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) |
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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. |
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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. |
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| 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 | 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 (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%HPMC 1%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% DMSO 40%PEG300 5%Tween-80 45% 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。 4. 请依序添加每种溶剂： 10% DMSO 90% (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。 *以上所有助溶剂都可在本网站选购。
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