2. Cell Cycle/DNA Damage
  3. Checkpoint Kinase (Chk)
  4. CHK1-IN-9

CHK1-IN-9 (compound 11) 是一个口服活性的 CHK1 抑制剂，IC50 值为 0.55 nM。CHK1-IN-9 可以增强 DNA 损伤药物对肿瘤细胞的作用，与 Gemcitabine (HY-17026) 具有协同抗癌作用。

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CHK1-IN-9 Chemical Structure

CHK1-IN-9 Chemical Structure

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

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CHK1-IN-9 相关抗体

Top Publications Citing Use of Products

查看 Checkpoint Kinase (Chk) 亚型特异性产品:

查看所有亚型
Chk1 Chk2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC50 value of 0.55 nM. CHK1-IN-9 can enhance the effect of DNA-damaging drugs on tumor cells. CHK1-IN-9 has synergistic anticancer effects with Gemcitabine (HY-17026)[1].

IC50 & Target

Chk1

0.55 nM (IC50)

体外研究
(In Vitro)

CHK1-IN-9 (compound 11) (11.11, 33.33, 100, and 300 nM, 16 h) 对肿瘤细胞具有增殖抑制作用，其中对 MV-4-11 细胞的 IC50 值为 202 nM[1]。

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

CHK1-IN-9 相关抗体:

Cell Proliferation Assay [1]

Cell Line: OVCAR3, HT-29, A549, HL-60, HCT116, A2780 and MDAMB-468 cells
Concentration: 11.11, 33.33, 100, and 300 nM
Incubation Time: 16 h
Result: Alone had an IC50 value of 1166.5 nM for HT-29, and 63.53 nM when combined with Gemcitabine (HY-17026).
体内研究
(In Vivo)

CHK1-IN-9 (compound 11) (每天使用 30 mg/kg，连续21天，iv or po) 单独使用时对 HT-29 异种移植小鼠模型的肿瘤生长抑制 (TGI) 值为 20.6％，与 Gemcitabine (HY-17026) 联合使用时显示出更大的抗肿瘤活性 (TGI = 42.8%)[1]。

HT-29异种移植小鼠模型中的药代动力学分析[1]

Route Dose (mg/kg) C0 (ng/mL) Cmax (ng/mL) T1/2 (h) Tmax (h) AUC0-t (ng·h/mL) AUC0-∞ (ng·h/mL) MRT0-t (h) MRT0-t (h) Cl (mL/kg/min) Vss (L/kg) F (%)
i.v. 2 860 526 5.70 0.08 327 341 2.67 3.91 98.4 23.3 /
p.o. 10 / 81.1 1.51 0.08 40.7 47.3 1.00 1.65 / / 2.77

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

412.40

Formula

C19H18F2N8O
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

CHK1-IN-9 相关分类

  • 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.

Keywords:

CHK1-IN-9Checkpoint Kinase (Chk)DNA damageMV-4-11 cellHT-29 xenograft mouse modelHT-29 cellcancercell proliferationInhibitorinhibitorinhibit

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目录号：
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