CDK5 inhibitor 20-223 - CAS:865317-30-2

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CDK5 inhibitor 20-223

目录号 : KM5108 CAS No. : 865317-30-2 纯度 : 98%

Data Sheet 产品使用指南

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。

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200mg	询价	In-stock

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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.

体外研究

CDK5 inhibitor 20-223 (10 nM-10 μM; 72 hours) potently inhibits cell growth in a panel of colorectal cancer (CRC) cell lines.
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.

Cell Viability Assay

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

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

CDK5 inhibitor 20-223 (8mg/kg; subcutaneously; for 14 injections) shows anti-tumor activity in human CRC xenograft tumors in nude mice.

Animal Model:	Athymic nude mice
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.

分子式

C₁₉H₁₉N₃O

分子量

305.37

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

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 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。