1. Protein Tyrosine Kinase/RTK Apoptosis PI3K/Akt/mTOR Stem Cell/Wnt JAK/STAT Signaling Epigenetics MAPK/ERK Pathway GPCR/G Protein
  2. Src Apoptosis IAP Survivin Akt mTOR JAK STAT Ras p38 MAPK
  3. K882

K882 (Compound 4e) 是一种 Src 抑制剂,KD 为 0.315 μM。K882 诱导凋亡(Apoptosis)。K882 抑制 XIAPSurvivin。K882 抑制 PI3K/Akt/mTORJak1/Stat3Ras/MAPK 信号通路的激活。K882 对非小细胞肺癌 具有抗肿瘤活性。

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K882 Chemical Structure

K882 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

K882 (Compound 4e) is a Src inhibitor, with KD of 0.315 μM. K882 induces Apoptosis. K882 inhibits XIAP and Survivin. K882 inhibits the activation of PI3K/Akt/mTOR, Jak1/Stat3, Ras/MAPK signaling pathways. K882 shows anti-tumor activity against non-small cell lung cancer[1].

IC50 & Target[1]

PI3Kα

 

XIAP

 

JAK1

 

Stat-3

 

体外研究
(In Vitro)

K882 (0.5-8 μM,24-72 h) 对 KRASG12C 突变 NCI-H358 细胞的增殖、迁移和侵袭表现出显著的抑制活性[1]

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

Cell Cycle Analysis[1]

Cell Line: NCI-H358
Concentration: 0.5, 1, 2 and 4 μM
Incubation Time: 24 h
Result: Blocked the NCI-H358 cell cycle in the G2/M phase.

Cell Cycle Analysis[1]

Cell Line: NCI-H358
Concentration: 1, 2, 4, 8 μM
Incubation Time: 24 h
Result: Increased the rate of apoptotic cells concentration-dependently.
Inhibited the expressions of two apoptosis inhibitory proteins (XIAP and Survivin).
体内研究
(In Vivo)

K882 (25-100 mg/kg,腹腔注射,每天一次,31天) 抑制 NCI-H358 异种移植肿瘤小鼠模型中KRASG12C 突变型 NSCLC 异种移植瘤的生长[1]

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

Animal Model: NCI-H358 xenograft tumor mice model[1]
Dosage: 25, 50 and 100 mg/kg,
Administration: Intraperitoneal injection (i.p.), once a day, 31 days
Result: Decreased tumor volume.
Showed the tumor inhibitory rates of 42.48 % (25 mg/kg), 49.72% (50 mg/kg) and 60.39 % (100 mg/kg).
Abrogated the phosphorylation at Y416 of Src.
Did not exhibit any apparent damage in the vital organs.
分子量

292.33

Formula

C18H16N2O2

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:
K882
目录号:
HY-168893
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