1. PI3K/Akt/mTOR Apoptosis Autophagy
  2. mTOR Apoptosis Autophagy
  3. ASCT2-IN-2

ASCT2-IN-2(化合物 25e)是一种 ASCT2 抑制剂,IC50 值是 5.14 μM。 ASCT2-IN-2 可以调节氨基酸代谢和 mTOR信号转导,诱导细胞凋亡(apoptosis)。ASCT2-IN-2 具有抗肿瘤活性。

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ASCT2-IN-2 Chemical Structure

ASCT2-IN-2 Chemical Structure

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Customer Review

查看 mTOR 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ASCT2-IN-2 (compound 25e) is an ASCT2 inhibitor with IC50 of 5.14 μM. ASCT2-IN-2 regulates amino acid metabolism as well as mTOR signaling and thereby induces cell apoptosis. ASCT2-IN-2 inhibits tumor growth[1].

体外研究
(In Vitro)

ASCT2-IN-2(50 μM,15 min)通过靶向 hASCT 抑制细胞 A549 和 HEK293 中 Glutamine 的摄取(摄取率是 55.62% 和 98.31%),IC50 值分别是 5.6 μM 和 3.5 μM[1]
ASCT2-IN-2(0-50 μM,15 min)提高了小鼠肝微粒体中的代谢稳定性,半衰期是 166.51 min,清除率是 8.27 μL/min•mg[1]
ASCT2-IN-2(0-50 μM,15 min)在细胞 A549 中提高转运蛋白 LAT1 的活性从而促进 leucine 的摄取[1]
ASCT2-IN-2(5-10 μM,24 h)在细胞 A549 中抑制 Gln 代谢,增进 ROS 生产从而诱导细胞凋亡[1]
ASCT2-IN-2(5-10 μM,24 h)在饥饿条件下抑制 AKT 磷酸化和 mTORC1 活性,促进细胞自噬 (autophagy)[1]
ASCT2-IN-2(5-10 μM,24 h)剂量依赖性地抑制 A549 增殖[1]
ASCT2-IN-2(0-10 nM,96 h)抑制 H1975 OR 和 HCC827 OR 细胞中 NSCLCs 的类器官增殖[1]

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

Cell Viability Assay[1]

Cell Line: A549
Concentration: 50 μM
Incubation Time: 72 h
Result: Exhibited antiproliferation activity in A549, with IC50 of 5.83 μM.
体内研究
(In Vivo)

ASCT2-IN-2(腹腔注射;25 或 50 mg/kg, 每两天一次,共三周)抑制 A549 肿瘤生长,TGI 值是 70%[1]

ASCT-2 在 SD 鼠体内的药代动力学分析[1]

Route Dose (mg/kg) AUC0→t (μg·h/L) AUC0→∞ (μg·h/L) T1/2 (h) Tmax (h) Cmax (ng/mL) V/F(L/kg) CL/F(L/h/kg) MRT0→∞(h) Fr(%)
i.p. 10 mg/kg 13804.10 14544.59 19.41 5.33 874.32 19.99 0.72 20.73 396.73

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

Animal Model: Tumor Growth in A549 Xenograft Model in BALB/c mice[1]
Dosage: 25 and 50 mg/kg, once every two days for 3 weeks
Administration: Intraperitoneal injection
Result: Inhibited tumor growth with a TGI of 70%
分子量

670.88

Formula

C44H50N2O4

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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产品名称:
ASCT2-IN-2
目录号:
HY-163199
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