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Palbociclib monohydrochloride
本半岛bd体育手机客户端 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。
Palbociclib monohydrochloride图片
CAS NO: 827022-32-2
包装与价格：
包装 价格(元)
10 mM * 1 mL in Water 电议
5mg 电议
10mg 电议
50mg 电议
100mg 电议
200mg 电议
500mg 电议
1 g 电议
5 g 电议

半岛bd体育手机客户端 名称
PD 0332991 monohydrochloride
半岛bd体育手机客户端 介绍
Palbociclib (PD 0332991) monohydrochloride 是一种具有口服活性的 CDK4和 CDK6选择性抑制剂， IC50值分别为 11 nM 和16 nM。Palbociclib monohydrochloride 对癌细胞具有抗增殖活性，并诱导其细胞周期阻滞，可用于 HR 阳性和 HER2 阴性乳腺癌，以及肝细胞癌的相关研究。
生物活性

Palbociclib (PD 0332991) monohydrochloride is an orally active selectiveCDK4andCDK6inhibitor withIC50values of 11 and 16 nM, respectively. Palbociclib monohydrochloride has potent anti-proliferative activity and inducescell cycle arrestincancercells, which can be used in the research of HR-positive and HER2-negative breastcancerand hepatocellular carcinoma[1][3][4].
IC50& Target[1]

Cdk4/cyclin D3

9 nM (IC50)

Cdk4/cyclin D1

11 nM (IC50)

Cdk6/cyclin D2

16 nM (IC50)

DYRK1A

2000 nM (IC50)

MAPK

8000 nM (IC50)
体外研究
(In Vitro)

Palbociclib monohydrochloride (0-1 μM, 24 h) inhibits Rb Phosphorylation at Ser795in MDA-MB-435 cells with an IC50value of 0.063 μM, and obtains similar effects on both Ser780and Ser795phosphorylation in the Colo-205 colon carcinoma[1].
Palbociclib monohydrochloride (0-10 μM, 24 h) arrests MDA-MB-453 cells exclusively in G1 phase[1].
Palbociclib monohydrochloride (500 nM, 7 days) increases expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells[2].
Palbociclib monohydrochloride (0-1 μM, 6 days) inhibits growth of several luminal ER-positive as well as HER2-amplified breast cancer cell lines, with IC50values ranging from 4 nM to 1 μM[3].
Palbociclib monohydrochloride (0-1 μM, 3 days) inhibits the proliferation of human liver cancer cell lines with IC50values ranging from 0.01 μM to 3.49 μM, and induces a reversible cell cycle arrest[4].

Cell Cycle Analysis[1]

Cell Line: MDA-MB-453 cells
Concentration: 0-1 μM
Incubation Time: 24 h
Result: Arrested MDA-MB-453 cells in G1.

Cell Proliferation Assay[3]

Cell Line: ER-positive as well as HER2-amplified breast cancer cell lines (MDA-MB-175, ZR-75-30, CAMA-1, etc.)
Concentration: 0-10 μM
Incubation Time: 6 days
Result: Inhibited growth of luminal ER-positive as well as HER2-amplified breast cancer cell lines.
体内研究
(In Vivo)

Palbociclib monohydrochloride (oral adminstration, 75 or 150 mg/kg, daily for 14 days) produces rapid tumor regressions and delays tumor growth[1].
Palbociclib monohydrochloride (oral adminstration, 90 mg/kg, daily for 12 days) reduces Treg numbers and the Treg:CD8 ratio in the spleen and lymph nodes in tumor-free mice, demonstrating the tumor-independent effects[2].
Palbociclib monohydrochloride (oral administration, 100 mg/kg, daily for 1 week) has potent antitumour effects in genetically engineered mosaic mouse model of liver cancer[4].

Animal Model: Mice bearing Colo-205 colon carcinoma xenografts (p16 deleted)[1]
Dosage: 75, 150 mg/kg, daily for 14 days
Administration: Oral adminstration
Result: Produced rapid tumor regressions and a corresponding tumor growth delay of ~50 days.
Animal Model: Tumor-free female FVB mice[2]
Dosage: 90 mg/kg (diluted in 50 nM sodium D-lactate), daily for 12 days
Administration: Oral adminstration
Result: Reduced total thymic mass and immature CD4+and CD8+double-positive thymocytes, and increased the fractions of CD4+and CD8+single-positive thymocytes.
Animal Model: Genetically engineered mosaic mouse model of liver cancer (Myc;p53-sgRNA)[4]
Dosage: 100 mg/kg, daily for 1 week.
Administration: Oral adminstration
Result: Decreased the luminescence signal in liver and delayed tumour growth.
Clinical Trial
分子量

483.99
性状

Solid
Formula

C24H30ClN7O2
CAS 号

827022-32-2
中文名称

帕布昔利布杂质75
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro:

H2O : 7.14 mg/mL(14.75 mM;ultrasonic and warming and heat to 60℃)

DMSO : 4.63 mg/mL(9.57 mM;ultrasonic and warming and heat to 80℃)

配制储备液
浓度溶剂体积质量 1 mg 5 mg 10 mg
1 mM 2.0662 mL 10.3308 mL 20.6616 mL
5 mM 0.4132 mL 2.0662 mL 4.1323 mL
10 mM 0.2066 mL 1.0331 mL 2.0662 mL
*

请根据半岛bd体育手机客户端 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半岛bd体育手机客户端 失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-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： 0.5%HPMC1%Tween80

    Solubility: 20 mg/mL (41.32 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： Lactic acid buffer (50 mM, pH 4.0)

    Solubility: 4.17 mg/mL (8.62 mM); Clear solution; Need ultrasonic

  • 3.

    请依序添加每种溶剂： 10% DMSO40%PEG3005%Tween-8045% saline

    Solubility: ≥ 0.54 mg/mL (1.12 mM); Clear solution

    此方案可获得 ≥ 0.54 mg/mL (1.12 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 5.4 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
  • 4.

    请依序添加每种溶剂： 10% DMSO90% (20%SBE-β-CDin saline)

    Solubility: ≥ 0.54 mg/mL (1.12 mM); Clear solution

    此方案可获得 ≥ 0.54 mg/mL (1.12 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 5.4 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。
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