi N, Nio K, Hayashi T, Nomura Y, Yoshida M, Hayashi T, Hashiba T, Asahina Y, Kondo M, Okada H, Sunagozaka H, Honda M, Kaneko S.Anticancer Res. 2015 Mar;35(3):1423-31. PMID: 25750293 5:Phase I study on the safety, pharmacokinetic profile, and efficacy of the combination of TSU-68, an oral antiangiogenic agent, and S-1 in patients with advanced hepatocellular carcinoma. Ikeda M, Shiina S, Nakachi K, Mitsunaga S, Shimizu S, Kojima Y, Ueno H, Morizane C, Kondo S, Sakamoto Y, Asaoka Y, Tateishi R, Koike K, Arioka H, Okusaka T.Invest New Drugs. 2014 Oct;32(5):928-36. doi: 10.1007/s10637-014-0109-2. Epub 2014 May 15. PMID: 24829073 Free PMC Article6:Combination of docetaxel and TSU-68, an oral antiangiogenic agent, in patients with metastatic breast cancer previously treated with anthracycline: randomized phase II multicenter trial. Kim SB, Yoo C, Ro J, Im SA, Im YH, Kim JH, Ahn JH, Jung KH, Song HS, Kang SY, Park HS, Chung HC.Invest New Drugs. 2014 Aug;32(4):753-61. doi: 10.1007/s10637-014-0093-6. Epub 2014 Apr 9. PMID: 24715580 7:A phase II open-label randomized multicenter trial of TSU-68 in combination with S-1 and oxaliplatin versus S-1 in combination with oxaliplatin in patients with metastatic colorectal cancer. Lee J, Shin SJ, Chung IJ, Kim TW, Chun HG, Shin DB, Kim YH, Song HS, Han SW, Kim JG, Kim SY, Choi YJ, Chung HC.Invest New Drugs. 2014 Jun;32(3):561-8. doi: 10.1007/s10637-014-0075-8. Epub 2014 Feb 27. PMID: 24573743 8:Randomised phase II study of S-1/cisplatin plus TSU-68 vs S-1/cisplatin in patients with advanced gastric cancer. Koizumi W, Yamaguchi K, Hosaka H, Takinishi Y, Nakayama N, Hara T, Muro K, Baba H, Sasaki Y, Nishina T, Fuse N, Esaki T, Takagi M, Gotoh M, Sasaki T.Br J Cancer. 2013 Oct 15;109(8):2079-86. doi: 10.1038/bjc.2013.555. Epub 2013 Sep 17. Erratum in: Br J Cancer. 2014 Dec 9;111(12):2382. PMID: 24045669 Free PMC Article9:A randomised phase II study of TSU-68 in patients with hepatocellular carcinoma treated by transarterial chemoembolisation. Inaba Y, Kanai F, Aramaki T, Yamamoto T, Tanaka T, Yamakado K, Kaneko S, Kudo M, Imanaka K, Kora S, Nishida N, Kawai N, Seki H, Matsui O, Arioka H, Arai Y.Eur J Cancer. 2013 Sep;49(13):2832-40. doi: 10.1016/j.ejca.2013.05.011. Epub 2013 Jun 10. PMID: 23764238 10:A multicenter phase II study of TSU-68, a novel oral multiple tyrosine kinase inhibitor, in patients with metastatic breast cancer progressing despite prior treatment with an anthracycline-containing regimen and taxane. Suzuki Y, Saeki T, Aogi K, Toi M, Fujii H, Inoue K, Watanabe T, Fujiwara Y, Ito Y, Takatsuka Y, Iwata H, Arioka H, Tokuda Y.Int J Clin Oncol. 2013 Aug;18(4):590-7. doi: 10.1007/s10147-012-0421-9. Epub 2012 May 15. PMID: 22585426