1. Cell Cycle/DNA Damage JAK/STAT Signaling
  2. CDK Pim
  3. CDK2/PIM1-IN-1

CDK2/PIM1-IN-1 是 CDK2 (IC50: 0.27 μM) 和 PIM1 (IC50: 0.67 μM) 激酶的抑制剂。CDK2/PIM1-IN-1 可诱导细胞凋亡 (apoptosis),并降低促进肿瘤的 TNF-α 表达。CDK2/PIM1-IN-1 具有抗肿瘤活性。

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CDK2/PIM1-IN-1 Chemical Structure

CDK2/PIM1-IN-1 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK2/PIM1-IN-1 is an inhibitor of CDK2 (IC50: 0.27 μM) and PIM1 (IC50: 0.67 μM) kinases. CDK2/PIM1-IN-1 induces apoptosis and reduces tumor-promoting TNF-α expression. CDK2/PIM1-IN-1 has antitumor activity[1].

IC50 & Target[1]

CDK2

0.27 μM (IC50)

PIM1

0.67 μM (IC50)

体外研究
(In Vitro)

CDK2/PIM1-IN-1 (Compound 6b) (24 小时) 对 MCF7 细胞 (IC50: 5.54 μM)、HCT-116 细胞 (IC50: 2.62 μM)、HepG2 细胞 (IC50: 3.99 μM) 和 HeLa 细胞系 (IC50: 8.31 μM) 均表现出抗增殖作用,并在正常乳腺细胞系 MCF-10A (IC50: 39.44 μM) 中呈现中等安全性[1]
CDK2/PIM1-IN-1 (24 小时) 在G0-G1 期抑制 HCT116 细胞系(%G0-G1: 83.43%),并诱导了显着的早期细胞 (8.28%) 和晚期细胞(20.09%)凋亡[1]
CDK2/PIM1-IN-1 (24 小时) 对 HCT116 细胞系中 CDK (IC50: 0.27 μM) 和 PIM1 (IC50: 0.67 μM) 均表现出抑制作用[1]

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

Cell Viability Assay[1]

Cell Line: Tumor cell line (MCF7 cells, HCT-116 cells, HepG2 cells, HeLa cell lines), and the normal breast cell line MCF-10A.
Concentration:
Incubation Time: 24 h
Result: Inhibited the cell viability of MCF7 cells (IC50: 5.54 μM), HCT-116 cells (IC50: 2.62 μM), HepG2 cells (IC50: 3.99 μM) and HeLa cell lines (IC50: 8.31 μM).
Showed moderate safety in the normal breast cell line MCF-10A (IC50: 39.44 μM).
体内研究
(In Vivo)

CDK2/PIM1-IN-1 (Compound 6b) (10 mg/kg; IP; three times weekly for two weeks) 可降低实体 Ehrlich 癌 (SEC) 小鼠模型中肿瘤的体积 (71.42%) 和重量 (70.58%),并表现出良好的耐受性[1]

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

Animal Model: Solid Ehrlich carcinoma (SEC) mouse model[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.), three times weekly for two weeks.
Result: Reduced tumor volume (71.42%) and weight (70.58%).
Showed good tolerability (indicated by stable body weight and 100% survival rate compared with the Dox-treated group).
Inhibited CDK2 (70.96%) and PIM1 (53.61%) levels in mouse tumors, tumor cell mitosis (27.35%).
Inhibited tumor TNF-α expression (17.61%).
分子量

421.49

Formula

C27H23N3O2

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:
CDK2/PIM1-IN-1
目录号:
HY-173224
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