PHA-793887

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PHA-793887

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

718630-59-2

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
2mg	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品介绍

PHA-793887 是一种有效的，ATP 竞争性的CDK抑制剂，可抑制 Cdk2，Cdk1，Cdk4 和 Cdk9 的活性，IC₅₀值分别为 8 nM，60 nM，62 nM 和 138 nM，同时可抑制糖原合酶激酶 3β (GSK-3β)，IC₅₀值为 79 nM。

生物活性

PHA-793887 is a potent, ATP-competitiveCDKinhibitor, can inhibitCdk2,Cdk1,Cdk4, andCdk9withIC₅₀s of 8 nM, 60 nM, 62 nM and 138 nM, respectively, and also inhibits glycogen synthase kinase 3β with anIC₅₀of 79 nM.

IC₅₀& Target^[4]

Cdk5/p25

5 nM (IC₅₀)

cdk2/cyclin A

8 nM (IC₅₀)

CDK2/cyclinE

8 nM (IC₅₀)

CDK7/cyclin H

10 nM (IC₅₀)

Cdk1/cyclin B

60 nM (IC₅₀)

Cdk4/cyclin D1

62 nM (IC₅₀)

CDK9/cyclinT1

138 nM (IC₅₀)

GSK-3β

79 nM (IC₅₀)

体外研究
(In Vitro)

PHA-793887 partially inhibits Rb phosphorylation at 1 μM and almost completely at 3 μM, in A2780 tumor cell line. PHA-793887 (1 μM) partially inhibits phosphorylation of the Cdk2 substrates Rb and NPM in A2780 tumor cell line. PHA-793887 (6 μM) significantly inhibits Rb and NPM phosphorylation in MCF7 cell line^[1]. PHA-793887 shows cytotoxic activities against leukemic cell lines in vitro, with IC₅₀ranging from 0.3 to 7 μM. In colony assays, PHA-793887 is highly cytotoxic for leukemia cell lines, with an IC₅₀<0.1 μM. PHA-793887 induces cell-cycle arrest, inhibits Rb and nucleophosmin phosphorylation, and modulates cyclin E and cdc6 expression at low doses of 0.2 to 1 μM and induces apoptosis at the highest dose of 5 μM. PHA-793887 is a novel inhibitor of several cdk, including cdk1, cdk2, cdk4, cdk5, cdk7, and cdk9 with IC₅₀in the 5 to 140 nM range^[3].

体内研究
(In Vivo)

PHA-793887 induces tumor growth inhibition in the range of 50% at dose of 15 mg/kg to 75% at dose of 30 mg/kg in CD-1 nude mice. PHA-793887 (30 mg/kg, i.v.) also induces significant downregulation of the 58-gene panel in the skin of CD-1 mice^[1]. PHA-793887 (20 mg/kg, i.v.) induces tumor regression in the HL60 model. In the K562 model, PHA-793887 significantly reduces tumor growth. Moreover, PHA-793887 (20 mg/kg, i.v.) inhibits human primary leukemia growth in engraftment setting in vivo^[3].

Clinical Trial

分子量

361.48

性状

Solid

Formula

C₁₉H₃₁N₅O₂

CAS 号

718630-59-2

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 : ≥ 50 mg/mL(138.32 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	2.7664 mL	13.8320 mL	27.6640 mL
5 mM	0.5533 mL	2.7664 mL	5.5328 mL
10 mM	0.2766 mL	1.3832 mL	2.7664 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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% (20%SBE-β-CDin saline)
Solubility: ≥ 2.5 mg/mL (6.92 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.92 mM，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 μL20% 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

*以上所有助溶剂都可在本网站选购。