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TIC10 ( ONC201 )

Catalog No.: 51802
Cas No.: 1616632-77-9
Purity : 98% 

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。

For research use only. We do not sell to patients.

Chemical Information

名称TIC10 ( ONC201 )
Iupac 化学名称2,4,6,7,8,9-hexahydro-4-((2-methylphenyl)methyl)-7-(phenylmethyl)imidazo(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 
SmileCC1=C(C=CC=C1)CN1C=2N(C3=C(C1=O)CN(CC3)CC3=CC=CC=C3)CCN2
InChiKeyVLULRUCCHYVXOH-UHFFFAOYSA-N
InChiInChI=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
Related CAS1616632-77-9 (free base) 1638178-82-1 (HCl)

Ordering Information

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Formulation类白色至浅黄色固体
纯度98% 
存储3 years -20ºCpowder 6 months-80ºCin solvent 
可溶性可溶解于DMSO
Handling
运输条件Shipped under ambient temperature 
HS Code
TargetsAkt and ERK inhibitor
MechanismTIC10 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.


化学结构

51802 - TIC10 ( ONC201 ) | CAS 1616632-77-9

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