1. Cell Cycle/DNA Damage
  2. CDK
  3. Palbociclib

Palbociclib  (Synonyms: PD 0332991)

Cat. No.: HY-50767 Purity: 99.76%
SDS COA Handling Instructions

Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 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.

For research use only. We do not sell to patients.

Palbociclib Chemical Structure

Palbociclib Chemical Structure

CAS No. : 571190-30-2

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10 mg USD 84 In-stock
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100 mg USD 132 In-stock
500 mg USD 312 In-stock
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Customer Review

Based on 167 publication(s) in Google Scholar

Top Publications Citing Use of Products

157 Publications Citing Use of MCE Palbociclib

WB
IHC
IF

    Palbociclib purchased from MedChemExpress. Usage Cited in: Life Sciences. 2023 Apr 1, 121652.

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

    Palbociclib purchased from MedChemExpress. 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 purchased from MedChemExpress. 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 purchased from MedChemExpress. 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 purchased from MedChemExpress. 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 purchased from MedChemExpress. 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 purchased from MedChemExpress. 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 purchased from MedChemExpress. 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 purchased from MedChemExpress. 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 purchased from MedChemExpress. 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.
    • Biological Activity

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    Description

    Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 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[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)

    Cellular Effect
    Cell Line Type Value Description References
    A2780 GI50
    0.032 μM
    Compound: Palbociclib
    Growth inhibition of human A2780 cells after 72 hrs by resazurin or MTT assay
    Growth inhibition of human A2780 cells after 72 hrs by resazurin or MTT assay
    [PMID: 28156111]
    A549 IC50
    > 10 μM
    Compound: Palbociclib
    Antiproliferative activity against human A549 cells assessed as growth inhibition by CCK-8 assay
    Antiproliferative activity against human A549 cells assessed as growth inhibition by CCK-8 assay
    [PMID: 36130661]
    A549 EC50
    0.4 μM
    Compound: Palbociclib
    Growth inhibition of human A549 cells measured after 72 hrs by propidium iodide staining based fluorescence assay
    Growth inhibition of human A549 cells measured after 72 hrs by propidium iodide staining based fluorescence assay
    [PMID: 30665142]
    A549 IC50
    1.32 μM
    Compound: V
    Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 30572179]
    A549 IC50
    8.07 μM
    Compound: Palbociclib
    Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    [PMID: 37011445]
    A549 IC50
    9.4 μM
    Compound: Palbociclib
    Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay
    [PMID: 34624191]
    BPH-1 GI50
    7.442 μM
    Compound: Palbociclib
    Growth inhibition of nontransformed human BPH1 cells after 72 hrs by resazurin or MTT assay
    Growth inhibition of nontransformed human BPH1 cells after 72 hrs by resazurin or MTT assay
    [PMID: 28156111]
    Calu-1 EC50
    33 μM
    Compound: Palbociclib
    Growth inhibition of human Calu1 cells measured after 72 hrs by propidium iodide staining based fluorescence assay
    Growth inhibition of human Calu1 cells measured after 72 hrs by propidium iodide staining based fluorescence assay
    [PMID: 30665142]
    COLO 205 IC50
    0.036 μM
    Compound: Palbociclib
    Antiproliferative activity against Rb-positive human COLO205 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis
    Antiproliferative activity against Rb-positive human COLO205 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis
    [PMID: 24641103]
    COLO 205 IC50
    300.6 nM
    Compound: Palbociclib
    Antiproliferative activity against human COLO 205 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay
    Antiproliferative activity against human COLO 205 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay
    [PMID: 32200202]
    CWR22R GI50
    0.435 μM
    Compound: Palbociclib
    Antiproliferative activity against human 22Rv1 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human 22Rv1 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay
    [PMID: 34875521]
    DU-145 GI50
    5.792 μM
    Compound: Palbociclib
    Growth inhibition of human DU145 cells after 72 hrs by resazurin or MTT assay
    Growth inhibition of human DU145 cells after 72 hrs by resazurin or MTT assay
    [PMID: 28156111]
    DU-145 IC50
    7.5 μM
    Compound: 31, PD-0332991
    Cytotoxicity against human DU145 cells after 96 hrs by Cell-Titer Blue assay
    Cytotoxicity against human DU145 cells after 96 hrs by Cell-Titer Blue assay
    [PMID: 24417566]
    HCC38 EC50
    1.4 μM
    Compound: 51
    Anticancer activity against human HCC38 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis
    Anticancer activity against human HCC38 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis
    [PMID: 33650861]
    HCT-116 IC50
    > 10 μM
    Compound: Palbociclib
    Antiproliferative activity against human HCT-116 cells assessed as growth inhibition by CCK-8 assay
    Antiproliferative activity against human HCT-116 cells assessed as growth inhibition by CCK-8 assay
    [PMID: 36130661]
    HCT-116 IC50
    7.11 μM
    Compound: 1
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    [PMID: 33197548]
    HCT-116 IC50
    8.9 μM
    Compound: V
    Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 30572179]
    HEK293 GI50
    9.608 μM
    Compound: Palbociclib
    Antiproliferative activity against human HEK293 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human HEK293 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay
    [PMID: 34875521]
    HeLa IC50
    > 10 μM
    Compound: Palbociclib
    Antiproliferative activity against human HeLa cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human HeLa cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay
    [PMID: 34624191]
    HeLa IC50
    13.3 μM
    Compound: 1
    Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    [PMID: 33197548]
    HepG2 IC50
    > 10 μM
    Compound: Palbociclib
    Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay
    [PMID: 34624191]
    HepG2 IC50
    9.92 μM
    Compound: Palbociclib
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    [PMID: 37011445]
    HL-60 GI50
    29.17 μM
    Compound: Palbociclib
    Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
    [PMID: 34958208]
    HL-60 GI50
    3.498 μM
    Compound: Palbociclib
    Antiproliferative activity against human HL-60 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human HL-60 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay
    [PMID: 34875521]
    HT-29 IC50
    3.56 μM
    Compound: 1
    Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    [PMID: 33197548]
    HT-29 IC50
    9.3 μM
    Compound: Palbociclib
    Antiproliferative activity against human HT-29 cells assessed as growth inhibition by CCK-8 assay
    Antiproliferative activity against human HT-29 cells assessed as growth inhibition by CCK-8 assay
    [PMID: 36130661]
    JeKo-1 GI50
    30 μM
    Compound: Palbociclib
    Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    [PMID: 30802730]
    Jurkat GI50
    > 100 μM
    Compound: Palbociclib
    Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
    [PMID: 32129996]
    K562 IC50
    > 10 μM
    Compound: Palbociclib
    Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay
    [PMID: 34624191]
    K562 IC50
    2 μM
    Compound: 31, PD-0332991
    Cytotoxicity against human K562 cells after 96 hrs by Cell-Titer Blue assay
    Cytotoxicity against human K562 cells after 96 hrs by Cell-Titer Blue assay
    [PMID: 24417566]
    K562 GI50
    2.455 μM
    Compound: Palbociclib
    Antiproliferative activity against human K562 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human K562 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay
    [PMID: 34875521]
    L02 GI50
    > 100 μM
    Compound: Palbociclib
    Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
    Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
    [PMID: 32129996]
    LNCaP C4-2B GI50
    4.15 μM
    Compound: Palbociclib
    Growth inhibition of human C4-2B cells after 72 hrs by resazurin or MTT assay
    Growth inhibition of human C4-2B cells after 72 hrs by resazurin or MTT assay
    [PMID: 28156111]
    MCF-10A GI50
    19.07 μM
    Compound: Palbociclib
    Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
    [PMID: 36350721]
    MCF7 IC50
    > 10 μM
    Compound: Palbociclib
    Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay
    [PMID: 34624191]
    MCF7 GI50
    > 100 μM
    Compound: Palbociclib
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
    [PMID: 32129996]
    MCF7 IC50
    0.34 μM
    Compound: PD0332991
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 33857728]
    MCF7 GI50
    0.557 μM
    Compound: Palbociclib
    Growth inhibition of human MCF7 cells after 72 hrs by resazurin or MTT assay
    Growth inhibition of human MCF7 cells after 72 hrs by resazurin or MTT assay
    [PMID: 28156111]
    MCF7 IC50
    0.78 μM
    Compound: Palbociclib
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    [PMID: 37011445]
    MCF7 IC50
    240 nM
    Compound: 1
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
    [PMID: 27448913]
    MCF7 GI50
    3.938 μM
    Compound: Palbociclib
    Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
    [PMID: 36350721]
    MCF7 IC50
    4.09 μM
    Compound: V
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 30572179]
    MCF7 IC50
    5.81 μM
    Compound: Palbociclib
    Antiproliferative activity against palbociclib-resistant human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against palbociclib-resistant human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    [PMID: 37011445]
    MDA-MB-231 GI50
    > 100 μM
    Compound: Palbociclib
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
    [PMID: 32129996]
    MDA-MB-231 EC50
    0.3 μM
    Compound: 51
    Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis
    Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis
    [PMID: 33650861]
    MDA-MB-231 IC50
    14.6 μM
    Compound: Paldociclib
    Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs
    Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs
    [PMID: 33139111]
    MDA-MB-231 IC50
    3.5 μM
    Compound: V
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 30572179]
    MDA-MB-231 GI50
    30 μM
    Compound: Palbociclib
    Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    [PMID: 30802730]
    MDA-MB-231 IC50
    4.72 μM
    Compound: PD0332991
    Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 33857728]
    MDA-MB-231 IC50
    5.62 μM
    Compound: Palbociclib
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    [PMID: 37011445]
    MDA-MB-231 IC50
    580 nM
    Compound: 1
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
    [PMID: 27448913]
    MDA-MB-231 IC50
    6.21 μM
    Compound: 1
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    [PMID: 33197548]
    MDA-MB-435 IC50
    0.16 μM
    Compound: 43(table 3)
    Inhibitory concentration was measured by the incorporation of [14C]-thymidine in (human breast carcinoma) MDA-MB-435 cell line
    Inhibitory concentration was measured by the incorporation of [14C]-thymidine in (human breast carcinoma) MDA-MB-435 cell line
    [PMID: 15801831]
    MDA-MB-435 IC50
    160 nM
    Compound: PD-0332991
    Antiproliferative activity against Rb-positive human MDA-MB-435 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis
    Antiproliferative activity against Rb-positive human MDA-MB-435 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis
    [PMID: 26115571]
    MDA-MB-436 EC50
    5 μM
    Compound: 51
    Anticancer activity against human MDA-MB-436 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis
    Anticancer activity against human MDA-MB-436 cells assessed as cell growth inhibition by crystal violet staining based haemocytometer analysis
    [PMID: 33650861]
    MDA-MB-453 GI50
    0.326 μM
    Compound: Palbociclib
    Growth inhibition of human MDA-MB-453 cells after 72 hrs by MTT assay
    Growth inhibition of human MDA-MB-453 cells after 72 hrs by MTT assay
    [PMID: 28156111]
    MDA-MB-453 IC50
    137 nM
    Compound: 1
    Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
    Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
    [PMID: 27448913]
    MDA-MB-453 IC50
    6.93 μM
    Compound: PD0332991
    Antiproliferative activity against human MDA-MB-453 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-453 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 33857728]
    MDA-MB-468 IC50
    > 3 μM
    Compound: PD-0332991
    Antiproliferative activity against Rb-negative human MDA-MB-468 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis
    Antiproliferative activity against Rb-negative human MDA-MB-468 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis
    [PMID: 26115571]
    MDA-MB-468 IC50
    > 3 μM
    Compound: 43(table 3)
    Inhibitory concentration was measured by the incorporation of [14C]thymidine in (human breast carcinoma) MDA-MB-468 cell line
    Inhibitory concentration was measured by the incorporation of [14C]thymidine in (human breast carcinoma) MDA-MB-468 cell line
    [PMID: 15801831]
    MDA-MB-468 EC50
    1.9 μM
    Compound: Palbociclib
    Growth inhibition of human MDA-MB-468 cells measured after 72 hrs by propidium iodide staining based fluorescence assay
    Growth inhibition of human MDA-MB-468 cells measured after 72 hrs by propidium iodide staining based fluorescence assay
    [PMID: 30665142]
    MDA-MB-468 GI50
    5.96 μM
    Compound: Palbociclib
    Growth inhibition of human MDA-MB-468 cells after 72 hrs by resazurin or MTT assay
    Growth inhibition of human MDA-MB-468 cells after 72 hrs by resazurin or MTT assay
    [PMID: 28156111]
    MDA-MB-468 IC50
    5424 nM
    Compound: Palbociclib
    Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay
    Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay
    [PMID: 32200202]
    MIA PaCa-2 IC50
    10.6 μM
    Compound: Palbociclib
    Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth by MTT assay
    Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth by MTT assay
    [PMID: 33316409]
    MM1.S IC50
    200 nM
    Compound: PD
    Antiproliferative activity against human MM1S cells after 84 hrs by CCK8 assay
    Antiproliferative activity against human MM1S cells after 84 hrs by CCK8 assay
    [PMID: 31330105]
    MOLM-13 IC50
    > 3 μM
    Compound: Palbociclib
    Inhibition of FLT3 ITD mutant in human MOLM13 cells assessed as inhibition of STAT5 phosphorylation at Tyr694 after 24 hrs
    Inhibition of FLT3 ITD mutant in human MOLM13 cells assessed as inhibition of STAT5 phosphorylation at Tyr694 after 24 hrs
    [PMID: 24641103]
    MOLM-13 GI50
    > 80 μM
    Compound: Palbociclib
    Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
    [PMID: 34958208]
    MOLM-13 IC50
    0.011 μM
    Compound: Palbociclib
    Inhibition of CDK4 in human MOLM13 cells assessed as inhibition of Rb phosphorylation at Ser780 after 24 hrs
    Inhibition of CDK4 in human MOLM13 cells assessed as inhibition of Rb phosphorylation at Ser780 after 24 hrs
    [PMID: 24641103]
    MOLM-13 GI50
    0.062 μM
    Compound: Palbociclib
    Growth inhibition of human MOLM13 cells after 72 hrs by resazurin or MTT assay
    Growth inhibition of human MOLM13 cells after 72 hrs by resazurin or MTT assay
    [PMID: 28156111]
    MOLM-13 IC50
    0.096 μM
    Compound: Palbociclib
    Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis
    Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis
    [PMID: 24641103]
    MOLM-13 IC50
    0.096 μM
    Compound: Palbociclib
    Antiproliferative activity against sorafenib-resistant human MOLM13 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis
    Antiproliferative activity against sorafenib-resistant human MOLM13 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis
    [PMID: 24641103]
    MRC5 GI50
    > 10 μM
    Compound: Palbociclib
    Growth inhibition of human MRC5 cells after 72 hrs by resazurin or MTT assay
    Growth inhibition of human MRC5 cells after 72 hrs by resazurin or MTT assay
    [PMID: 28156111]
    MV4-11 GI50
    0.05 μM
    Compound: Palbociclib
    Growth inhibition of human MV4-11 cells after 72 hrs by resazurin assay
    Growth inhibition of human MV4-11 cells after 72 hrs by resazurin assay
    [PMID: 28156111]
    NB-4 GI50
    0.066 μM
    Compound: Palbociclib
    Growth inhibition of human NB4 cells after 72 hrs by resazurin or MTT assay
    Growth inhibition of human NB4 cells after 72 hrs by resazurin or MTT assay
    [PMID: 28156111]
    NCI-H1299 IC50
    8.92 μM
    Compound: PD0332991
    Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 33857728]
    OVCAR-3 IC50
    > 3 μM
    Compound: 1
    Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 6 days by CyQuant assay
    Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 6 days by CyQuant assay
    [PMID: 34110834]
    PC-3 GI50
    0.071 μM
    Compound: Palbociclib
    Growth inhibition of human PC3 cells after 72 hrs by resazurin or MTT assay
    Growth inhibition of human PC3 cells after 72 hrs by resazurin or MTT assay
    [PMID: 28156111]
    PC-3 IC50
    2.2 μM
    Compound: V
    Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 30572179]
    Raji GI50
    30 μM
    Compound: Palbociclib
    Antiproliferative activity against human Raji cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    Antiproliferative activity against human Raji cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    [PMID: 30802730]
    RPMI-8226 GI50
    2.215 μM
    Compound: Palbociclib
    Antiproliferative activity against human RPMI-8226 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human RPMI-8226 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay
    [PMID: 34875521]
    Sf9 IC50
    > 10 μM
    Compound: Palbociclib
    Inhibition of human full length N-terminal GST-fused CDK2 (M1 to L298 residues)/human full length Cyclin-A2 (M1 to L432 residues) expressed in Sf9 cells using histone H1 as substrate measured after 1 hr by ADP-glo luminescence assay
    Inhibition of human full length N-terminal GST-fused CDK2 (M1 to L298 residues)/human full length Cyclin-A2 (M1 to L432 residues) expressed in Sf9 cells using histone H1 as substrate measured after 1 hr by ADP-glo luminescence assay
    [PMID: 30665142]
    Sf9 IC50
    > 10 μM
    Compound: Palbociclib
    Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    [PMID: 30234987]
    Sf9 IC50
    > 10 μM
    Compound: Palbociclib
    Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    [PMID: 30234987]
    Sf9 IC50
    > 100 μM
    Compound: Palbociclib
    Inhibition of recombinant human N-terminal GST/His6-tagged CDK1 (M1 to M297 residues)/CyclinB1 (M1 to V433 residues) expressed in Sf9 insect cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence assay
    Inhibition of recombinant human N-terminal GST/His6-tagged CDK1 (M1 to M297 residues)/CyclinB1 (M1 to V433 residues) expressed in Sf9 insect cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence assay
    [PMID: 30665142]
    Sf9 IC50
    > 100 μM
    Compound: Palbociclib
    Inhibition of N-terminal GST-HIS6 fusion protein tagged human full length CDK9 (M1 to F372 residues)/N-terminal HIS6-fused human Cyclin-T1 (M1 to K726 residues) expressed in Sf9 cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence as
    Inhibition of N-terminal GST-HIS6 fusion protein tagged human full length CDK9 (M1 to F372 residues)/N-terminal HIS6-fused human Cyclin-T1 (M1 to K726 residues) expressed in Sf9 cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence as
    [PMID: 30665142]
    Sf9 IC50
    0.005 μM
    Compound: Palbociclib
    Inhibition of recombinant human full-length N-terminal His-tagged CDK6/cyclinD3 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 60 mins by ADP-glo assay
    Inhibition of recombinant human full-length N-terminal His-tagged CDK6/cyclinD3 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 60 mins by ADP-glo assay
    [PMID: 32129996]
    Sf9 IC50
    0.013 μM
    Compound: Palbociclib
    Inhibition of recombinant human N-terminal GST-tagged CDK4 (S4 to E303 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence assay
    Inhibition of recombinant human N-terminal GST-tagged CDK4 (S4 to E303 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using RBCTF as substrate measured after 1 hr by ADP-glo luminescence assay
    [PMID: 30665142]
    Sf9 IC50
    0.013 μM
    Compound: Palbociclib
    Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    [PMID: 30234987]
    Sf9 IC50
    1.1 μM
    Compound: Palbociclib
    Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    [PMID: 30234987]
    Sf9 IC50
    1.207 μM
    Compound: Palbociclib
    Inhibition of recombinant human full-length N-terminal GST-tagged CDK9/cyclinK expressed in baculovirus infected Sf9 insect cells using PDKtide as substrate measured after 120 mins by ADP-glo assay
    Inhibition of recombinant human full-length N-terminal GST-tagged CDK9/cyclinK expressed in baculovirus infected Sf9 insect cells using PDKtide as substrate measured after 120 mins by ADP-glo assay
    [PMID: 32129996]
    Sf9 IC50
    8.75 μM
    Compound: Palbociclib
    Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA2 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 10 mins by ADP-glo assay
    Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA2 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 10 mins by ADP-glo assay
    [PMID: 32129996]
    Sf9 IC50
    9.1 μM
    Compound: Palbociclib
    Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    [PMID: 30234987]
    Sf9 IC50
    9.2 μM
    Compound: PD-0332991
    Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP
    Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP
    [PMID: 26851505]
    Sf9 IC50
    9.8 μM
    Compound: Palbociclib
    Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    [PMID: 30234987]
    SK-MEL19 GI50
    30 μM
    Compound: Palbociclib
    Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    [PMID: 30802730]
    T47D EC50
    0.35 μM
    Compound: Palbociclib
    Growth inhibition of human T47D cells measured after 72 hrs by propidium iodide staining based fluorescence assay
    Growth inhibition of human T47D cells measured after 72 hrs by propidium iodide staining based fluorescence assay
    [PMID: 30665142]
    T47D GI50
    1.056 μM
    Compound: Palbociclib
    Antiproliferative activity against human T47D cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human T47D cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
    [PMID: 36350721]
    U-266 GI50
    11.274 μM
    Compound: Palbociclib
    Antiproliferative activity against human U-266 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human U-266 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay
    [PMID: 34875521]
    U-87MG ATCC IC50
    345.2 nM
    Compound: Palbociclib
    Antiproliferative activity against human U-87 MG cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay
    Antiproliferative activity against human U-87 MG cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay
    [PMID: 32200202]
    U-937 IC50
    0.14 μM
    Compound: Palbociclib
    Antiproliferative activity against human U937 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis
    Antiproliferative activity against human U937 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis
    [PMID: 24641103]
    ZR-75-1 GI50
    2.279 μM
    Compound: Palbociclib
    Antiproliferative activity against human ZR-75-1 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human ZR-75-1 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
    [PMID: 36350721]
    In Vitro

    Palbociclib (0-1 μM, 24 h) inhibits Rb Phosphorylation at Ser795 in MDA-MB-435 cells with an IC50 value of 0.063 μM, and obtains similar effects on both Ser780 and Ser795 phosphorylation in the Colo-205 colon carcinoma[1].
    Palbociclib (0-10 μM, 24 h) arrests MDA-MB-453 cells exclusively in G1 phase[1].
    Palbociclib (500 nM, 7 days) increases expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells[2].
    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[3].
    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[4].

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

    Palbociclib (oral adminstration, 75 or 150 mg/kg, daily for 14 days) produces rapid tumor regressions and delays tumor growth[1].
    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[2].
    Palbociclib (oral administration, 100 mg/kg, daily for 1 week) has potent antitumour effects in genetically engineered mosaic mouse model of liver cancer[4].

    MedChemExpress (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
    Molecular Weight

    447.53

    Formula

    C24H29N7O2

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1C(C(C)=O)=C(C2=CN=C(N=C2N1C3CCCC3)NC4=CC=C(N5CCNCC5)C=N4)C

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

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

    Solvent & Solubility
    In Vitro: 

    0.1 M HCL : 25 mg/mL (55.86 mM; ultrasonic and adjust pH to 4 with 0.1 M HCL)

    DMSO : 5 mg/mL (11.17 mM; ultrasonic and adjust pH to 5 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2345 mL 11.1724 mL 22.3449 mL
    5 mM 0.4469 mL 2.2345 mL 4.4690 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2 mg/mL (4.47 mM); Clear solution

      This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2 mg/mL (4.47 mM); Clear solution

      This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  15% Cremophor EL    85% Saline

      Solubility: 25 mg/mL (55.86 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  0.5% CMC/saline water

      Solubility: 6.67 mg/mL (14.90 mM); Suspended solution; Need ultrasonic and warming and heat to 42°C

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.94%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / 0.1 M HCL 1 mM 2.2345 mL 11.1724 mL 22.3449 mL 55.8622 mL
    5 mM 0.4469 mL 2.2345 mL 4.4690 mL 11.1724 mL
    10 mM 0.2234 mL 1.1172 mL 2.2345 mL 5.5862 mL
    0.1 M HCL 15 mM 0.1490 mL 0.7448 mL 1.4897 mL 3.7241 mL
    20 mM 0.1117 mL 0.5586 mL 1.1172 mL 2.7931 mL
    25 mM 0.0894 mL 0.4469 mL 0.8938 mL 2.2345 mL
    30 mM 0.0745 mL 0.3724 mL 0.7448 mL 1.8621 mL
    40 mM 0.0559 mL 0.2793 mL 0.5586 mL 1.3966 mL
    50 mM 0.0447 mL 0.2234 mL 0.4469 mL 1.1172 mL
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