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Palbociclib

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Chemical Structure| 571190-30-2 同义名 : 帕布昔利布 ;PD 0332991
CAS号 : 571190-30-2
货号 : A295334
分子式 : C24H29N7O2
纯度 : 99%
分子量 : 447.533
MDL号 : MFCD11840850
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 10 mg/mL(22.34 mM)，配合低频超声，水浴加热至45℃，并调节pH至4，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

0.1 M HCL: 25 mg/mL(55.86 mM)，配合低频超声，并调节pH至4
动物实验配方：
生物活性
靶点

  • CDK4

    CDK4/CyclinD3, IC50:9 nM

    CDK4/CyclinD1, IC50:11 nM

  • CDK6

    CDK6/CyclinD2, IC50:15 nM
描述 Palbociclib (PD 0332991) is an orally active, selective inhibitor of CDK4 and CDK6, showing IC50 values of 11 nM and 16 nM respectively. It exhibits strong anti-proliferative properties and is capable of inducing cell cycle arrest in cancer cells. This makes it a valuable agent in the study of HR-positive and HER2-negative breast cancer as well as hepatocellular carcinoma[1].[3].[4].
作用机制 Palbociclib can inhibit CDK4/6 in an ATP-competitive manner through its pyridopyrimidine structure[1][3][4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03007979 Breast Cancer ... 展开 >> Breast Carcinoma Cancer of Breast Malignant Tumor of Breast 收起 << Phase 2 Recruiting June 30, 2021 United States, Missouri ... 展开 >> Washington University School of Medicine Recruiting Saint Louis, Missouri, United States, 63110 Contact: Cynthia X Ma, M.D., Ph.D.    314-362-9383    cynthiaxma@wustl.edu    Principal Investigator: Cynthia X Ma, M.D., Ph.D.          Sub-Investigator: Foluso O Ademuyiwa, M.D.          Sub-Investigator: Ron Bose, M.D., Ph.D.          Sub-Investigator: Mathew Cherian, M.D.          Sub-Investigator: Ashley Frith, M.D.          Sub-Investigator: Leonel Hernandez Aya, M.D.          Sub-Investigator: Peter Oppelt, M.D.          Sub-Investigator: Haeseong Park, M.D.          Sub-Investigator: Caron Rigden, M.D.          Sub-Investigator: Rama Suresh, M.D.          Sub-Investigator: Katherine Weilbaecher, M.D.          Sub-Investigator: Rebecca Aft, M.D., Ph.D.          Sub-Investigator: Lindsay Peterson, M.D.          United States, Nebraska University of Nebraska Recruiting Lincoln, Nebraska, United States, 68588 Contact: Jairam Krishnamurthy, M.D.    402-559-1800    jairam.krishnamurthy@unmc.edu    Principal Investigator: Jairam Krishnamurthy, M.D.          Sub-Investigator: Kenneth Cowan, M.D.          Sub-Investigator: Elizabeth Reed, M.D.          Sub-Investigator: Pavankumar Tandra, M.D. 收起 <<
NCT01907607 Advanced Gastrointestinal Stro... 展开 >>mal Tumors 收起 << Phase 2 Active, not recruiting April 2019 France ... 展开 >> Institut Bergonié Bordeaux, Gironde, France, 33076 Centre Georges-Francois Leclerc Dijon, France, 21079 Centre Oscar Lambret Lille, France, 59020 Centre Léon Bérard Lyon, France, 69373 Hôpital de la Timone - AP-HM Marseille, France, 13385 Centre René Gauducheau Nantes, France, 44805 Hôpital Saint-Antoine (AP-HP) Paris, France, 75571 CHU de REIMS - Hôpital Robert Debré Reims, France, 51092 Institut Gustave Roussy Villejuif, France, 94800 收起 <<
NCT03304080 Breast Neoplasms ... 展开 >> Breast Diseases 收起 << Phase 1 Phase 2 Recruiting November 1, 2019 United States, New York ... 展开 >> Mount Sinai Beth Israel Comprehensive Cancer Center West Recruiting New York, New York, United States, 10011 Contact: Paula Klein, MD    212-604-6021    paula.klein@mountsinai.org    Perlmutter Cancer Center NYU Langone Not yet recruiting New York, New York, United States, 10016 Contact: Sylvia Adams, MD    212-731-5795    sylvia.adams@nyumc.org    Sub-Investigator: Sylvia Adams, MD          Mount Sinai West Recruiting New York, New York, United States, 10019 Contact: Krystal Cascetta, MD    212-523-8692    krystal.cascetta@mountsinai.org    New York Presbyterian Herbert Irving Comprehensive Cancer Center at Columbia University Not yet recruiting New York, New York, United States, 10032 Contact: Kevin Kalinsky, MD    212-305-1945    Kk2693@columbia.edu    New York Presbyterian Meyer Cancer Center at Weill Cornell Not yet recruiting New York, New York, United States, 10065 Contact: Eleni Andreopoulou, MD    646-962-9888    ela9082@med.cornell.edu 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.23mL

0.45mL

0.22mL

11.17mL

2.23mL

1.12mL

22.34mL

4.47mL

2.23mL
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, et al. PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro. Breast Cancer Res. 2009;11(5):R77.

[4]Bollard J, et al. Palbociclib (PD-0332991), a selective CDK4/6 inhibitor, restricts tumour growth in preclinical models of hepatocellular carcinoma. Gut. 2017 Jul;66(7):1286-1296.