2. Cell Cycle/DNA Damage
  3. CDK
  4. Palbociclib hydrochloride

Palbociclib hydrochloride  (Synonyms: PD-0332991 hydrochloride)

目录号: HY-50767C 纯度: 99.93%
COA 产品使用指南 技术支持

Palbociclib (PD 0332991) hydrochloride 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 hydrochloride 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。

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Palbociclib hydrochloride Chemical Structure

Palbociclib hydrochloride Chemical Structure

CAS No. : 571189-11-2

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10 mg ￥700
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100 mg ￥1250
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500 mg ￥1700
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1 g ￥2200
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Customer Review

Other Forms of Palbociclib hydrochloride:

Palbociclib hydrochloride 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 170 篇科研文献

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IHC
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    Palbociclib hydrochloride purchased from MCE. Usage Cited in: Life Sciences. 2023 Apr 1, 121652.

    Palbociclib (1 µM; 48 h) decreases the expression of PPARγ in SVFs.

    Palbociclib hydrochloride purchased from MCE. Usage Cited in: EBioMedicine. 2019 May;43:225-237.  [Abstract]

    Representative images of immunohistochemical staining for proteins as indicated in A2780 xenografted tumors (n=6 per treatment group) treated with AZD2281 and Palbociclib either as single-agents or in combination for 4 days.

    Palbociclib hydrochloride purchased from MCE. Usage Cited in: Nat Commun. 2018 Oct 9;9(1):4180.  [Abstract]

    MCF7, MCF7-LEM4, and MCF7-TAMR cells are treated with 5% DCC-FBS (vehicle), 4-OHT (1 μM), PD0332991 (PD) (0.2 μM), or a combination of 4-OHT and PD0332991. Immunoblots of lysates from cells are tested.

    Palbociclib hydrochloride purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Sep 20;37(1):233.  [Abstract]

    Western blot of the nine cell cycle-related proteins in C666-1 cells treated with different concentrations of GEM (0.1, 1, and 10 μM) and PAL (0.1, 1, and 5 μM) after 48 h.

    Palbociclib hydrochloride purchased from MCE. Usage Cited in: Eur J Cancer. 2018 Oct;102:10-22.  [Abstract]

    Head-to-head comparison of the effect of Palbociclib and Ribociclib on DNA damage response (DDR) signalling in liver cancer cells.

    Palbociclib hydrochloride purchased from MCE. Usage Cited in: Nature. 2017 Jun 15;546(7658):426-430.  [Abstract]

    In vitro kinase reactions using immunoprecipitated endogenous CDK6 and recombinant PFKP or PKM2 with or without Palbociclib (PALBO). 32P-PFKP and 32P-PKM2 denote phosphorylated proteins, IB, immunoblotting.

    Palbociclib hydrochloride purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.  [Abstract]

    Inhibition of AMPK reverses Palbociclib-induced autophagy and apoptosis. Hep3B cells are incubated with AMPK inhibitor (Compound C, 2.5 μM) for 4 h and then treated with Palbociclib for 24 h. Apoptotic cells are determined by flow cytometry.

    Palbociclib hydrochloride purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.  [Abstract]

    Effects of Palbociclib on CDK4/6-Rb pathway. HCC cells are treated with different doses of Palbociclib for 24 h, and then, the cells are subjected to western blot analysis.

    Palbociclib hydrochloride purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.  [Abstract]

    Effects of CDK4/6 inhibitors on AMPK phosphorylation and apoptosis-related signals. After 24 h of drug treatment, the cells are subjected to western blot analysis. AMPK phosphorylation level is quantified by the ratio of band intensities of phospho-AMPKα vs. AMPKα.

    Palbociclib hydrochloride purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2017 Nov 20;1865(2):354-363.  [Abstract]

    LAPC-4 cells are grown in charcoal-stripped serum medium (CSS) for 24 hours and then stimulated by R1881 alone or with different doses of Palbociclib (PD). Palbociclib is added 30 min before androgen treatment. Cellular expression of all proteins is detected by immunoblotting analysis. β-actin is included as a control for protein loading.

    查看 CDK 亚型特异性产品:

    查看所有亚型
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Palbociclib (PD 0332991) hydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib hydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib hydrochloride can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma[1][3][4].

    IC50 & Target[1]

    DYRK1A

    2000 nM (IC50)

    MAPK

    8000 nM (IC50)

    Cdk4/cyclin D3

    9 nM (IC50)

    Cdk4/cyclin D1

    11 nM (IC50)

    Cdk6/cyclin D2

    16 nM (IC50)

    体外研究
    (In Vitro)

    Palbociclib (0-1 μM; 24 小时) 盐酸盐在 MDA-MB-435 细胞中抑制视网膜母细胞瘤磷酸化 (Ser795) ，其 IC50 为 0.063 μM，并在 Colo-205 结肠癌细胞中对 Ser780 和 Ser795 磷酸化产生类似效果[1].
    Palbociclib (0-10 μM; 24 小时) 盐酸盐使 MDA-MB-453 细胞停滞于 G1 期[1].
    Palbociclib (500 nM; 7 天) 盐酸盐增加 MDA-MB-453 和 MDA-MB-361 细胞中 H2d1、H2k1 和 B2m 的表达[2].
    Palbociclib (0-1 μM; 6 天) 盐酸盐抑制多种 ER 阳性和 HER2 扩增乳腺癌细胞系的生长，IC50 值范围为 4 nM 至 1 μM[3].
    Palbociclib (0-1 μM; 3 天) 盐酸盐抑制人肝癌细胞系的增殖，其 IC50 值范围为 0.01 μM 至 3.49 μM，并诱导可逆的细胞周期停滞[4].

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

    Palbociclib hydrochloride 相关抗体:

    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: 0-1 μM
    Incubation Time: 6 days
    Result: Inhibited growth of luminal ER-positive as well as HER2-amplified breast cancer cell lines.

    Cell Cycle Analysissup>[1]

    Cell Line: MDA-MB-453 cells
    Concentration: 0-1 μM
    Incubation Time: 24 h
    Result: Arrested MDA-MB-453 cells in G1.
    体内研究
    (In Vivo)

    Palbociclib (口服给药，75 或 150 mg/kg，每天 1 次，共 14 天) 盐酸盐可快速使肿瘤退缩并延缓肿瘤生长[1]。
    Palbociclib (口服给药，90 mg/kg，每天 1 次，共 12 天) 盐酸盐可减少无肿瘤小鼠脾脏和淋巴结中的 Treg 数量及 Treg 比例，证明其具有独立于肿瘤的作用[2]。
    Palbociclib (口服给药，100 mg/kg，每天 1 次，共 1 周) 盐酸盐在基因工程化肝癌镶嵌小鼠模型中表现出强大的抗肿瘤效果[4]。

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

    Animal Model: Mice bearing Colo-205 colon carcinoma xenografts (p16 deleted)[1]
    Dosage: 75, 150 mg/kg
    Administration: Oral administration; daily for 14 days
    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
    Administration: Oral administration; daily for 12 days
    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
    Administration: Oral administration; daily for 1 week
    Result: Decreased the luminescence signal in liver and delayed tumour growth.
    Clinical Trial
    分子量

    514.99

    Formula

    C24H30ClN7O2
    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    中文名称

    帕波西利盐酸盐
    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
    细胞实验： 

    H2O 中的溶解度 : 2 mg/mL (3.88 mM; 超声助溶 (<60°C))

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.9418 mL 9.7089 mL 19.4179 mL
    5 mM --- --- ---
    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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    • 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
    计算结果
    工作液所需浓度 : mg/mL
    您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.93%

    COA (292 KB) RP-HPLC (468 KB)

    产品使用指南 (1538 KB)
    参考文献

    Palbociclib hydrochloride 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O 1 mM 1.9418 mL 9.7089 mL 19.4179 mL 48.5446 mL

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    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:

    Palbociclib571189-11-2PD-0332991帕波西利盐酸盐PD0332991PD 0332991CDKCyclin dependent kinaseBreast cancerhepatocellular carcinomaHCCestrogen receptorERHER2cell cycleInhibitorinhibitorinhibit

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