2. Cell Cycle/DNA Damage
  3. Checkpoint Kinase (Chk)
  4. Chk1-IN-6

Chk1-IN-6 是一种具有选择性且口服活性的 Chk1 抑制剂，其 IC50 值为 16.1 nM。Chk1-IN-6 对 MV-4-11 细胞具有抗增殖活性。Chk1-IN-6 在 MV-4-11 肿瘤移植小鼠模型中表现出有效反应。Chk1-IN-6 与 Gemcitabine (HY-17026) 具有协同的抗癌效果。Chk1-IN-6 可用于急性髓系白血病和结直肠腺癌等癌症的研究。

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Chk1-IN-6

Chk1-IN-6 Chemical Structure

CAS No. : 2428423-77-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2444
In-stock
1 mg ￥1208
In-stock
5 mg ￥3040
In-stock
10 mg ￥4840
In-stock
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Chk1-IN-6 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 BUBR1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Chk1-IN-6 is a selective and orally active Chk1 inhibitor with an IC50 of 16.1 nM. Chk1-IN-6 shows antiproliferative activity of MV-4-11 cells. Chk1-IN-6 exerts effective response in the MV-4-11 xenograft mouse model. Chk1-IN-6 exhibits synergistic anticancer effect with Gemcitabine (HY-17026). Chk1-IN-6 can be used in the research of cancers such as acute myeloid leukemia and colorectal adenocarcinoma[1].

IC50 & Target[1]

Chk1

16.1 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MV4-11 IC50
0.14 μM
Compound: 6c
Antiproliferation activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Antiproliferation activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
[PMID: 34665631]
Z-138 IC50
3.28 μM
Compound: 6c
Antiproliferation activity against human Z138 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Antiproliferation activity against human Z138 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
[PMID: 34665631]
体外研究
(In Vitro)

Chk1-IN-6 (Compound 6c) 对 MV-4-11 和 Z138 细胞表现出抗增殖活性，IC50 值分别为 0.14 和 3.28 μM[1]。
Chk1-IN-6 (0-5 nM，72 小时) 与 Gemcitabine 联合使用，对 HT-29、A549 和 RPMI-8226 细胞表现出协同作用[1]。
Chk1-IN-6 (0-800 nM，2 小时) 在 MV-4-11 细胞中抑制磷酸化的 S296 CHK1 (pS296 CHK1) ，并诱导磷酸化的 S345 CHK1 (pS345 CHK1)[1]。

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

Chk1-IN-6 相关抗体:

Western Blot Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 0, 50, 100, 200, 400 and 800 nM
Incubation Time: 2 h
Result: Caused a dose-dependent decrease in pS296 CHK1.
Induced a dose-dependent increase in pS345.
With Gemcitabine at 1.1 μM in different concentrations could lead to a pronounced reduction in pS296 CHK1 and induced an increase in γ-H2A.X.
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Mice 20 mg/kg p.o. T1/2 10.84 h
Mice 20 mg/kg p.o. Tmax 4.00 h
Mice 20 mg/kg p.o. Cmax 1447 ng/mL
Mice 20 mg/kg p.o. AUC0-t 17679 ng·h/mL
Mice 20 mg/kg p.o. AUC0-∞ 22679 ng·h/mL
Mice 20 mg/kg p.o. MRT0-∞ 14.73 h
体内研究
(In Vivo)

Chk1-IN-6 (Compound 6c) (5-30 mg/kg，口服，每日一次，共 21 天) 在 MV-4-11 异种移植小鼠模型中以剂量依赖性方式显著抑制体内肿瘤生长[1]。
Chk1-IN-6 (5-30 mg/kg，口服，连续 5 天/周，共 22 天) 在 HT-29 异种移植小鼠模型中表现出与 Gemcitabine 协同抗癌作用[1]。

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

Animal Model: MV-4-11 xenograft model established in NU/NU nude mice[1]
Dosage: 5, 15 and 30 mg/kg
Administration: Oral administration (p.o.), once daily for 21 days
Result: Significantly inhibited tumor growth in vivo in a dose-dependent manner and showed inhibition of tumor growth of 51.62, 95.52, and 94.90% at doses of 5, 15, 30 mg/kg, respectively.
Animal Model: HT-29 xenograft model established in NU/NU nude mice[1]
Dosage: 30 mg/kg with or without Gemcitabine
Administration: Oral administration (p.o.), continuously for 5 days/week for 22 days
Result: Showed mild antitumor effect with T/C values of 69.05% and in combination with Gemcitabine showed a significant increase in efficacy (T/C = 11.99%).
分子量

365.36

Formula

C16H18F3N7
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 25 mg/mL (68.43 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7370 mL 13.6851 mL 27.3703 mL
5 mM 0.5474 mL 2.7370 mL 5.4741 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Chk1-IN-6 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7370 mL 13.6851 mL 27.3703 mL 68.4257 mL
5 mM 0.5474 mL 2.7370 mL 5.4741 mL 13.6851 mL
10 mM 0.2737 mL 1.3685 mL 2.7370 mL 6.8426 mL
15 mM 0.1825 mL 0.9123 mL 1.8247 mL 4.5617 mL
20 mM 0.1369 mL 0.6843 mL 1.3685 mL 3.4213 mL
25 mM 0.1095 mL 0.5474 mL 1.0948 mL 2.7370 mL
30 mM 0.0912 mL 0.4562 mL 0.9123 mL 2.2809 mL
40 mM 0.0684 mL 0.3421 mL 0.6843 mL 1.7106 mL
50 mM 0.0547 mL 0.2737 mL 0.5474 mL 1.3685 mL
60 mM 0.0456 mL 0.2281 mL 0.4562 mL 1.1404 mL
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-62428423-77-0Checkpoint Kinase (Chk)Checkpoint kinase 1MV-4-11 cellsHT-29 cellsmice modelorally bioavailableInhibitorinhibitorinhibit

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