CAS NO: | 1616632-77-9 |
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 |
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] |
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体外研究 (In Vitro) | TIC10 transcriptionally induces TRAIL in a p53-independent manner and crosses the blood-brain barrier[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 |
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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
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