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TIC10
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TIC10图片
CAS NO:1616632-77-9
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议
1 g电议

产品名称
ONC-201
产品介绍
TIC10 (ONC-201) 是一种有效,有口服活性,稳定的肿瘤坏死因子相关的凋亡诱导配体TRAIL诱导剂,其通过抑制AktERK起作用,从而激活 Foxo3a 并显着诱导细胞表面 TRAIL。TIC10 可透过血脑屏障。
生物活性

TIC10 (ONC-201) is a potent, orally active, and stable tumor necrosis factor-related apoptosis-inducing ligand(TRAIL)inducer which acts by inhibitingAktandERK, consequently activating Foxo3a and significantly inducing cell surface TRAIL. TIC10 can cross the blood-brain barrier[1].

IC50& Target[1]

TRAIL

 

体外研究
(In Vitro)

TIC10 transcriptionally induces TRAIL in a p53-independent manner and crosses the blood-brain barrier[1].
TIC10 induces a sustained up-regulation of TRAIL in tumors and normal cells that may contribute to the demonstrable antitumor activity of TIC10[1].
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[1].
TIC10 is an efficacious antitumor therapeutic agent that acts on tumor cells and their micro-environment to enhance the concentrations of the endogenous tumor suppressor TRAIL[1].
TIC10 also causes a down-regulation of the total expression of ERK[1].

体内研究
(In Vivo)

In DLD-1 colon cancer xenografts, TIC10 induces tumor stasis at 1 week after treatment, whereas TRAIL-treated tumors progress after a single dose. A single dose of TIC10 also induces a sustained regression of the SW480 xenograft and is equally effective when delivered by intraperitoneal or oral route, suggesting favorable oral bioavailability for TIC10. Titration of a single oral dose of TIC10 in the HCT116 xenograft model reveals sustained antitumor efficacy at 25 mg/kg. Exposure to oral TIC10 at 25 mg/kg weekly for 4 weeks in immunocompetent mice does not cause any changes in selected serum chemistry markers. The same oral dosing schedule is applied to Eμ-myc transgenic mice, which spontaneously develop meta-static lymphoma from weeks 9 to 12 of age, and TIC10 significantly (P=0.00789) prolongs the survival of these mice by 4 weeks[1].

Clinical Trial
分子量

386.49

性状

Solid

Formula

C24H26N4O

CAS 号

1616632-77-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 9.38 mg/mL(24.27 mM;ultrasonic and warming and heat to 60℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5874 mL12.9369 mL25.8739 mL
5 mM0.5175 mL2.5874 mL5.1748 mL
10 mM0.2587 mL1.2937 mL2.5874 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。