TIC10

Product Name: TIC10
CAS No.: 1616632-77-9
Chemical Name: TIC10
Synonyms: imipridone;TIC10;ONC201;CS-2579;ONC201,TIC10;dordaviprone;TIC-10 (ON201);TIC10(ONC-201);TIC 10 active isomer;TIC10 (imipridone, ONC201, NSC350625)
CBNumber: CB12711459
Molecular Formula: C24H26N4O
Formula Weight: 386.49
MOL File: 1616632-77-9.mol

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TIC10 Property

Boiling point:: 559.7±60.0 °C(Predicted)
Density: 1.24±0.1 g/cm3(Predicted)
storage temp.: Sealed in dry,Store in freezer, under -20°C
solubility: Soluble in DMSO (up to 25 mg/ml with warming).
pka: 6.38±0.20(Predicted)
form: solid
color: Pale yellow
Stability:: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.
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
InChIKey: VLULRUCCHYVXOH-UHFFFAOYSA-N
SMILES: C12=NCCN1C1CCN(CC3=CC=CC=C3)CC=1C(=O)N2CC1=CC=CC=C1C

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 16109
Product name: TIC10
Purity: ≥98%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 16109
Product name: TIC10
Purity: ≥98%
Packaging: 5mg
Price: $109
Updated: 2024/03/01

Cayman Chemical

Product number: 16109
Product name: TIC10
Purity: ≥98%
Packaging: 10mg
Price: $199
Updated: 2024/03/01

Cayman Chemical

Product number: 16109
Product name: TIC10
Purity: ≥98%
Packaging: 25mg
Price: $420
Updated: 2024/03/01

TRC

Product number: B285480
Product name: 7-Benzyl-4-(2-methylbenzyl)-1,2,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(4H)-one
Packaging: 50mg
Price: $160
Updated: 2021/12/16

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TIC10 Chemical Properties,Usage,Production

Description

TIC10 induces the expression of TNF-related apoptosis-inducing ligand (TRAIL) at 1-5 μM in a p53-independent manner. It is orally active, stable, and crosses the blood-brain barrier. The induction of TRAIL results from dual inhibition of Akt and ERK1/2 combined with nuclear translocation of the transcription factor FOXO3a. TIC10 suppresses the growth of orthotopic human glioblastoma multiforme tumors in mice.

Uses

7-Benzyl-4-(2-methylbenzyl)-1,2,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(4H)-one is used in biological studies for structure confirmation and pharmacophore reassignment for induction of immunosurveillance cytokine TRAIL in macrophages. The structure of this compound was misassigned for many years as H291055. The resolution of this issue was recently highlighted in Chemical and Engeneering News 92(23) 32 (2014).

Biological Activity

TIC10 (also named ONC21), a first-in-class small molecule inducer of TRAIL, has been developed. Preclinical studies have shown that it potently induces TRAIL expression. TIC10 treatment in cancer cells blocks Akt and Erk signalling to activate Foxo3a, which transcriptionally up-regulates the TRAIL gene. TIC10 has displayed ideal properties as a potential anti-cancer drug, including a broad spectrum of activity, wide safety margin, robust stability, aqueous solubility, favourable pharmacokinetics, and oral activity[5].

in vitro

TIC10/ONC201, a first-in-class small-molecule inducer of tumor necrosis (TNF)-related apoptosis-inducing ligand (TRAIL). The in vitro results showed that TIC10 induced potent cytotoxic and cytostatic activities in several human pancreatic cancer cell lines (Panc-1, Mia-PaCa2, AsPC-1 or L3.6). TIC10 activated both extrinsic (TRAIL-caspase-8-dependent) and endogenous/mitochondrial (caspase-9-dependent) apoptosis pathways in the pancreatic cancer cells. Molecularly, TIC10 inhibited Akt-Erk activation yet induced TRAIL expression in pancreatic cancer cells. Significantly, TIC10, at a relatively low concentration, sensitized gemcitabine-induced growth inhibition and apoptosis against pancreatic cancer cells. Further, TIC10 and gemcitabine synergistically inhibited Panc-1 xenograft growth in SCID mice. The combination treatment also significantly improved mice survival. In addition, Akt-Erk in-activation and TRAIL/cleaved-caspase-8 induction were observed in TIC10-treated Panc-1 xenografts[5].

References

1) Allen?et al.?(2013)?Dual Inactivation of Akt and ERK by TIC10 Signals Foxo3a Nuclear Translocation, TRAIL Gene Induction, and Potent Antitumor Effects, Sci. Transl. Med.?5?171ra17 2) Allen?et al.?(2015)?Identification of TRAIL-inducing compounds highlights small molecule ONC201/TIC10 as a unique anti-cancer agent that activates the TRAIL pathway,?Mol. Cancer.?14?99 3) Allen?et al.?(2016)?Discovery and Clinical Introduction of First-In-Class Imipridone ONC201, Oncotarget?7?74380 4) Ishizawa?et al.?(2019)?Mitochondrial ClpP-Mediated Proteolysis Induces Selective Cancer Cell Lethality, Cancer Cell?35?721
[6] Qiangbo Zhang . “The preclinical evaluation of TIC10/ONC201 as an anti-pancreatic cancer agent.” Biochemical and biophysical research communications 476 4 (2016): Pages 260-266.

TIC10 Preparation Products And Raw materials

Raw materials

Preparation Products

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TIC10 Suppliers

China 79 India 1 The Netherlands 1 United States 13 Global 94

Shanghai SuperLan Chemcial Technique Centre

Tel: 021-2022843681 15618226720
Fax: +86-21-51601218
Email: lucy@atkchemical.com
Country: China
ProdList: 9952
Advantage: 58

Shenzhen Yaoyuan R&D Center Co., Ltd

Tel: 13421666688 13421666688
Email: 664261110@qq.com
Country: China
ProdList: 410
Advantage: 58

Wuhan Topule

Tel: +86-02787215551 +86-19945035818
Fax: 027-87215551
Email: 2936752263@qq.com
Country: China
ProdList: 7977
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WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.

Tel: 17702719238 17702719238
Email: sales@sun-shinechem.com
Country: China
ProdList: 985
Advantage: 64

Xi‘an Deeptech Biotechnology Co.,LTD

Tel: +86-15114901355 +86-15114901355
Email: 15114901355@163.com
Country: China
ProdList: 189
Advantage: 58

Shanghai Chaolan Chemical Technology Center

Tel: 021-QQ：65489617 15618227136
Fax: 21-5161 9052
Email: Sales@ATKchemical.com
Country: China
ProdList: 7296
Advantage: 58

Haoyuan Chemexpress Co., Ltd.

Tel: 021-58950125
Fax: (86) 21-58955996
Email: info@chemexpress.com
Country: China
ProdList: 7552
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Suzhou yacoo science co.,Ltd

Tel: 0512-87182056 18013166090
Fax: 0512-87182056
Email: lingling.qi@yacoo.com.cn
Country: China
ProdList: 7295
Advantage: 60

AdooQ Bioscience CHINA

Tel: 025-58849295 18951903616;
Fax: 025-68650336
Email: info@adooq.cn
Country: China
ProdList: 2990
Advantage: 60

LETOPHARM LIMITED

Tel: +86-21-5821 5861
Fax: +86-21-5106 2861
Email: sales@letopharm.com
Country: China
ProdList: 2384
Advantage: 58

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View Lastest Price from TIC10 manufacturers

Zhejiang J&C Biological Technology Co.,Limited

Product: TIC10 1616632-77-9
Price: US $0.00/gram
Min. Order: 1gram
Purity: 99%
Supply Ability: 10kg
Release date: 2022-02-18

Career Henan Chemical Co

Product: 4-[5-methyl-4-[(4-methylphenyl)sulfonylmethyl]-1,3-oxazol-2-yl]-N-(pyridin-3-ylmethyl)benzamide 1616632-77-9
Price: US $1.00/KG
Min. Order: 1KG
Purity: Min98% HPLC
Supply Ability: g/kg/ton
Release date: 2020-01-01

1616632-77-9, TIC10Related Search:

Volasertib (BI 6727) NORFLUOXETINE HYDROCHLORIDE RESINIFERATOXIN Imiquimod Felodipine NYLON 6

ONC201,TIC10

TIC-10 (ON201)

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

imipridone

ONC201; ONC 201; ONC-201; NSC350625; NSC-350625; NSC 350625; TIC10; TIC 10; TIC-10; TRAIL INDUCING COMPOUND 10; IMIPRIDONE

TIC10(ONC-201)

TIC 10 active isomer

ONC201

7-Benzyl-4-(2-methylbenzyl)-1,2,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(4H)-on

(11-benzyl-7-[(2-methylphenyl)methyl]-2,5,7,11-tetraazatricyclo[7.4.0.02,6]trideca-1(9),5-dien-8-one)

CS-2579

Imidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1H)-one, 2,4,6,7,8,9-hexahydro-4-[(2-methylphenyl)methyl]-7-(phenylmethyl)-

TIC10

TIC10 (imipridone, ONC201, NSC350625)

dordaviprone

1616632-77-9

APL

APIS