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  2. Cell Cycle/DNA Damage
  3. CDK
  4. Abemaciclib

Abemaciclib  (Synonyms: LY2835219)

目錄號(hào): HY-16297A 純度: 99.97%
COA 產(chǎn)品使用指南

Abemaciclib (LY2835219) 是具有選擇性的 CDK4/6 抑制劑，能夠抑制 CDK4/CDK6 的活性，IC50 分別為 2 nM 和 10 nM。

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Abemaciclib Chemical Structure

Abemaciclib Chemical Structure

CAS No. : 1231929-97-7

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Customer Review

Other Forms of Abemaciclib:

MCE 顧客使用本產(chǎn)品發(fā)表的 86 篇科研文獻(xiàn)

WB

    Abemaciclib purchased from MCE. Usage Cited in: Nature. 2017 Aug 24;548(7668):471-475.  [Abstract]

    Western blot of SKBR3, BT474, MDA-MB-453, and MDA-MB-361 cells treated with DMSO, GW572016, or Abemaciclib for 48?h. Western blot of MDA-MB-453 cells pretreated with DMSO or Abemaciclib (500?nM) for 0, 1, or 7 days before exposure to Staurosporine (500?nM) for 4?h.

    Abemaciclib purchased from MCE. Usage Cited in: Cancer Res. 2017 May 1;77(9):2488-2499.  [Abstract]

    Treatment with PD 0332991 and Abemaciclib shows an induction of S241 P-PDK1 as early as 1 h after drug exposure without an increased in total PDK1 protein.

    Abemaciclib 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.

    Abemaciclib purchased from MCE. Usage Cited in: Biochem Pharmacol. 2017 Jan 15;124:29-42.  [Abstract]

    Effect of LY2835219 on the expression of ABCB1 or ABCG2 in MDR cells. The protein level of ABCB1 and ABCG2 on MDR cells after 0, 0.1, 0.2 and 0.4 μM LY2835219 stimulation for 48h are measured by Western blot analysis, and mRNA level are measured by PCR (GAPDH as loading control).

    Abemaciclib purchased from MCE. Usage Cited in: Oncotarget. 2017 Jul 27;8(56):95116-95134.  [Abstract]

    Abemaciclib causes increased PARP cleavage in RCC. In 786-O cells Abemaciclib exposure results in increased PARP cleavage. This effect is more rapid and pronounced when Abemaciclib is combined with SU 11248.

    Abemaciclib purchased from MCE. Usage Cited in: Oncotarget. 2017 Jul 27;8(56):95116-95134.  [Abstract]

    Abemaciclib causes increased PARP cleavage in RCC. In Caki-1 cells Abemaciclib exposure results in increased PARP cleavage. This effect is more rapid and pronounced when Abemaciclib is combined with SU 11248.

    Abemaciclib purchased from MCE. Usage Cited in: Oncotarget. 2017 Jun 27;8(40):67422-67438.  [Abstract]

    GTSE1 protein and mRNA levels in MDA-MB-157 and MDA-MB-231 cell lines treated respectively with Abemaciclib 0.5 μM for 24h. Data are presented as mean±SEM of three independent experiments.

    Abemaciclib purchased from MCE. Usage Cited in: Cancer Res. 2016 Nov 15;76(22):6723-6734.  [Abstract]

    The effects of the CDK inhibitor Abemaciclib, PD 0332991 and Ribocilib on Trop2 ICD cleavage. CDK inhibitors decrease Trop2 ICD abundance after the 2nd day of CDK inhibitor treatment.

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

    IC50 & Target[3]

    Cdk4/cyclin D1

    2 nM (IC50)

    CDK6/cyclinD1

    10 nM (IC50)

    CDK9/cyclinT1

    57 nM (IC50)

    CDK5/p35

    287 nM (IC50)

    Cdk5/p25

    355 nM (IC50)

    CDK2/cyclinE

    504 nM (IC50)

    CDK7/Mat1/cyclinH1

    3910 nM (IC50)

    CDK1/cyclinB1

    1627 nM (IC50)

    PIM1

    50 nM (IC50)

    PIM2

    3400 nM (IC50)

    HIPK2

    31 nM (IC50)

    DYRK2

    61 nM (IC50)

    CK2

    117 nM (IC50)

    GSK3b

    192 nM (IC50)

    JNK3

    389 nM (IC50)

    FLT3 (D835Y)

    403 nM (IC50)

    FLT3

    3960 nM (IC50)

    DRAK1

    659 nM (IC50)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A 172 EC50
    0.2 μM
    Compound: 3
    Antiproliferative activity against human A172 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
    Antiproliferative activity against human A172 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
    		[PMID: 31307887]
    A549 IC50
    253 nM
    Compound: Abemaciclib
    Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay
    Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay
    		[PMID: 31200237]
    COLO 205 IC50
    0.217 μM
    Compound: Abemaciclib
    Antiproliferative activity against human COLO205 cells after 96 hrs by CCK8 assay
    Antiproliferative activity against human COLO205 cells after 96 hrs by CCK8 assay
    		[PMID: 29459274]
    COLO 205 IC50
    0.46 μM
    Compound: LY2835219
    Antiproliferative activity against human COLO205 cells after 96 hrs by CCK-8 assay
    Antiproliferative activity against human COLO205 cells after 96 hrs by CCK-8 assay
    		[PMID: 29074254]
    COLO 205 IC50
    120 nM
    Compound: LY-2835219
    Inhibition of CDK4/6 in human COLO205 cells assessed as inhibition of Rb phosphorylation after 24 hrs by propidium iodide staining-based laser-scanning fluorescence microplate cytometric analysis
    Inhibition of CDK4/6 in human COLO205 cells assessed as inhibition of Rb phosphorylation after 24 hrs by propidium iodide staining-based laser-scanning fluorescence microplate cytometric analysis
    		[PMID: 26115571]
    COLO 205 IC50
    253 nM
    Compound: Abemaciclib
    Antiproliferative activity against human COLO205 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay
    Antiproliferative activity against human COLO205 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay
    		[PMID: 31200237]
    COLO 205 IC50
    253 nM
    Compound: Abemaciclib
    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
    0.348 μM
    Compound: Abemaciclib
    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]
    DBTRG-05MG EC50
    0.19 μM
    Compound: 3
    Antiproliferative activity against human DBTRG-05MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
    Antiproliferative activity against human DBTRG-05MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
    		[PMID: 31307887]
    EMT6 IC50
    4.18 μM
    Compound: Abemaciclib
    Antiproliferative activity against mouse EMT6 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    Antiproliferative activity against mouse EMT6 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    		[PMID: 35447031]
    HEK293 GI50
    10.925 μM
    Compound: Abemaciclib
    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
    768 nM
    Compound: Abemaciclib
    Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    		[PMID: 31382120]
    HL-60 GI50
    0.664 μM
    Compound: Abemaciclib
    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-22 IC50
    12.2 μM
    Compound: 1
    Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
    Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
    		[PMID: 36876904]
    HUVEC IC50
    403 nM
    Compound: Abemaciclib
    Antiproliferative activity against HUVEC cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    Antiproliferative activity against HUVEC cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    		[PMID: 31382120]
    Jurkat GI50
    4.63 μM
    Compound: Abemaciclib
    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 GI50
    0.624 μM
    Compound: Abemaciclib
    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]
    M059J EC50
    9.24 μM
    Compound: 3
    Antiproliferative activity against human M059J assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
    Antiproliferative activity against human M059J assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
    		[PMID: 31307887]
    MCF-10A GI50
    5.088 μM
    Compound: Abemaciclib
    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 GI50
    0.832 μM
    Compound: Abemaciclib
    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 GI50
    4.01 μM
    Compound: Abemaciclib
    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
    99.8 nM
    Compound: Abemaciclib
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay
    		[PMID: 31200237]
    MDA-MB-231 IC50
    > 20 μM
    Compound: Abemaciclib
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    		[PMID: 35447031]
    MDA-MB-231 IC50
    191 nM
    Compound: LY2835219
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by DAPI staining based assay
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by DAPI staining based assay
    		[PMID: 29429832]
    MDA-MB-231 GI50
    3.45 μM
    Compound: Abemaciclib
    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 IC50
    62 nM
    Compound: Abemaciclib
    Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    		[PMID: 31382120]
    MDA-MB-468 IC50
    > 20 μM
    Compound: Abemaciclib
    Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    		[PMID: 35447031]
    MDA-MB-468 IC50
    1144 nM
    Compound: Abemaciclib
    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]
    MDA-MB-468 IC50
    4.808 μM
    Compound: Abemaciclib
    Antiproliferative activity against human MDA-MB-468 cells after 96 hrs by CCK8 assay
    Antiproliferative activity against human MDA-MB-468 cells after 96 hrs by CCK8 assay
    		[PMID: 29459274]
    MIA PaCa-2 IC50
    5.8 μM
    Compound: Abemaciclib
    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]
    RPMI-8226 GI50
    1.479 μM
    Compound: Abemaciclib
    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]
    SF-539 EC50
    3.22 μM
    Compound: 3
    Antiproliferative activity against human SF539 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
    Antiproliferative activity against human SF539 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
    		[PMID: 31307887]
    Sf9 IC50
    0.005 μM
    Compound: Abemaciclib
    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
    0.01 μM
    Compound: Abemaciclib
    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
    0.065 μM
    Compound: Abemaciclib
    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
    0.101 μM
    Compound: Abemaciclib
    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
    0.273 μM
    Compound: Abemaciclib
    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
    0.347 μM
    Compound: Abemaciclib
    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
    0.371 μM
    Compound: LY2835219
    Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP
    Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP
    		[PMID: 26741853]
    Sf9 IC50
    0.371 μM
    Compound: Abemaciclib
    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]
    Sf9 IC50
    0.405 μM
    Compound: Abemaciclib
    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
    3.1 μM
    Compound: Abemaciclib
    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]
    SiHa IC50
    861 nM
    Compound: Abemaciclib
    Antiproliferative activity against human SiHa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human SiHa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    		[PMID: 31382120]
    T47D GI50
    0.771 μM
    Compound: Abemaciclib
    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]
    T47D IC50
    145 nM
    Compound: Abemaciclib
    Antiproliferative activity against human T47D cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human T47D cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    		[PMID: 31382120]
    T47D IC50
    34.3 nM
    Compound: Abemaciclib
    Antiproliferative activity against human T47D cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay
    Antiproliferative activity against human T47D cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay
    		[PMID: 31200237]
    T98G EC50
    0.54 μM
    Compound: 3
    Antiproliferative activity against human T98G assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
    Antiproliferative activity against human T98G assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
    		[PMID: 31307887]
    U-266 GI50
    2.701 μM
    Compound: Abemaciclib
    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 EC50
    0.12 μM
    Compound: 3
    Antiproliferative activity against human U87MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
    Antiproliferative activity against human U87MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
    		[PMID: 31307887]
    U-87MG ATCC IC50
    48.1 nM
    Compound: Amebaciclib
    Antiproliferative activity against human U87MG cells after 72 hrs by DAPI staining based assay
    Antiproliferative activity against human U87MG cells after 72 hrs by DAPI staining based assay
    		[PMID: 29247857]
    U-87MG ATCC IC50
    706 nM
    Compound: Abemaciclib
    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]
    Vero CC50
    > 50 μM
    Compound: Abemaciclib
    Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
    Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
    		10.1101/2020.03.20.999730
    Vero IC50
    6.62 μM
    Compound: Abemaciclib
    Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
    Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
    		10.1101/2020.03.20.999730
    ZR-75-1 IC50
    83.4 nM
    Compound: Abemaciclib
    Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay
    Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay
    		[PMID: 31200237]
    體外研究
    (In Vitro)

    Abemaciclib reduces cell viability with the IC50 values ranging from 0.5 μM to 0.7 μM, inhibits Akt and ERK signaling but not mTOR activation at head and neck squamous cell carcinoma (HNSCC) cells[1]. Abemaciclib shows inhibition on A375R1-4, M14R, and SH4R with EC50 values ranging from 0.3 to 0.6 μM; Abemaciclib inhibits the proliferation of the parental A375 and resistant A375RV1 and A375RV2 cells with similar potencies with IC50 values of 395, 260, and 463 nM, respectively[2]. Abemaciclib inhibits CDK4 and CDK6 with low nanomolar potency, inhibits Rb phosphorylation resulting in a G1 arrest and inhibition of proliferation, and its activity is specific for Rb-proficient cells[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    Abemaciclib (45 mg/kg, p.o.) in combination with RAD001 causes a cooperative antitumor effect in HNSCC xenograft tumor[1]. Abemaciclib (45 or 90 mg/kg, p.o.) shows significant tumor growth inhibition in an A375 xenograft model[2].

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

    506.59

    Formula

    C27H32F2N8
    CAS 號(hào)
    性狀

    固體

    顏色

    Off-white to yellow

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式

    4°C, protect from light

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

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

    DMSO 中的溶解度 : 2.94 mg/mL (5.80 mM; 超聲助溶 (<80°C); 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 1.9740 mL 9.8699 mL 19.7398 mL
    5 mM 0.3948 mL 1.9740 mL 3.9480 mL
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)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)：

    以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑： 0.5% Hydroxyethyl cellulose in Water

      Solubility: 3.33 mg/mL (6.57 mM); 懸濁液; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)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(guò)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
    純度 & 產(chǎn)品資料

    純度: 99.97%

    參考文獻(xiàn)
    Cell Assay
    [1]

    Cells are seeded in a 96-well plate, allowed to adhere overnight, and treated with DMSO control (0.1% v/v) or the indicated compounds for 72 h. Cell viability and proliferation are determined using a Cell Counting Kit according to the manufacturer's instructions. The interaction between Abemaciclib and mTOR inhibitor is determined using CompuSyn. Combination index (CI) values of 1 indicates and additive drug interaction, whereas a CI of <1 is synergistic and a CI of >1 is antagonistic.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Six-week-old BALB/c female nude mice are injected subcutaneously with OSC-19 (1×106) cells. When tumor sizes reach approximately 100 mm3, mice are randomized by tumor size and subjected to each treatment. At least 5 mice per treatment group are included. Each group of mice is dosed via daily oral gavage with vehicle, Abemaciclib (45 mg/kg/d or 90 mg/kg/d), RAD001 (5 mg/kg/d), or a combination of both. The Abemaciclib is dissolved in 1% HEC in 20 mM phosphate buffer (pH2.0). Tumor size and body weight are measured twice weekly. Tumor volumes are calculated using the following formula: V=(L×W2)/2. Mice are gavaged a final time on day 14 and sacrificed the following day. The tumors are removed for Western blot and immunohistochemistry.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?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 1 mM 1.9740 mL 9.8699 mL 19.7398 mL 49.3496 mL
    5 mM 0.3948 mL 1.9740 mL 3.9480 mL 9.8699 mL
    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.

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    產(chǎn)品名稱：
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    目錄號(hào)：
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