CDK5 inhibitor 20-223

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CDK5 inhibitor 20-223  纯度: 99.64%

CDK5 inhibitor 20-223 是一种有效的 CDK2 和 CDK5 抑制剂，IC50 分别为 6.0 和 8.8 nM。CDK5 inhibitor 20-223 有潜力用于结肠直肠癌 (CRC) 的研究。

CDK5 inhibitor 20-223

CDK5 inhibitor 20-223 Chemical Structure

CAS No. : 865317-30-2

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10 mM * 1 mL in DMSO ￥2200 In-stock
5 mg ￥2000 In-stock
10 mg ￥3500 In-stock
25 mg ￥6500 In-stock
50 mg ￥9500 In-stock
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CDK5 inhibitor 20-223 相关产品

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生物活性

CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent[1].

IC50 & Target[1]

CDK2

6.0 nM (IC50)

CDK5

8.8 nM (IC50)

体外研究
(In Vitro)

CDK5 inhibitor 20-223 (10 nM-10 μM; 72 hours) potently inhibits cell growth in a panel of colorectal cancer (CRC) cell lines[1].
CDK5 inhibitor 20-223 (0.3125-20 μM; 6 hours) induces a dose-dependent decrease in pRB (S807/811) and pFAK (S732) levels in each of the three CRC cell lines[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.

Cell Viability Assay[1]

Cell Line: CRC cell lines SW620, DLD1, HT29, HCT116, FET, CBS, and GEO cells
Concentration: 10 μM, 1 μM, 100 nM, 10 nM
Incubation Time: 72 hours
Result: Reduced cell growth. IC50s of 168±20, 480±41, 360±72, 763±92, 117±49, 568±49, 79±31 nM for SW620, DLD1, HT29, HCT116, FET, CBS, and GEO cells.

Western Blot Analysis[1]

Cell Line: CRC cell lines GEO, HCT116 and HT29
Concentration: 20, 10, 5, 2.5, 1.25, 0.625, 0.3125 μM
Incubation Time: 6 hours
Result: Did not affect the total levels of CDK2/5, and the levels of total FAK or total Retinoblastoma protein (Rb).
Induced a dose-dependent decrease in pRB (S807/811) and pFAK (S732) levels.

体内研究
(In Vivo)

CDK5 inhibitor 20-223 (8mg/kg; subcutaneously; for 14 injections) shows anti-tumor activity in human CRC xenograft tumors in nude mice[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 Model: Athymic nude mice[1]
Dosage: 8 mg/kg
Administration: Injections were given subcutaneously daily for the first week and every other day for two more weeks for a total of 14 injections.
Result: Reduced tumor growth and tumor weight in vivo.

分子量

305.37

Formula

C19H19N3O
CAS 号

865317-30-2
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 : 100 mg/mL (327.47 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2747 mL 16.3736 mL 32.7472 mL
5 mM 0.6549 mL 3.2747 mL 6.5494 mL
10 mM 0.3275 mL 1.6374 mL 3.2747 mL

*

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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    90% corn oil

    Solubility: ≥ 5 mg/mL (16.37 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (16.37 mM，饱和度未知) 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 50.0 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]. Caroline M Robb, et al. Characterization of CDK(5) Inhibitor, 20-223 (Aka CP668863) for Colorectal Cancer Therapy. Oncotarget. 2017 Dec 28;9(4):5216-5232.

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