Orantinib (SU6668;TSU-68) 是一种多靶点受体酪氨酸激酶抑制剂，可有效抑制PDGFR自磷酸化及Flk-1与FGFR1的反式磷酸化，而对IGF-1R、Met、Src、Lck、Zap70、Abl、CDK2及EGFR无明显抑制活性，目前已进入三期临床试验。
| 英文别名 (English Synonym) | TSU-68 (SU6668, Orantinib) |
| 中文名称 (Chinese Name) | |
| 靶点 (Target) | VEGFR |
| 通路 (Pathway) | Protein Tyrosine Kinase |
| CAS号 (CAS NO.) | 252916-29-3 |
| 分子式 (Formula) | C18H18N2O3 |
| 分子量 (Molecular Weight) | 310.35 |
| 纯度 (Purity) | ≥98% |
| 溶解性 (Solubility) | 溶于DMSO |
-25~-15℃保存，有效期3年
[1] Laird AD, Vajkoczy P, Shawver LK, Thurnher A, Liang C, Mohammadi M, Schlessinger J, Ullrich A, Hubbard SR, Blake RA, Fong TA, Strawn LM, Sun L, Tang C, Hawtin R, Tang F, Shenoy N, Hirth KP, McMahon G, Cherrington. SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Res. 2000 Aug 1;60(15):4152-60. PMID: 10945623.[2]Smolich BD, Yuen HA, West KA, Giles FJ, Albitar M, Cherrington JM. The antiangiogenic protein kinase inhibitors SU5416 and SU6668 inhibit the SCF receptor (c-kit) in a human myeloid leukemia cell line and in acute myeloid leukemia blasts. Blood. 2001 Mar 1;97(5):1413-21. doi: 10.1182/blood.v97.5.1413. PMID: 11222388.[3]Marzola P, Degrassi A, Calderan L, Farace P, Crescimanno C, Nicolato E, Giusti A, Pesenti E, Terron A, Sbarbati A, Abrams T, Murray L, Osculati F. In vivo assessment of antiangiogenic activity of SU6668 in an experimental colon carcinoma model. Clin Cancer Res. 2004 Jan 15;10(2):739-50. doi: 10.1158/1078-0432.ccr-0828-03. PMID: 14760097.[4]Kim HC, Chung JW, Choi SH, Im SA, Yamasaki Y, Jun S, Jae HJ, Park JH. Augmentation of chemotherapeutic infusion effect by TSU-68, an oral targeted antiangiogenic agent, in a rabbit VX2 liver tumor model. Cardiovasc Intervent Radiol. 2012 Feb;35(1):168-75. doi: 10.1007/s00270-010-0081-y. Epub 2010 Dec 24. PMID: 21184227.
