2. PI3K/Akt/mTOR
  3. Akt
  4. PX-316

PX-316 是一种 Akt 抑制剂。PX-316 可使 Akt 磷酸化，但不抑制 PDK1 或 PKC 的磷酸化。PX-316 能特异性地增加一组线粒体相关基因的表达。PX-316 可用于结肠癌和乳腺癌的研究。

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PX-316

PX-316 Chemical Structure

CAS No. : 253440-95-8

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PX-316 相关抗体

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Akt Akt1 Akt2 Akt3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PX-316 is an Akt inhibitor. PX-316 can phosphorylate Akt, but does not inhibit the phosphorylation of PDK1 or PKC. PX-316 uniquely increases the expression of a group of mitochondrial-related genes. PX-316 can be used for the study of colon cancer and breast cancer[1].

IC50 & Target

Akt

 

体外研究
(In Vitro)

PX-316 (0-15 μM，2 小时) 特异性抑制 HT-29 人结肠癌细胞中 Akt 的激活 (IC50 = 1.7 μM) ，而不影响上游激酶 PDK1 或相关激酶 PKC[1]。
PX-316 (0.5-20 μM，3 天) 抑制 MCF-7 和 HT-29 细胞的增殖[1]。

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

PX-316 相关抗体:

Western Blot Analysis[1]

Cell Line: HT-29 human colon cancer cells
Concentration: 0 μM, 5 μM, 10 μM, 15 μM
Incubation Time: 2 h
Result: Inhibited EGF-induced Akt phosphorylation (phosphorylation of Ser473 site) in a concentration-dependent manner with an IC50 value of 1.7 μM, but did not inhibit PDK1 phosphorylation (Ser241 site) or PKC phosphorylation (Thr638/641 site).
体内研究
(In Vivo)

PX-316 (37.5-150 mg/kg，腹腔注射，单次) 能有效抑制 HT-29 细胞异种移植小鼠模型中的 Akt 信号通路及其下游靶点，且多次给药后仍能维持抑制作用[1]。
PX-316 (50-150 mg/kg，腹腔注射，单次，连续4-10天) 在两种不同的人类肿瘤小鼠异种移植模型 (MCF-7 和 HT-29) 中均表现出剂量和给药方案依赖性的抗肿瘤活性[1]。

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

Animal Model: HT-29 colon cancer cells(107)were injected subcutaneously into the flanks of male severe combined immunodeficient (scid) mice[1].
Dosage: 37.5 mg/kg, 75 mg/kg, 150 mg/kg
Administration: I.p., once
Result: A single administration of 150 mg/kg inhibited Akt (Ser473) phosphorylation in tumors by up to 78% at 10 hours, recovering to 34% inhibition after 48 hours.
The half-maximal inhibitory dose (ID50) for Akt phosphorylation in tumors was 80 mg/kg, while the ID50 for normal tissue (spleen) was 128 mg/kg.
At a concentration of 150 mg/kg, phosphorylation of GSK-3β (Ser9), a downstream target of Akt, was also inhibited, with inhibition rates of 53% and 77% at 5 hours and 24 hours, respectively.
At a dose of 75 mg/kg, whether administered once daily for 5 consecutive days or once every 3 days for 5 consecutive days, Akt activity was consistently inhibited (inhibition rate of 70%-80%).
Animal Model: MCF-7 human breast cancer cells (107 cells) were mixed with Matrigel and subcutaneously injected into the flank of female SCID mice. One day before tumor cell inoculation, mice were subcutaneously implanted with 60-day sustained-release 17-β-estradiol pellets to support the growth of this estrogen-dependent tumor[1].
Dosage: 50 mg/kg, 75 mg/kg, 100 mg/kg
Administration: I.p., once daily for 10 days, 10 days and 5 days, respectively
Result: 75 mg/kg showed a good inhibitory effect (T/C = 20%), while 100 mg/kg showed a slightly weaker effect (T/C = 39%).
Animal Model: HT-29 human colon cancer cells (107 cells) were subcutaneously injected into the flank of SCID mice[1].
Dosage: 100 mg/kg, 150 mg/kg
Administration: I.p., once daily for 4 days
Result: Caused growth inhibition of 5-day HT-29 colon cancer xenografts when administered for 4 days IP at 150 mg/kg/day (T/C33.3%, P<0.05) but no activity at 100 mg/kg/day.
分子量

584.72

Formula

C28H57O10P
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

PX-316 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

PX-316253440-95-8PX316PX 316AktPKBProtein kinase BD-3-Deoxy-phosphatidyl-myo-inositol ether lipidAntitumor activityPharmacodynamicsInhibitorinhibitorinhibit

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产品名称：
PX-316
目录号：
HY-119134
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