2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. PHA-793887

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。

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PHA-793887 Chemical Structure

PHA-793887 Chemical Structure

CAS No. : 718630-59-2

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10 mM * 1 mL in DMSO ￥716
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2 mg ￥500
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5 mg ￥900
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10 mg ￥1450
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50 mg ￥4350
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Customer Review

PHA-793887 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

PHA-793887 is a potent, ATP-competitive CDK inhibitor, can inhibit Cdk2, Cdk1, Cdk4, and Cdk9 with IC50s of 8 nM, 60 nM, 62 nM and 138 nM, respectively, and also inhibits glycogen synthase kinase 3β with an IC50 of 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)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A2780 IC50
0.09 μM
Compound: 31
Antiproliferative activity against human A2780 cells after 72 hrs by fluorescence assay
Antiproliferative activity against human A2780 cells after 72 hrs by fluorescence assay
[PMID: 20153204]
A-375 IC50
0.396 μM
Compound: 31
Antiproliferative activity against human A375 cells after 72 hrs by SRB assay
Antiproliferative activity against human A375 cells after 72 hrs by SRB assay
[PMID: 20153204]
BXPC-3 IC50
3.444 μM
Compound: 31
Antiproliferative activity against human BxPC3 cells after 72 hrs by SRB assay
Antiproliferative activity against human BxPC3 cells after 72 hrs by SRB assay
[PMID: 20153204]
COLO 205 IC50
0.188 μM
Compound: 31
Antiproliferative activity against human COLO205 cells after 72 hrs by SRB assay
Antiproliferative activity against human COLO205 cells after 72 hrs by SRB assay
[PMID: 20153204]
DU-145 IC50
0.303 μM
Compound: 31
Antiproliferative activity against human DU145 cells after 72 hrs by SRB assay
Antiproliferative activity against human DU145 cells after 72 hrs by SRB assay
[PMID: 20153204]
HCT-116 IC50
0.163 μM
Compound: 31
Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay
Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay
[PMID: 20153204]
MCF7 IC50
1.284 μM
Compound: 31
Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay
Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay
[PMID: 20153204]
PC-3 IC50
0.601 μM
Compound: 31
Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay
Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay
[PMID: 20153204]
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 IC50 ranging 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 IC50 in the 5 to 140 nM range[3].

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

PHA-793887 相关抗体:
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].

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

361.48

Formula

C19H31N5O2
CAS 号
性状

固体

颜色

White to yellow

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 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 50 mg/mL (138.32 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 2.7664 mL 13.8320 mL 27.6640 mL
5 mM 0.5533 mL 2.7664 mL 5.5328 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.92 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。

    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: 99.25%

COA (295 KB) RP-HPLC (259 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[3]

Cytotoxicity assays are performed using the Alamar blue vital dye. For each cell line, preliminary dose−response curves are performed to establish the cell-concentration range, giving a linear relationship with fluorescence. For cell lines, 5,000 to 20,000 cells are plated in 200 μL complete medium in 96-well plates, in the presence or absence of increasing doses of drugs (0.01−10 μM). For ALL-2 and AML-PS leukemias 10 × 105 cells/well are plated in StemSpanSFEM medium and treated with the same range of drug concentrations. Peripheral blood mononuclear cells and cord blood CD34+ cells are plated 1 × 105 cells/well in presence or absence of 1 μg/mL phytohemagglutin or growth factor cocktail (50 ng/mL stem cell factor, 20 ng/mL each of granulocyte-macrophage colony-stimulating factor, granulocyte colony-stimulating factor, interleukin-3, interleukin-6, and 3 U/mL erythropoietin), respectively. In all cases, after 48 hours culture, 1/10 volume Alamar blue solution is added and incubated overnight. The plates are then read in a fluorimeter with excitation at 535 nm and emission at 590 nm. Cytotoxicity is calculated as percentage of fluorescence with respect to untreated control, after subtracting for background fluorescence in absence of cells.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

107 HL60 and K562 cells are inoculated subcutaneously in SCID mice. Animals are randomized in seven mice per group. PHA-793887 is administered at 20 mg/kg intravenous (IV) once a day, continuously for 10 days (from day 9 to day 18) in HL60 model and with a two 5-day cycles (from day 9 to day 13 and from day 17 to day 21) in K562-bearing mice. Glivec is orally administered for 9 consecutive days from day 9 onward in the K562 xenograft model. Tumor growth and net body weight are evaluated twice a week. The tumor weight is calculated according to the following formula: tumor weight = length (mm) × width2 (mm) /2. The effect of the anticancer treatment is determined as the delay in onset of an exponential growth of tumors. This delay (T − C value) is defined as the difference of median time (in days) required for the tumors of treatment (T) and control groups (C) to reach a predetermined size. Toxicity is evaluated on the basis of the body weight reduction.

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

PHA-793887 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7664 mL 13.8320 mL 27.6640 mL 69.1601 mL
5 mM 0.5533 mL 2.7664 mL 5.5328 mL 13.8320 mL
10 mM 0.2766 mL 1.3832 mL 2.7664 mL 6.9160 mL
15 mM 0.1844 mL 0.9221 mL 1.8443 mL 4.6107 mL
20 mM 0.1383 mL 0.6916 mL 1.3832 mL 3.4580 mL
25 mM 0.1107 mL 0.5533 mL 1.1066 mL 2.7664 mL
30 mM 0.0922 mL 0.4611 mL 0.9221 mL 2.3053 mL
40 mM 0.0692 mL 0.3458 mL 0.6916 mL 1.7290 mL
50 mM 0.0553 mL 0.2766 mL 0.5533 mL 1.3832 mL
60 mM 0.0461 mL 0.2305 mL 0.4611 mL 1.1527 mL
80 mM 0.0346 mL 0.1729 mL 0.3458 mL 0.8645 mL
100 mM 0.0277 mL 0.1383 mL 0.2766 mL 0.6916 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:

PHA-793887718630-59-2PHA793887PHA 793887CDKApoptosisCyclin dependent kinaseInhibitorinhibitorinhibit

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