2. PI3K/Akt/mTOR Autophagy
  3. mTOR Autophagy
  4. CC214-2

CC214-2 是一种口服有效的 mTOR 激酶抑制剂。CC214-2 靶向 mTORC1 (pS6) 和 mTORC2 (pAktS473)。CC214-2 诱导自噬，自噬即是结核病宿主定向治疗 (HDT) 的潜在靶点。CC214-2 对结核病 (TB) 表现出协同抑菌和杀菌活性，并能够缩短产生效力的时间。CC214-2 还抑制雷帕霉素 (HY-10219) 耐药信号，并在体外和体内抑制胶质母细胞瘤的生长。

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CC214-2 Chemical Structure

CC214-2 Chemical Structure

CAS No. : 1228012-18-7

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CC214-2 相关抗体

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mTOR mTORC1 mTORC2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CC214-2 is an oral active and selective mTOR kinase inhibitor. CC214-2 targets to both of mTORC1 (pS6) and mTORC2 (pAktS473). CC214-2 induces autophagy, which is a potential target for host-directed therapy (HDT) in tuberculosis. CC214-2 exhibits synergistic bactericidal and sterilizing activity agasinst tuberculosis (TB), and shortens the treatment duration. CC214-2 also inhibits Rapamycin (HY-10219)-resistant signaling and the growth of glioblastomas in vitro and in vivo[1][2].

IC50 & Target[1][2]

mTORC1

 

mTORC2

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
PC-3 IC50
0.315 μM
Compound: 10b, CC214-2
Inhibition of mTORC2 in human PC3 cells assessed as inhibition of AKTS473 phosphorylation after 1 hr by sandwich immunoassay
Inhibition of mTORC2 in human PC3 cells assessed as inhibition of AKTS473 phosphorylation after 1 hr by sandwich immunoassay
[PMID: 23414803]
PC-3 IC50
0.32 μM
Compound: 26, CC214-2
Inhibition of mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S473 after 1 hr
Inhibition of mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S473 after 1 hr
[PMID: 26083478]
PC-3 IC50
0.386 μM
Compound: 10b, CC214-2
Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr by sandwich immunoassay
Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr by sandwich immunoassay
[PMID: 23414803]
PC-3 IC50
0.39 μM
Compound: 26, CC214-2
Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr
Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr
[PMID: 26083478]
PC-3 IC50
1.55 μM
Compound: 10b, CC214-2
Cytotoxicity against human PC3 cells assessed as growth inhibition after 3 days by WST1 assay
Cytotoxicity against human PC3 cells assessed as growth inhibition after 3 days by WST1 assay
[PMID: 23414803]
体内研究
(In Vivo)

CC214-2 (25 mg/kg，50 mg/kg；口服；每天一次，持续 21 天) 导致 PC3 肿瘤异种移植模型中的肿瘤体积减小[1]。
CC214-2 (30 mg/kg，100 mg/kg；口服；单次剂量) 在体内分别抑制 mTORC1 (pS6) 和 mTORC2 (pAktS473) 至少 8 小时和 24 小时[1]。
CC214-2 (30 毫克/千克；口服) 减少结核杆菌 CFU 数量和预防慢性结核感染小鼠的死亡率[1]。
CC214-2 (50 mg/kg；口服；每天一次，持续 6 天) 显着降低小鼠 U87EGFRvIII 侧腹异种移植物的生长[2]。
CC214-2 (100 mg/kg；口服；每 2 天一次，持续 6 天) 抑制颅内胶质母细胞瘤模型中的 mTORC1 和 mTORC2 信号传导[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: U87EGFRvIII flank xenografts in mice[2]
Dosage: 50 mg/kg
Administration: PO; once daily for 6 days
Result: Inhibited tumor growth.
Similarly activated autophagy in U87EGFRvIII xenografts.
分子量

383.44

Formula

C20H25N5O3
CAS 号
性状

固体

颜色

Light yellow to light brown

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料

纯度: 98.41%

COA (285 KB) HNMR (259 KB) LCMS (268 KB)

产品使用指南 (1538 KB)
参考文献

CC214-2 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CC214-21228012-18-7mTORAutophagyMammalian target of RapamycinmTORC1mTORC2Mycobacterium tuberculosisautophagyTBInhibitorinhibitorinhibit

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目录号：
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