TIC10 ( ONC201 )
TIC10 ( ONC201 ), Bulk in stock, contact us by email for detailed quotation.
ONC201/TIC10 is a novel small molecule inducer of the human TRAIL gene that improves efficacy-limiting properties of recombinant TRAIL and is in clinical trials in advanced cancers based on its promising safety and antitumor efficacy in several preclinical models. ONC201/TIC10 can cross the blood-brain barrier.
For research use only. We do not sell to patients.
Chemical Information
| Name | TIC10 ( ONC201 ) |
|---|---|
| Iupac Chemical Name | 7-benzyl-4-(2-methylbenzyl)-2,4,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1H)-one |
| Synonyms | ONC201 ; ONC 201 ; ONC-201 ; NSC350625 ; NSC-350625 ; NSC 350625 ; TIC10 ; TIC 10 ; TIC-10 ; |
| Molecular Formula | C24H26N4O |
| Molecular Weight | 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 Number | 1616632-77-9 |
| Related CAS | 1616632-77-9 (free base) 1638178-82-1 (HCl) |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Off-white to Light-yellow solid |
|---|---|
| Purity | 99.85% |
| Storage | Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years). |
| Solubility | 2mg/ml in DMSO |
| Handling | Refer to MSDS |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code | 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.
Chemical Structure
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