TIC10 ( ONC201 )
ONC201 / TIC10是人类TRAIL基因的新型小分子诱导剂，可改善重组TRAIL的功效限制特性，并基于其在若干临床前模型中的有希望的安全性和抗肿瘤功效，正在进行晚期癌症的临床试验。
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | TIC10 ( ONC201 ) |
|---|---|
| Iupac 化学名称 | 7-benzyl-4-(2-methylbenzyl)-2,4,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1H)-one |
| 同义词 | ONC201 ; ONC 201 ; ONC-201 ; NSC350625 ; NSC-350625 ; NSC 350625 ; TIC10 ; TIC 10 ; TIC-10 ; |
| 英文同义词 | ONC201 ; ONC 201 ; ONC-201 ; NSC350625 ; NSC-350625 ; NSC 350625 ; TIC10 ; TIC 10 ; TIC-10 ; |
| 分子式 | C24H26N4O |
| 分子量 | 386.49 |
| Smile | CC1=C(C=CC=C1)CN1C=2N(C3=C(C1=O)CN(CC3)CC3=CC=CC=C3)CCN2 |
| InChiKey | VLULRUCCHYVXOH-UHFFFAOYSA-N |
| InChi | InChI=1S/C24H26N4O/c1-18-7-5-6-10-20(18)16-28-23(29)21-17-26(15-19-8-3-2-4-9-19)13-11-22(21)27-14-12-25-24(27)28/h2-10H,11-17H2,1H3 |
| Cas号 | 1616632-77-9 |
| 相关CAS号 | 1616632-77-9 (free base) 1638178-82-1 (HCl) |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 类白色至浅黄色固体 |
|---|---|
| 纯度 | 99.85% |
| 存储 | 0-4℃，可保存几天到几周；-20℃，可保存 几个月。 |
| 可溶性 | 可溶解于DMSO |
| 处理方式 | Refer to MSDS |
| 运输条件 | 可以在室温下进行运输。 |
| 海关编码 | 2934200090 |
| Targets | Akt and ERK inhibitor |
|---|---|
| Mechanism | TIC10 is a potent, orally active, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer which acts by inhibiting Akt and ERK, consequently activating Foxo3a and significantly inducing cell surface TRAIL. TIC10 can cross the blood-brain barrier. |
| Cell study | |
| Animal study | |
| Clinical study |
1: Fang Z, Wang J, Clark LH, Sun W, Yin Y, Kong W, Pierce SR, West L, Sullivan SA, Tran AQ, Prabhu VV, Zhou C, Bae-Jump V. ONC201 demonstrates anti-tumorigenic and anti-metastatic activity in uterine serous carcinoma in vitro. Am J Cancer Res. 2018 Aug 1;8(8):1551-1563. eCollection 2018. PubMed PMID: 30210923; PubMed Central PMCID: PMC6129479.
2: Bárány P, Oláh RS, Kovács I, Czuczi T, Szabó CL, Takács A, Lajkó E, Láng O, Kőhidai L, Schlosser G, Bősze S, Mező G, Hudecz F, Csámpai A. Ferrocene-Containing Impiridone (ONC201) Hybrids: Synthesis, DFT Modelling, In Vitro Evaluation, and Structure⁻Activity Relationships. Molecules. 2018 Sep 3;23(9). pii: E2248. doi: 10.3390/molecules23092248. PubMed PMID: 30177664.
3: Ralff MD, Lulla AR, Wagner J, El-Deiry WS. ONC201: a new treatment option being tested clinically for recurrent glioblastoma. Transl Cancer Res. 2017 Oct;6(Suppl 7):S1239-S1243. doi: 10.21037/tcr.2017.10.03. PubMed PMID: 30175049; PubMed Central PMCID: PMC6117120.
4: Karpel-Massler G, Siegelin MD. TIC10/ONC201-a potential therapeutic in glioblastoma. Transl Cancer Res. 2017 Dec;6(Suppl 9):S1439-S1440. doi: 10.21037/tcr.2017.10.51. PubMed PMID: 30148071; PubMed Central PMCID: PMC6108585.
5: Chari A, Barlogie B. Imipridone ONC201: combination therapy in hematologic malignancies. Cell Cycle. 2018;17(16):1947-1948. doi: 10.1080/15384101.2018.1490861. Epub 2018 Sep 11. PubMed PMID: 29929441; PubMed Central PMCID: PMC6224273.
6: Romaguera JE, Lee HJ, Tarapore R, Prabhu V, Allen J, Schalop L, Zloza A, Ok CY, Sadimin ET, Schenkel J, Badillo M, Wang M. Integrated stress response and immune cell infiltration in an -refractory mantle cell lymphoma patient following ONC201 treatment. Br J Haematol. 2018 May 8. doi: 10.1111/bjh.15271. [Epub ahead of print] PubMed PMID: 29740811.
7: Greer YE, Porat-Shliom N, Nagashima K, Stuelten C, Crooks D, Koparde VN, Gilbert SF, Islam C, Ubaldini A, Ji Y, Gattinoni L, Soheilian F, Wang X, Hafner M, Shetty J, Tran B, Jailwala P, Cam M, Lang M, Voeller D, Reinhold WC, Rajapakse V, Pommier Y, Weigert R, Linehan WM, Lipkowitz S. ONC201 kills breast cancer cells in vitro by targeting mitochondria. Oncotarget. 2018 Apr 6;9(26):18454-18479. doi: 10.18632/oncotarget.24862. eCollection 2018 Apr 6. PubMed PMID: 29719618; PubMed Central PMCID: PMC5915085.
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