TIC10 isomer

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抑制剂描述：

产品名称：TIC10 isomer

产品别名：见爱必信官网

英文别名：TIC10 isomer

靶点：Akt

CAS：41276-02-2

纯度：>98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

TIC10抑制Akt和ERK活性，通过FoxO3a诱导TRAIL，具有优越的耐药性，可以穿透血脑屏障，具有超强的稳定性，和改善的药代动力学。TIC10导致TRAIL mRNA增加，这种作用存在剂量依赖性，诱导TRAIL蛋白按p53非依赖性的方式定位在一些肿瘤细胞系的细胞表面。TIC10在体外对多种恶性肿瘤具有广谱活性，并诱导sub-G1 DNA含量增加，说明TRAIL敏感的HCT116 p53^?/?细胞发生细胞死亡，但是按同等剂量处理正常的成纤维细胞，不改变细胞周期谱。TIC10降低了肿瘤细胞系的克隆存活。

溶解性：DMSO ：9 mg/mL (23.3 mM)

体外研究：

TIC10 causes a dose-dependent increase in TRAIL mRNA and induces TRAIL protein localization on the cell surface of several cancer cell lines in a p53-independent manner. TIC10 has broad-spectrum activity against multiple malignancies in vitro and induces an increase in sub-G1 DNA content suggestive of cell death in TRAIL-sensitive HCT116 p53?/? cells, but does not alter the cell cycle profiles of normal fibroblasts at equivalent doses. TIC10 decreases the clonogenic survival of cancer cell lines and spares normal fibroblasts. TIC10 increases the percentage of sub-G1 DNA in cancer cells in a p53-independent and Bax-dependent manner, as previously reported for TRAIL-mediated apoptosis. TIC10-induced TRAIL up-regulation is Foxo3a-dependent, which also up-regulates TRAIL death receptor DR5 among other targets, potentially allowing for sensitization of some TRAIL-resistant tumor cells. 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.

体内研究：TIC10 and TRAIL treatment causes tumor regression in the HCT116 p53?/? xenograft to a comparable extent when both are administered as multiple doses. TIC10 also induces regression of MDA-MB-231 human triple-negative breast cancer xenografts, whereas TRAIL-treated tumors progressed. In DLD-1 colon cancer xenografts, TIC10 induces tumor stasis at 1 week after treatment, whereas TRAIL-treated tumors progresses 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. TIC10 causes tumor-specific cell death by TRAIL-mediated direct and bystander effects. TIC10 is an effective antitumor agent against orthotopic human glioblastoma multiforme tumors.

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