CC-671

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

CC-671  纯度: 99.08%

CC-671 是一个双重 TTK 蛋白激酶/CDC2 样激酶 (CLK2) 抑制剂, 对于 TTK 和 CLK2 的 IC50 值分别为 0.005 和 0.006 μM。

CC-671

CC-671 Chemical Structure

CAS No. : 1618658-88-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3157 In-stock
5 mg ¥2800 In-stock
10 mg ¥4480 In-stock
25 mg ¥8600 In-stock
50 mg ¥13800 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

CC-671 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

CC-671 is a dual TTK protein kinase/CDC2-like kinase (CLK2) inhibitor with IC50s of 0.005 and 0.006 μM for TTK and CLK2, respectively.

IC50 & Target

CLK2

0.006 μM (IC50)

体外研究
(In Vitro)

CC-671 (compound 23) is a dual TTK protein kinase/CDC2-like kinase (CLK2) inhibitor with IC50s of 0.005 and 0.006 μM for TTK and CLK2, respectively. HCT-116 cell lysates treated with CC-671 at 3 μM for 1 h demonstrates that only four kinases show cellular binding of 75% or more including CLK2, CAMKK2, PIP4K22, and JNK[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

CC-671 (compound 23) demonstrates significant tumor growth inhibition (TGI) ((vehicle -treated/vehicle) ×100%) of 71% at both 10 and 20 mg/kg on a every 3 days (q3d) dosing schedule. The body weight loss (BWL) in the CC-671 treated group (20 mg/kg ) is higher than in the 10 mg/kg group (17% vs 5%)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

512.56

Formula

C28H28N6O4

CAS 号

1618658-88-0

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
In Vitro: 

DMSO : ≥ 60 mg/mL (117.06 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9510 mL 9.7550 mL 19.5099 mL
5 mM 0.3902 mL 1.9510 mL 3.9020 mL
10 mM 0.1951 mL 0.9755 mL 1.9510 mL

*

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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.06 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.06 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (4.06 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (4.06 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: 2.08 mg/mL (4.06 mM); Clear solution; Need warming

    此方案可获得 2.08 mg/mL (4.06 mM) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Riggs JR, et al. The Discovery of a Dual TTK Protein Kinase/CDC2-Like Kinase (CLK2) Inhibitor for the Treatmentof Triple Negative Breast Cancer Initiated from a Phenotypic Screen. J Med Chem. 2017 Nov 9;60(21):8989-9002.

Kinase Assay
[1]

The kinase selectivity profile of CC-671 (compound 23) is assessed. The screen is conducted with the concentration of CC-671 held constant at 3 μM. The TTK binding affinity is measured using the kinase binding assays. The kinase binding assays are based on the binding and displacement of a proprietary, Alexa Fluor 647-labeled, ATP-competitive kinase inhibitor scaffold[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Female SCID mice are inoculated subcutaneously with 5×106 Cal-51 cells. Mice with tumors of approximately 125 mm3 are randomized and treated intravenously at various doses and schedules of CC-671 (compound 23) (n=8 to10/group). Tumors are measured twice a week for the duration of the study. The long and short axes of each tumor are measured using a digital caliper in millimeters and the tumor volumes are calculated[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Riggs JR, et al. The Discovery of a Dual TTK Protein Kinase/CDC2-Like Kinase (CLK2) Inhibitor for the Treatmentof Triple Negative Breast Cancer Initiated from a Phenotypic Screen. J Med Chem. 2017 Nov 9;60(21):8989-9002.

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