2. Cell Cycle/DNA Damage
  3. CDK
  4. Fadraciclib

Fadraciclib  (Synonyms: CYC065)

目录号: HY-101212 纯度: 99.70%
COA 产品使用指南

摩尔计算器

Fadraciclib (CYC065) 是第二代口服有效的 ATP 竞争性的 CDK2/CDK9 激酶抑制剂，IC50 分别为 5 和 26 nM。

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Fadraciclib Chemical Structure

Fadraciclib Chemical Structure

CAS No. : 1070790-89-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3850
In-stock
1 mg ￥1450
In-stock
5 mg ￥3500
In-stock
10 mg ￥4918
In-stock
25 mg 现货 询价
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

Fadraciclib 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Fadraciclib (CYC065) is a second-generation, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases[1] with IC50s of 5 and 26 nM, respectively[2].

IC50 & Target[1]

CDK2

 

CDK9

 

体外研究
(In Vitro)

Fadraciclib blocks cells in the G1 phase of the cell cycle and inhibits cell growth specifically in cyclin E1 (CCNE1)-overexpressing uterine serous carcinomas (USCs). USC cell lines expressing high CCNE1 mRNA and protein levels to be significantly more sensitive to treatment with Fadraciclib in vitro when compared with low CCNE1-expressing cell lines (IC50: mean±s.d.=124.1±57.8 nM in CCNE1-overexpressing USC cell lines vs 415±117.5 nM in CCNE1 low expressors, respectively; P=0.0003). Importantly, low concentrations of Fadraciclib (i.e., 100 nM) causes an arrest in the G1 phase of the cell cycle only in the CCNE1-overexpressing USC cell lines (i.e., USC-ARK-2, USC-ARK-7) [1].

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

Fadraciclib 相关抗体:
体内研究
(In Vivo)

To evaluate the therapeutic potential of Fadraciclib as a single agent, USC-ARK-2-derived xenografts are treated daily with Fadraciclib (22.5 mg/kg) for a 3-week period. Tumor size and mouse weight are recorded two times a week. The daily administration of Fadraciclib results in a significant reduction of tumor growth compared with the vehicle-treated mice (P=0.012 starting at day 9 of the treatment). No significant weight loss is reported during the entire treatment period[1].

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

397.52

Formula

C21H31N7O
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 1 year
-20°C 6 months
溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 100 mg/mL (251.56 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" 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 2.5156 mL 12.5780 mL 25.1560 mL
5 mM 0.5031 mL 2.5156 mL 5.0312 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6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

动物实验：

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

  • 方案 一

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

    Solubility: ≥ 2.5 mg/mL (6.29 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

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

    Solubility: ≥ 2.5 mg/mL (6.29 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 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。

    20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
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
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.78%

COA (196 KB) LCMS (119 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[1]

The effect of CYC065 on the viability and IC50 of USC-ARK-1, USC-ARK-2, USC-ARK-7, USC-ARK-4 and USC-ARK-6 USC primary cell lines is determined in flow-cytometry assay. Briefly, tumour cells are plated in six-well plates and treated with a titration of CYC065 concentrations (i.e., ranging from 100 to 500 nM). After 72 h, cells are harvested, washed and stained with propidium iodide (PI; 5 μg/mL) for flow cytometric counts. The percentage of viable cells is then normalised considering the vehicle-treated cells as 100% viable. Half-maximal inhibitory concentration values are determined using GraphPad Prism5 version 6. For drug combination studies, USC-ARK-1 and USC-ARK-2 cell lines are incubated with the combination of Taselisib and CYC065 at multiple paired concentrations including the IC50, the IC50/2 and the IC50*2 of each cell line to the corresponding drug (i.e., 10 nM of Taselisib and 198 nM of CYC065 for USC-ARK-1 and 50 nM of Taselisib and 62.5 nM of CYC065 for USC-ARK-2). Synergism is assessed by the combination index (CI). CI values <1 define a synergistic activity of the combination treatment. The CI values are calculated using the CompuSyn software[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
The in vivo efficacy of CYC065 used as a single agent is evaluated on xenograft mouse models derived from the CCNE1-amplified USC-ARK-2 USC cell line. Xenografts derived from the CCNE1-amplified, PIK3CA-mutated USC-ARK-1 cell line are used for evaluating the in vivo combination of CYC065 and Taselisib. Briefly, 5-7-week-old SCID mice are injected into the subcutaneous region with USC cells. A minimum of five animals per group are used. Treatments are administrated by oral gavage starting 1 week after tumor implantation when the size of the tumor is 0.125-0.150 cm3. Uterine serous carcinoma-ARK-2-derived xenografts are divided into two groups: one group of animal receive the vehicle, whereas the experimental group receive CYC065 (22.5 mg/kg daily for 3 weeks). Uterine serous carcinoma-ARK-1-derived xenografts are instead divided into four groups: one group receive the vehicle (0.5% methylcellulose-0.2% Tween-80), one group receive CYC065 (22.5 mg/kg daily for 3 weeks), one group receive Taselisib (10 mg/kg daily, 5 days per week per 3 weeks) and the last group receive the combination of CYC065 and Taselisib. The size of the tumor at the initiation of treatment is 0.125-0.150 cm3. Mouse weight and tumor size is recorded two times a week for the entire experimental period. Tumor volume is calculated.

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

Fadraciclib 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6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 2.5156 mL 12.5780 mL 25.1560 mL 62.8899 mL
5 mM 0.5031 mL 2.5156 mL 5.0312 mL 12.5780 mL
10 mM 0.2516 mL 1.2578 mL 2.5156 mL 6.2890 mL
15 mM 0.1677 mL 0.8385 mL 1.6771 mL 4.1927 mL
20 mM 0.1258 mL 0.6289 mL 1.2578 mL 3.1445 mL
25 mM 0.1006 mL 0.5031 mL 1.0062 mL 2.5156 mL
30 mM 0.0839 mL 0.4193 mL 0.8385 mL 2.0963 mL
40 mM 0.0629 mL 0.3144 mL 0.6289 mL 1.5722 mL
50 mM 0.0503 mL 0.2516 mL 0.5031 mL 1.2578 mL
60 mM 0.0419 mL 0.2096 mL 0.4193 mL 1.0482 mL
80 mM 0.0314 mL 0.1572 mL 0.3144 mL 0.7861 mL
100 mM 0.0252 mL 0.1258 mL 0.2516 mL 0.6289 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:

Fadraciclib1070790-89-4CYC065CYC 065CYC-065CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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