Palbociclib|571190-30-2|(帕博西尼; PD 0332991)-陌孚医药/Medlife

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Palbociclib (Synonyms: 帕博西尼; PD 0332991)

目录号: PL05086 纯度: ≥99%

CAS No. :571190-30-2

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中文名称	Palbociclib
中文别名	6-乙酰基-8-环戊基-5-甲基-2-[[5-(哌嗪-1-基)吡啶-2-基]氨基]-8H-吡啶并[2,3-d]嘧啶-7-酮;帕博西尼;帕布昔利布;6-乙酰基-8-环戊基-5-甲基-2-[[5-(1-哌嗪基)-2-吡啶基]氨基]-吡啶并[2,3-d]嘧啶-7(8H)-酮;6-乙酰基-8-环戊基-5-甲基-2-[[5-(哌嗪-1-基)吡啶-2-基]氨基]-;palbociclib杂质;阿伐那非;帕博西林;帕博西尼（帕布昔利布）;帕布昔利布（palbociclib）;帕布昔利布（帕泊昔布）杂质;依曲韦林;帕布昔利布杂质26
英文名称	Palbociclib
英文别名	6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(piperazin-1-yl)pyridin-2-yl]amino]-8H-pyrido[2,3-d]pyrimidin-7-one;PD 0332991;Palbociclib;6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one;6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(piperazin-1-yl)-pyridin-2-yl]amino]-8H-pyrido[2,3-d]pyrimidin-7-one;Flurbiprofen Axetil;OTAVA-BB 1115529;Palbocillib;Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-;PD 0332991 isethionate;DMXBA;GTS21 dihydrochloride;PD-0332991;PD332991;Palbociclib Impurity 26;6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one;Ibrance;PD991;PD0332991;Palbociclib(PD0332991);6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one;G9ZF61LE7G;PD 332991;6-ACETYL-8-CYCLOPENTYL-5-METHYL-2-[(5-PIPERAZIN-1-YLPYRIDIN-2-YL)AMINO]PYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONE;6-Acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-y
Cas No.	571190-30-2
分子式	C₂₄H₂₉N₇O₂
分子量	447.53
包装储存	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

产品详情

Palbociclib (PD 0332991) 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 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) is an orally active selective CDK4 and CDK6 inhibitor with IC 50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.

性状

Solid

IC50 & Target[1][2]

Cdk4/cyclin D3 9 nM (IC50) Cdk4/cyclin D1

体外研究(In Vitro)

Palbociclib (0-1 μM, 24 h) inhibits Rb Phosphorylation at Ser in MDA-MB-435 cells with an IC50 value of 0.063 μM, and obtains similar effects on both Ser and Ser phosphorylation in the Colo-205 colon carcinoma.
Palbociclib (0-10 μM, 24 h) arrests MDA-MB-453 cells exclusively in G1 phase.
Palbociclib (500 nM, 7 days) increases expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells.
Palbociclib (0-1 μM, 6 days) inhibits growth of several luminal ER-positive as well as HER2-amplified breast cancer cell lines, with IC50 values ranging from 4 nM to 1 μM.
Palbociclib (0-1 μM, 3 days) inhibits the proliferation of human liver cancer cell lines with IC50 values ranging from 0.01 μM to 3.49 μM, and induces a reversible cell cycle arrest. has not in

体内研究(In Vivo)

Palbociclib (oral adminstration, 75 or 150 mg/kg, daily for 14 days) produces rapid tumor regressions and delays tumor growth.
Palbociclib (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.
Palbociclib (oral administration, 100 mg/kg, daily for 1 week) has potent antitumour effects in genetically engineered mosaic mouse model of liver cancer. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

ClinicalTrial

参考文献

[1]. Fry DW, et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38.
[2]. Goel S, et al. CDK4/6 inhibition triggers anti-tumour immunity. Nature. 2017 Aug 24;548(7668):471-475.
[3]. Richard S Finn,

溶解度数据	In Vitro: DMSO : 25 mg/mL (55.86 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 60°C)0.1 M HCL : 25 mg/mL (55.86 mM; ultrasonic and adjust pH to 4 with 0.1 M HCL)H₂O : 0.1 mg/mL (0.22 mM; Need ultrasonic)

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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