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

Palbociclib isethionate  (Synonyms: 帕博西尼羥乙基磺酸鹽; PD 0332991 isethionate)

目錄號: HY-A0065 純度: 99.99%
COA 產(chǎn)品使用指南

Palbociclib (PD 0332991) isethionate 是一種具有口服活性的 CDK4 和 CDK6 選擇性抑制劑，IC50 值分別為 11 nM 和16 nM。Palbociclib dihydrochloride 對癌細(xì)胞具有抗增殖活性，并誘導(dǎo)其細(xì)胞周期阻滯，可用于 HR 陽性和 HER2 陰性乳腺癌，以及肝細(xì)胞癌的相關(guān)研究。

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Palbociclib isethionate Chemical Structure

Palbociclib isethionate Chemical Structure

CAS No. : 827022-33-3

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥760
In-stock
1 mg ￥250
In-stock
5 mg ￥550
In-stock
10 mg ￥800
In-stock
50 mg ￥1620
In-stock
100 mg ￥2340
In-stock
200 mg ￥2880
In-stock
500 mg ￥5940
In-stock
1 g   詢價(jià)  
5 g   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Palbociclib isethionate:

MCE 顧客使用本產(chǎn)品發(fā)表的 154 篇科研文獻(xiàn)

WB
IHC
IF

    Palbociclib isethionate 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 isethionate 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 isethionate 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 isethionate 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 isethionate 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 isethionate 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 isethionate 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 isethionate 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 isethionate 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 isethionate 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.

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Palbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib isethionate 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[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)

    體外研究
    (In Vitro)

    Palbociclib isethionate dihydrochloride (0-1 μM，24 h) 抑制 MDA-MB-435 細(xì)胞中 Ser795 位點(diǎn)的 Rb 磷酸化，IC50 值為 0.063 μM，并獲得類似的結(jié)果對 Colo -205 結(jié)腸癌中 Ser780 和 Ser795 磷酸化的影響[1]。
    Palbociclib isethionate dihydrochloride (0-10 μM，24 小時(shí)) 僅在 G1 期阻止 MDA-MB-453 細(xì)胞[1]。
    Palbociclib isethionate dihydrochloride (500 nM，7 天) 增加同源基因的表達(dá) (H2d1、H2k1，和 B2m) 在 MDA-MB-453 和 MDA-MB-361 細(xì)胞中[2]。
    Palbociclib isethionate dihydrochloride (0-1 μM，6 天) 抑制幾種管腔 ER-陽性和 HER2 擴(kuò)增的乳腺癌細(xì)胞系，IC50 值范圍為 4 nM-1 μM[3]。
    Palbociclib isethionate dihydrochloride (0-1 μM，3 天) 抑制人肝癌細(xì)胞系的增殖，IC50 值范圍為 0.01 μM 至 3.49 μM，并誘導(dǎo)可逆的細(xì)胞周期停滯[4]。

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

    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.
    體內(nèi)研究
    (In Vivo)

    Palbociclib isethionate isethionate (口服，75 或 150 mg/kg，每日一次，持續(xù) 14 天) 可使腫瘤快速消退并延緩腫瘤生長[1]。
    Palbociclib isethionate isethionate (口服，90 mg/kg kg，每日一次，持續(xù) 12 天) 減少無腫瘤小鼠脾臟和淋巴結(jié)中的 Treg 數(shù)量和 Treg：CD8 比率，證明了腫瘤非依賴性效應(yīng)[2]。
    Palbociclib isethionate isethionate (口服給藥，100 mg/kg，每日一次，持續(xù) 1 周) 在肝癌基因工程鑲嵌小鼠模型中具有有效的抗腫瘤作用[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, 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

    573.66

    Formula

    C26H35N7O6S
    CAS 號
    性狀

    固體

    顏色

    Light yellow to yellow

    中文名稱

    帕布昔利布雜質(zhì)74
    運(yùn)輸條件

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

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    H2O 中的溶解度 : 50 mg/mL (87.16 mM; 超聲助溶)

    DMSO 中的溶解度 : 10 mg/mL (17.43 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 1.7432 mL 8.7160 mL 17.4319 mL
    5 mM 0.3486 mL 1.7432 mL 3.4864 mL
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C儲存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，請?jiān)?個(gè)月內(nèi)使用。

    * 備注：如您選擇水作為儲備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn)：

    請根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 1 mg/mL (1.74 mM); 澄清溶液

      此方案可獲得 ≥ 1 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 10.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      20% SBE-β-CD in Saline 的配制（4°C，儲存一周）：2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
    動(dòng)物溶解方案計(jì)算器
    請輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    該產(chǎn)品水溶性佳，請具體參考實(shí)測 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
    您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    純度 & 產(chǎn)品資料

    純度: 99.99%

    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C儲存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，請?jiān)?個(gè)月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 1.7432 mL 8.7160 mL 17.4319 mL 43.5798 mL
    5 mM 0.3486 mL 1.7432 mL 3.4864 mL 8.7160 mL
    10 mM 0.1743 mL 0.8716 mL 1.7432 mL 4.3580 mL
    15 mM 0.1162 mL 0.5811 mL 1.1621 mL 2.9053 mL
    H2O 20 mM 0.0872 mL 0.4358 mL 0.8716 mL 2.1790 mL
    25 mM 0.0697 mL 0.3486 mL 0.6973 mL 1.7432 mL
    30 mM 0.0581 mL 0.2905 mL 0.5811 mL 1.4527 mL
    40 mM 0.0436 mL 0.2179 mL 0.4358 mL 1.0895 mL
    50 mM 0.0349 mL 0.1743 mL 0.3486 mL 0.8716 mL
    60 mM 0.0291 mL 0.1453 mL 0.2905 mL 0.7263 mL
    80 mM 0.0218 mL 0.1089 mL 0.2179 mL 0.5447 mL

    * 備注：如您選擇水作為儲備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

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    • 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.

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    產(chǎn)品名稱：
    Palbociclib isethionate
    目錄號：
    HY-A0065
    需求量：