2. PI3K/Akt/mTOR
  3. PI3K mTOR
  4. PI3K/mTOR Inhibitor-12

PI3K/mTOR Inhibitor-12 是一种口服有效的选择性 PI3K/mTOR 抑制剂，对 PI3Kα 和 mTOR 的 IC50 值分别为 0.06 nM 和 3.12 nM。PI3K/mTOR Inhibitor-12 具有抗肿瘤活性。PI3K/mTOR Inhibitor-12 具有较低的肝毒性。

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PI3K/mTOR Inhibitor-12 Chemical Structure

PI3K/mTOR Inhibitor-12 Chemical Structure

CAS No. : 2891692-83-2

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PI3K/mTOR Inhibitor-12 相关抗体

Top Publications Citing Use of Products

查看 PI3K 亚型特异性产品:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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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

PI3K/mTOR Inhibitor-12 is a potent, orally active and selective PI3K/mTOR inhibitor with IC50 values of 0.06 nM and 3.12 nM for PI3Kα and mTOR, respectively. PI3K/mTOR Inhibitor-12 has antitumor activity. PI3K/mTOR Inhibitor-12 has lower liver toxicity[1].

IC50 & Target[1]

PI3Kα

0.06 nM (IC50)

mTOR

3.12 nM (IC50)

体外研究
(In Vitro)

PI3K/mTOR Inhibitor-12 (compound 48; 72 h) inhibits cancer cells growth with IC50 values of 0.07, 0.09, 0.54, 0.54, and 0.68 μM for PC-3, HT-29,HCT116, LOVO, and HUVEC cells, respectively[1].
PI3K/mTOR Inhibitor-12 (0.25-1 μM; 12-48 h; HCT116 and HT-29 cells) inhibits the activation of PI3K and mTOR in the cellular context[1].

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

PI3K/mTOR Inhibitor-12 相关抗体:

Western Blot Analysis[1]

Cell Line: HCT116 and HT-29 cells
Concentration: 0.25, 0.5, and 1 μM
Incubation Time: 12, 24, and 48 hours
Result: Inhibited the expression levels of AKT, p70S6K and their phosphorylated forms in a dose- and time-dependent manner.
体内研究
(In Vivo)

PI3K/mTOR Inhibitor-12 (compound 48; 20 mg/kg; p.o.; daily, for 14 d) inhibits tumor growth of HCT116 xenografts in female BALB/c nude mice[1].
PI3K/mTOR Inhibitor-12 (1 and 5 mg/kg; i.v. and p.o.; male SD rats) has fast plasma clearance (1428 mL/h/kg) and short T1/2 (2.33 h) and the AUC0-∞ is 1356 h*ng/mL[1].

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

Animal Model: HCT116 xenografts in female BALB/c nude mice[1]
Dosage: 20 mg/kg
Administration: Oral administration, daily, for 14 days
Result: Reduced the growth of HCT116 tumors, and the tumor growth inhibition (TGI) was 73.33%.
Had lower liver toxicity of HCT116 xenografts in female BALB/c nude mice.
Animal Model: Male SD rats[1]
Dosage: 1 and 5 mg/kg
Administration: Intravenous injection (1 mg/kg) and oral administration (5 mg/kg)
Result: 1.19
Parameter I.V. (1 mg/kg) Parameter P.O. (5 mg/kg)
T1/2 (h) 0.6 T1/2 (h) 2.33
CL (mL/h/kg) 1428 Cmax (ng/mL) 1218
Vdss (mL/Kg) 528 AUC0-∞ (h*ng/mL) 1356
AUC0-∞ (h*ng/mL) 760 F% 33.1
分子量

611.62

Formula

C27H27F2N9O4S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PI3K/mTOR Inhibitor-12 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

PI3K/mTOR Inhibitor-122891692-83-2PI3KmTORPhosphoinositide 3-kinaseMammalian target of Rapamycinanticancerliver toxicityHCT116HT-29phosphorylationInhibitorinhibitorinhibit

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