Cofttek holdings limited

Akt &GSK-3

TIC10 (1616632-77-9)

TIC10 (ONC-201) is a potent, orally active, and stable small molecule that transcriptionally induces TRAIL in a p53-independent manner and crosses the blood-brain barrier.

Not Intended for Therapeutic Use. For research use only.

CAS: 1616632-77-9 Category

TIC10 (1616632-77-9) Description:

ONC-201, also known as TIC10 and imipridone, is a potent, orally active, and stable small molecule that transcriptionally induces TRAIL in a p53-independent manner and crosses the blood-brain barrier. TIC10 induces a sustained up-regulation of TRAIL in tumors and normal cells that may contribute to the demonstrable antitumor activity of TIC10. TIC10 inactivates kinases Akt and extracellular signal-regulated kinase (ERK), leading to the translocation of Foxo3a into the nucleus, where it binds to the TRAIL promoter to up-regulate gene transcription. TIC10 is an efficacious antitumor therapeutic agent that acts on tumor cells and their microenvironment to enhance the concentrations of the endogenous tumor suppressor TRAIL.

TIC10 (1616632-77-9) Specifications:

Product Name TIC10
Synonym ONC201; ONC 201; ONC-201; NSC350625; NSC-350625; NSC 350625; TIC10; TIC 10; TIC-10; TRAIL inducing compound 10; imipridone
Chemical Name 7-benzyl-4-(2-methylbenzyl)-1,2,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(4H)-one
Drug Class Antineoplastics
Purity ≥98% (HPLC)
CAS Number 1616632-77-9
Molecular Formula C24H26N4O
Molecular Weight 386.48944
Monoisotopic Mass 386.21066 g/mol
MDL number MFCD28118993
InChIKey VLULRUCCHYVXOH-UHFFFAOYSA-N
InChi Code 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,11-17H2,1H33-12,17-21H,2,13-16H2,1H3
SMILES O=C1N(CC2=CC=CC=C2C)C3=NCCN3C4=C1CN(CC5=CC=CC=C5)CC4
Form Powder
Color White to off-white
Solubility  Soluble in DMSO, not soluble in water
Storage Temp.  0 – 4 C for short term (days to weeks), or -20 C for long term (months)
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application TIC10(ONC-201) is a potent, orally active, and stable small molecule

 


=

RIDADR NONH for all modes of transport

References:

[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.

1 review for TIC10 (1616632-77-9)

  1. Cofttek

    Never had such good experience before,The TIC10 (1616632-77-9) is high purity,also customer service is pretty nice !gotta try!!

Add a review

Your email address will not be published. Required fields are marked *