Palbociclib (PD-0332991) HCl

Licensed by Pfizer Catalog No.S1116

Palbociclib (PD-0332991) HCl Chemical Structure

Molecular Weight(MW): 483.99

Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

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8 Customer Reviews

  • PD-0332991 causes inhibition of proliferation of EAC cells in a dose-dependent manner. Western blots showing the phosphorylation status of pRB at Ser780 and Ser795 after incubation with 125 nmol/L PD-0332991 for 24 and 72 hours. Reduction in cyclin A expression and the expression of RB2 (p130) tumor suppressor 72 hours after PD-0332991 treatment are shown (bottom). Total pRB (RB1) and actin are loading controls and T293 cell lysate (293) is a positive control for total pRB and phospho-pRB (Ph-RB). E, anchorage-independent growth of the 3 cell lines in the presence or absence (Cnt) of 125 nmol/L PD-0332991 for 3 weeks.

    Clin Cancer Res 2011 17(13), 4513-22. Palbociclib (PD-0332991) HCl purchased from Selleck.

    b, c MelJuso cells were treated for 12–48 h with 1 µM Selumetinib or 5 µM Palbociclib and the cells were fixed, stained with propidium iodide and cell cycle distribution was determined by flow cytometry (b) and whole cell extracts were fractionated by SDS-PAGE, transferred onto PVDF membrane and immuno-blotted with the indicated antibodies (c). Data is from a single experiment representative of three separate experiments with similar results. The data in (b) are mean ± S.D. from a single experiment with three replicate dishes of cell per data point; similar results were obtained in two additional experiments

    Cell Mol Life Sci, 2016, 73(4):883-900. Palbociclib (PD-0332991) HCl purchased from Selleck.

  • (A) Percentage of DN3a cells in S-phase (as gated on DAPI profile) from control (Zfp36l1/2fl/fl) and Zfp36l1/2fl/fl; CD2Cre (DCKO) mice, after 1 d of treatment with vector or palbociclib (drug).

    J Immunol, 2016, 197(7):2673-85. Palbociclib (PD-0332991) HCl purchased from Selleck.

     

    Patient tumor cell sensitivity to combinatorial treatment with histone deacetylase (HDAC)/cyclin-dependent kinase (CDK) inhibitors in 3-D culture. The effect of each drug or drug combination was assessed by fluorescent dye to identify live (green) and dead cells (red). Cells from breast reduction patients were used as non-cancer control in the assay.

    Pharmacogenomics J 2013 13(1), 94-104. Palbociclib (PD-0332991) HCl purchased from Selleck.

  •  

    Cdk4 is upregulated in ARMS and mMSCs transfected with PAX7-FKHR fusion gene (MP7F), and can be specifi cally inhibited. D: IF results showing overexpression of cdk4 in MP7F cells compared to parental mMSCs and reduced expression of cdk4 after treatment of MP7F cells with the cdk4 inhibitor, PD-0332991. E: IF results showing MyoD1 expression in parental mMSCs cells, and MP7F cells untreated and after treatment with the cdk4 inhibitor, PD-0332991.

    Clin Transl Oncol 2012 14(3), 197-206 . Palbociclib (PD-0332991) HCl purchased from Selleck.

    WM3734 melanoma cells were treated by PD-0332991 for 36 hours; melanoma cells treated by Doxorubicin (DXR)  at 0.5 μM is included as a control.

     

     

    Dr. Gao Zhang of University of Pennsylvania. Palbociclib (PD-0332991) HCl purchased from Selleck.

  • Serum-deprived T98G glioma cells are restimulated with serum(FBS) with or without 1 μΜ PD-0332991.

     

     

    Dr. Sabine Paternot and Dr Pierre Roger of IRIBHM, ULB, Brussels. Palbociclib (PD-0332991) HCl purchased from Selleck.

    P16INK4A knockdown in INK4A/ARF-wt human glioma cell LN319 potentiates PDGF-Apromoted anchorage-dependent growth in vitro. Soft agar growth of Ink4a/Arf-deficient mAst and LN444 cells treated with PD0332991. (A) IB analysis. (B) Quantification of soft agar assays. β-actin was used as a loading control in all IB experiments. Data are presented as mean ± s.d. and representative of two independent experiments. **, P < 0.01; ***, P < 0.001

    Dr. Kun-Wei Liu from University of Pittsburgh. Palbociclib (PD-0332991) HCl purchased from Selleck.

Purity & Quality Control

Choose Selective CDK Inhibitors

Biological Activity

Description Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.
Features Non-cytotoxic, and halts cancer cell growth & could be used in glioblastoma that has relapsed after temozolomide treatment (a chemotherapeutic used to treat many cancers).
Targets
CDK4/CyclinD3 [1]
(Cell-free assay)
CDK4/CyclinD1 [1]
(Cell-free assay)
CDK6/CyclinD2 [1]
(Cell-free assay)
9 nM 11 nM 15 nM
In vitro

PD 0332991 has little effect on other protein kinases including EGFR, FGFR, PGFR, IR. PD 0332991 is a non-ATP competitive inhibitor of Cdk4. PD 0332991 inhibits MDA-MB-435 breast carcinoma cells with IC50 of 66 nM, which is due to reduced Rb phosphorylation at Ser780. PD 0332991 inhibits thymidine incorporation into the DNA of Rb-positive human breast, colon, and lung carcinomas as well as human leukemias, with IC50 values ranging from 0.04-0.17 μM. PD 0332991 shows no activity in Rb-negative cells. PD 0332991 causes an accumulation of cells in G1 in MDA-MB-453 breast and Colo-205 carcinoma cells. [1] PD 0332991 also shows activity in 5T33MM myeloma cells (immunocompetent model) and sensitizes the cells to killing by bortezomib. [2] PD 0332991 inhibits luminal ER-positive as well as HER2-amplified breast cancer cell lines including MDA-MB-175, ZR-75-30, CAMA-1, MDA-MB-134, HCC-202 and UACC-893. PD 0332991 enhances the activity of tamoxifen and trastuzumab in these cell lines. PD 0332991 enhances the sensitivity of tamoxifen in the MCF7 tamoxifen-resistant cells. [3] A recent study shows that PD 0332991 could suppress malignant rhabdoid tumor (MRT) cell lines including MP-MRT-AN, KP-MRT-RY, G401, KP-MRT-NS and the sensitivity of the MRT cell lines to PD 0332991 is inversely correlated with expression of p16. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MOLM13 NIfFb29McW6jc3WgRZN{[Xl? Mn2wNlQhcA>? MWrJcohq[mm2aX;uJI9nKEOGS{SgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDSZkBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMECyJO69VQ>? Mo[2NlQ3PDFzMEO=
COLO205 M3LTS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUC3NkBp NWPWNlBySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|ZYPz[YQh[XNiaX7jc5Jxd3KjdHnvckBw\iCdM1jdeIh6dWmmaX7lJIlvfG9iRF7BJJdqfGhiSVO1NEBw\iByLkCzOkDPxE1? M13LcFI1PjRzMUCz
U937 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfUSFE4OiCq MmjDRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{\XO|ZXSgZZMhcW6lb4Lwc5JifGmxbjDv[kBcO0ifdHj5cYllcW6nIHnueI8hTE6DIIfpeIghUUN3MDDv[kAxNjF2IN88US=> MmnsNlQ3PDFzMEO=
MOLM13 NITkWINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTZUWY{PzJiaB?= M4racGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTV;MUVE{KGOnbHzzJIhiemKxcnnu[{BHVFR|IFnUSEBufXSjboSgZZN{\XO|ZXSgZZMhcW6lb4Lwc5JifGmxbjDv[kBcO0ifdHj5cYllcW6nIHnueI8hTE6DIIfpeIghUUN3MDDv[kAxNjB7NjFOwG0> MVeyOFY1OTFyMx?=
MOLM13 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHwO|IhcA>? MknURY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDzc5Ji\mWwaXKtdoV{cXO2YX70JIh2dWGwIF3PUG0yOyClZXzsd{Bie3Onc4Pl[EBieyCrbnPvdpBwemG2aX;uJI9nKFt|SG30bJlucWSrbnWgbY51dyCGTlGge4l1cCCLQ{WwJI9nKDBwMEm2JO69VQ>? NX[weFhiOjR4NEGxNFM>
MDA-MB-435 M3Hk[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3kSYdbOjRiaB?= MUfJR|UxRTBwMU[g{txO MoPXNVU5ODF6M{G=
K562 NX;V[4NsS3m2b4TvfIlkKEG|c3H5 M1n4Wlk3KGh? NGHkZpJFVVOR NVTlNHdHUUN3ME2yJO69VQ>? MkXBNlQ1OTd3Nk[=
DU145 Ml[2R5l1d3SxeHnjJGF{e2G7 MWG5OkBp NIDyOXhFVVOR NGruTmpKSzVyPUeuOUDPxE1? M{TkR|I1PDF5NU[2
MDA-MB-231 NYK2d3VST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HzdFEh|ryP MmXUNlQhcA>? M4rNemROW09? MnzNR4VtdCCleXPs[UBienKnc4SgZZN{\XO|ZXSgZZMh[WOldX31cIF1cW:wIHH0JGcyKHCqYYPl MVKyOFQyPzV4Nh?=
MCF7 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfmNUDPxE1? NVW3UYl1OjRiaB?= MX3EUXNQ MomyR4VtdCCleXPs[UBienKnc4SgZZN{\XO|ZXSgZZMh[WOldX31cIF1cW:wIHH0JGcyKHCqYYPl MmHwNlQ1OTd3Nk[=
MCF7 MmTjT4lv[XOnIFHzd4F6 MoPtOUDPxE1? NFj6N3MzPCCq MWLEUXNQ M1vrVGlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgR2RMPC:leXPsbY5FOSCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKHKndHnuc4Jt[XO2b33hJJBpd3OyaH;yfYxifGmxbjDheEBU\XJ5OEC= MoXnNlQ1OTd3Nk[=
MDA-MB-231 NIfXSWNMcW6jc3WgRZN{[Xl? MUS1JO69VQ>? MkXQNlQhcA>? NF3yTmJFVVOR NFHIdWVKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JGNFUzRxY4njcIlvTDFiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iC{ZYTpco9jdGG|dH;tZUBxcG:|cHjvdplt[XSrb36gZZQhW2W{N{iw M3PBTVI1PDF5NU[2
MDA-MB-231 NVXkbm5GTnWwY4Tpc44hSXO|YYm= NEPPPIYyNTFyIN88US=> MUiyOEBp MW\EUXNQ M2nacYRw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYOgZZN{\XO|ZXSgZZMhWEGUUDDjcIVifmGpZR?= Mo\pNlQ1OTd3Nk[=
MCF7 MWDGeY5kfGmxbjDBd5NigQ>? M4LFcVEuOTBizszN MkO1NlQhcA>? MUnEUXNQ MVfkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m|IHHzd4V{e2WmIHHzJHBCWlBiY3zlZZZi\2V? MXuyOFQyPzV4Nh?=
MDA-MB-231 NWfPR241TnWwY4Tpc44hSXO|YYm= NFqwSWExNjVvMTFOwG0> NXXscmJxPDhiaB?= Mkn2SG1UVw>? M3nneohieyCwbzDD[YxtKGO7Y3zlJIFzemW|dDDhd5Nme3OnZDDhd{Bi[2O3bYXsZZRqd25iYYSgd5VjNUdzIIDoZZNm NYD3TFQ1OjR2MUe1OlY>
MCF7 MYLGeY5kfGmxbjDBd5NigQ>? NF\2WGYxNjVvMTFOwG0> NGPBdG41QCCq Mn;VSG1UVw>? NXr0[VR1cGG|IH7vJGNmdGxiY4njcIUh[XK{ZYP0JIF{e2W|c3XkJIF{KGGlY4XteYxifGmxbjDheEB{fWJvR{GgdIhie2V? MnfNNlQ1OTd3Nk[=
697 NYT3TGNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHhXll4UUN3ME2xOFgvOzhibl2= NUD4R3c6W0GQR1XS
P12-ICHIKAWA M12wd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTl4LkC0JI5O MkPWV2FPT0WU
NB69 NH3VcoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTF4MT64JI5O M{fNRnNCVkeHUh?=
EoL-1 NIP3b3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1u2emlEPTB;MUi3MlI3KG6P NXntdGN2W0GQR1XS
BHT-101 M3v1TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVv3Rld[UUN3ME2xPVgvOjVibl2= M3LqSnNCVkeHUh?=
SK-NEP-1 NEi5T2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2npR2lEPTB;MkKwMlAzKG6P M2LpNHNCVkeHUh?=
MHH-NB-11 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWD3bnRbUUN3ME2yNlAvOTlibl2= NYPnT24yW0GQR1XS
AsPC-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXwSml{UUN3ME2yOVIvPTNibl2= NVW0c3NRW0GQR1XS
ES1 M2iyZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTJ3Nj6yOUBvVQ>? MYXTRW5ITVJ?
LAMA-84 NEi3e2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInlUGdKSzVyPUK1PE4yQSCwTR?= MYjTRW5ITVJ?
MOLT-16 NVfCfmtLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTLToxqUUN3ME2yOVgvPDlibl2= NF;pNVJUSU6JRWK=
ES7 MlfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTJ5Mz6wPUBvVQ>? M1XVZXNCVkeHUh?=
KY821 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTNzND6xJI5O MXTTRW5ITVJ?
RT-112 NXvUepdqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTN{MT6wOUBvVQ>? MmP6V2FPT0WU
HL-60 NVzPUZQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDOcm1IUUN3ME2zOFAvPjZibl2= M1XjbXNCVkeHUh?=
MOLT-4 MlfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVK0T5NPUUN3ME2zOFUvOTNibl2= NXKwW2VGW0GQR1XS
KARPAS-45 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fyPWlEPTB;M{e2MlE3KG6P NVf2cnBwW0GQR1XS
SK-N-AS MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPITWM2OD1|OEeuPFMhdk1? MULTRW5ITVJ?
CTB-1 NVr6[5NnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnjTWM2OD12MEWuNFIhdk1? NWPt[XBFW0GQR1XS
NKM-1 Mk\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7GTWM2OD12MUGuPFkhdk1? M37KbXNCVkeHUh?=
HTC-C3 M4C3O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M363PWlEPTB;NEOyMlk2KG6P NUXGbmtiW0GQR1XS
BE-13 MkfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPRWXZKSzVyPUS0OE4zPyCwTR?= M37ROHNCVkeHUh?=
KOSC-2 M2fWU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTR4Nj65JI5O M4K1cXNCVkeHUh?=
NB14 NYWybWlyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHz2dmNKSzVyPUS4N{42QCCwTR?= M2\4R3NCVkeHUh?=
CAL-27 MlixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfHS|RKSzVyPUS5OE42QSCwTR?= NIPXc25USU6JRWK=
H9 M3qyXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfXXFRVUUN3ME20PVUvPDNibl2= NGTmb|RUSU6JRWK=
RS4-11 NGK4Z5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\mN49KSzVyPUWwOE44OyCwTR?= NF:4Z3RUSU6JRWK=
PA-1 NWCwboNDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\yNJB2UUN3ME21NFkvQDZibl2= MVfTRW5ITVJ?
MV-4-11 MlH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHHeJlWUUN3ME21NVMvQDVibl2= M3m4dnNCVkeHUh?=
OS-RC-2 NUXRbYRmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvjTWM2OD13MkGuOlIhdk1? M3fXfHNCVkeHUh?=
RPMI-8226 NWfmbmwxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\held7UUN3ME21NlYvQDZibl2= NYnYXFBFW0GQR1XS
HGC-27 NH;v[ZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnBTWM2OD13NkSuPVkhdk1? M1XPe3NCVkeHUh?=
CHP-212 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPyWWlKSzVyPUW5N{42QSCwTR?= M2KwS3NCVkeHUh?=
NB10 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDleVBrUUN3ME21PVkvOThibl2= MY\TRW5ITVJ?
HH MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPVR3RKSzVyPUW5PU41OyCwTR?= NWD5OoZMW0GQR1XS
EW-16 M4Pu[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTZyMz61NkBvVQ>? M3rjfXNCVkeHUh?=
ES8 M2DiZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGn4ZXJKSzVyPU[wOU4zOSCwTR?= M1;POnNCVkeHUh?=
HAL-01 NVLrOo9GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjyNFk4UUN3ME22NFUvPjdibl2= NUfKXXNpW0GQR1XS
A204 NIr4RYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTZ|Mz65NUBvVQ>? Ml3rV2FPT0WU
MHH-PREB-1 MmjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2T4c2lEPTB;NkO2Mlk6KG6P NFPlT5lUSU6JRWK=
EM-2 NYHTflZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnKzTWM2OD14NUCuOlQhdk1? Mk\3V2FPT0WU
BV-173 M{POcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37XV2lEPTB;NkWyMlQ5KG6P MYPTRW5ITVJ?
ONS-76 NYLnPVNTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofwTWM2OD14N{euPFIhdk1? MWTTRW5ITVJ?
KM-H2 M1HPe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH36TWZKSzVyPU[5OU42PCCwTR?= MX3TRW5ITVJ?
D-263MG M{HwS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTdzNz6xNkBvVQ>? Mn;ZV2FPT0WU
ES3 MorpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXSUJg2UUN3ME23NlgvQTNibl2= NIDUT3hUSU6JRWK=
VA-ES-BJ MojkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LJWWlEPTB;N{OyMlI4KG6P NYPSVllCW0GQR1XS
NBsusSR NXnPN3pWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVj5[XBCUUN3ME23OFIvQTlibl2= MXHTRW5ITVJ?
NCI-H520 NYrqSoNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTd2Nj61NkBvVQ>? NF\wSYNUSU6JRWK=
ES5 NFfPfWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7NOnk3UUN3ME23OVIvQCCwTR?= NG[2XHZUSU6JRWK=
T-24 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3DTFRWUUN3ME23O|gvPzFibl2= M3\qNXNCVkeHUh?=
SW962 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU[2fW9WUUN3ME24NFgvPjNibl2= M{TKc3NCVkeHUh?=
EW-3 M3m3Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRThyOD63OkBvVQ>? MkTHV2FPT0WU
RXF393 NF\1OFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnTW5lKSzVyPUixNk44QSCwTR?= MYnTRW5ITVJ?
U251 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPiTWM2OD16MUOuPFghdk1? NX\hNVNMW0GQR1XS
CAMA-1 NXO5fmU6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33yXWlEPTB;OEOzMlk1KG6P NV74U3JbW0GQR1XS
JVM-3 NVu2cnJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjpN|hKSzVyPUi1NU44QCCwTR?= MXfTRW5ITVJ?
COLO-800 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnuUVdKSzVyPUi5O{44QCCwTR?= NHnXUXFUSU6JRWK=
OVCAR-5 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlmzTWM2OD17MECuNUBvVQ>? Mo\SV2FPT0WU
LB1047-RCC NFXTdYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTl{Nz61OkBvVQ>? M{Dz[nNCVkeHUh?=
SW954 NW\YSI9JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfLTWM2OD17MkmuOFEhdk1? NF\OU5pUSU6JRWK=
J-RT3-T3-5 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTl|Nj6wOkBvVQ>? M33yTHNCVkeHUh?=
Mewo NYjIXI5ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzUTWM2OD17M{[uOkBvVQ>? MoLjV2FPT0WU
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NCI-H1573 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;0OIgzUUN3ME2yMlA4Ojl6IN88US=> NV:0eYhDW0GQR1XS
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D-423MG NYXRdI9sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnzTWM2OD14Lke2NVE4KM7:TR?= M1zLXXNCVkeHUh?=
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D-247MG MonCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLSZpJGUUN3ME23MlA4QDhzIN88US=> NEf5O|JUSU6JRWK=
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EW-13 MojNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHr5XWNKSzVyPUeuN|UyPjJizszN M{LrWnNCVkeHUh?=
DOHH-2 MnXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTdwNESwNkDPxE1? MV7TRW5ITVJ?
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KYSE-520 MkHZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvZNndwUUN3ME23MlU2PTF3IN88US=> NUDKT|A{W0GQR1XS
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HCE-4 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHGclNQUUN3ME23MlYzOjd7IN88US=> MXLTRW5ITVJ?
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KYSE-180 M4jiOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTdwN{GxOlkh|ryP Mmr3V2FPT0WU
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NCI-H1581 MkLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoGyTWM2OD16LkCxNkDPxE1? Ml34V2FPT0WU
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SK-OV-3 Mni2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4T1cmlEPTB;OD60Olc3PSEQvF2= NGLo[nJUSU6JRWK=
KNS-62 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\yT5NKSzVyPUiuOVE4PjFizszN NIjDNY9USU6JRWK=
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RPMI-2650 NUj0bHI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\aW|FKUUN3ME24MlcyQTV3IN88US=> NG\MOlVUSU6JRWK=
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KYSE-450 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVP6[nY4UUN3ME24Mlg3PTR6IN88US=> NXrDdVk6W0GQR1XS
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HCC1806 NXjxOot[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlX4TWM2OD1zNj63NFcyKM7:TR?= NWTaeFByW0GQR1XS
NCI-H2170 NGjHNYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjITWM2OD1zNz6yOFQ5KM7:TR?= NVPLNHF4W0GQR1XS
AGS NF\DOHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvVenFKSzVyPUG3MlM5ODhizszN MoLlV2FPT0WU
MEL-HO MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLadWVTUUN3ME2xO{44PTB|IN88US=> MUPTRW5ITVJ?
SW48 M4rQS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTF5Lke3NVYh|ryP M{PoRXNCVkeHUh?=
HuP-T4 MmqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoT0TWM2OD1zOD6wNlA3KM7:TR?= NGjvPXVUSU6JRWK=
NCI-H720 M3K2cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DXeGlEPTB;MUiuNVQxOiEQvF2= M3vkVHNCVkeHUh?=
RCC10RGB NWPXTolMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI[zUmpKSzVyPUG4MlE3QTdizszN MlnYV2FPT0WU
HD-MY-Z MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmf1TWM2OD1zOD6yNlU1KM7:TR?= MkfzV2FPT0WU
A427 NWDseFJyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHrTHdGUUN3ME2xPE42ODl2IN88US=> M4X2bnNCVkeHUh?=
HCC2998 M1nLPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnT2TWM2OD1zOD62NFUyKM7:TR?= MkHhV2FPT0WU
EPLC-272H M2fRPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTF7LkC0N|Qh|ryP NVzQXoU5W0GQR1XS
C32 NGj0XoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nudWlEPTB;MUmuNFQ2KM7:TR?= Mon3V2FPT0WU
UMC-11 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\KVWlEPTB;MUmuNlEzOyEQvF2= NEfoWoNUSU6JRWK=
CaR-1 Mn\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrES4lNUUN3ME2xPU43QDB2IN88US=> NInzNlZUSU6JRWK=
KYSE-410 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXy1OVl4UUN3ME2xPU46OTN7IN88US=> MmrpV2FPT0WU
HuCCT1 MoTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XRfmlEPTB;MkCuOlI6PCEQvF2= M362UHNCVkeHUh?=
LB996-RCC NWnvOGNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYC3Sm5VUUN3ME2yNE44OTZ6IN88US=> M37kPHNCVkeHUh?=
KYSE-70 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPyTWM2OD1{MD64NFU6KM7:TR?= NHLzfmdUSU6JRWK=
CAL-72 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYeyUldVUUN3ME2yNE46OTVizszN NHL3TXhUSU6JRWK=
Capan-2 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3:yfmlEPTB;MkGuNFQyOyEQvF2= MWTTRW5ITVJ?
PANC-08-13 M3KweWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHGSHI{UUN3ME2yNU4zPTF3IN88US=> M2roV3NCVkeHUh?=
SBC-1 NVjKeol[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTJzLkOwPFEh|ryP NWjUUpZwW0GQR1XS
MFM-223 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTJzLkOzOFIh|ryP NI\uT2JUSU6JRWK=
BB49-HNC MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{K3TmlEPTB;MkGuOVcyPiEQvF2= M2[4NnNCVkeHUh?=
SH-4 M4jUPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTJzLk[2NVgh|ryP NYTTeZh4W0GQR1XS
HuO9 NW[xU5FzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jISGlEPTB;MkGuPVgzPSEQvF2= MkHGV2FPT0WU
AM-38 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LpW2lEPTB;MkKuNFQ5PSEQvF2= M3\KT3NCVkeHUh?=
A431 NYLFXWx[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXaVFVKSzVyPUKzMlIyOTlizszN NFnwU5JUSU6JRWK=
YAPC NXTyVIh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfnTWM2OD1{Mz6yOlUyKM7:TR?= NWjqOGJRW0GQR1XS
LU-139 NFG2TmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTJ|LkS4NFkh|ryP MUfTRW5ITVJ?
HEC-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{W0bmlEPTB;MkOuOFk{PyEQvF2= MVTTRW5ITVJ?
SCC-25 NWLSZldxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvzTWM2OD1{ND6zNFA3KM7:TR?= NWXiNGpGW0GQR1XS
HT-29 NV65WXRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnmwTWM2OD1{ND6zPFI{KM7:TR?= NHHERndUSU6JRWK=
PC-14 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTJ2Lk[1O|Eh|ryP NELNR3hUSU6JRWK=
Calu-6 NEnJSIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjhXIJKSzVyPUK1MlUxPzFizszN M{SwPHNCVkeHUh?=
SJRH30 M{DoSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\5TWM2OD1{NT62OFk3KM7:TR?= NVj6UHBsW0GQR1XS
ChaGo-K-1 Mn3PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;HTWM2OD1{Nj6xOlI6KM7:TR?= M3r1UnNCVkeHUh?=
IA-LM MlHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTJ4LkO2OFUh|ryP Mne4V2FPT0WU
GP5d MnP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjaelRVUUN3ME2yOk41PDlzIN88US=> M2O5PXNCVkeHUh?=
NCI-H2291 Ml62S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfjWIlKSzVyPUK2MlY2PDFizszN Ml7yV2FPT0WU
BALL-1 NWrwU5pVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PUPWlEPTB;Mk[uPVM6PyEQvF2= MWXTRW5ITVJ?
HCC1954 NUW4THR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17KVWlEPTB;Mk[uPVgxQCEQvF2= NV3afpA5W0GQR1XS
NCI-H2452 NWXWblM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{m1ZWlEPTB;MkeuOFE3OyEQvF2= M3zvWHNCVkeHUh?=
LU-99A M{HRWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjUbYZyUUN3ME2yO{42PTh{IN88US=> MnS3V2FPT0WU
NTERA-S-cl-D1 MmLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjoS2VNUUN3ME2yO{44Ojl7IN88US=> MnOyV2FPT0WU
PANC-10-05 NIK3dZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jydWlEPTB;MkeuO|c4PSEQvF2= NXftS5NNW0GQR1XS
NCI-H2405 NYPsfYFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTJ5LkmzPFch|ryP NYjyPVZqW0GQR1XS
MDA-MB-415 NU\kOnI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTrT24zUUN3ME2yPE41OTN5IN88US=> NHLwb|NUSU6JRWK=
NCI-H2342 M{XOeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFz1OIVKSzVyPUK4MlUzQDFizszN NIntc3VUSU6JRWK=
TGBC24TKB NVztTGc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWj5dWxkUUN3ME2yPE44OTF5IN88US=> NYPCdIJUW0GQR1XS
LU-134-A M4K0W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\2VmlEPTB;MkiuPVI3OSEQvF2= MVXTRW5ITVJ?
SCC-4 NF\VcFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jySmlEPTB;M{GuNFQ6PCEQvF2= MYrTRW5ITVJ?
Saos-2 M2XOd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfGNolZUUN3ME2zNU46OzB4IN88US=> M4PuT3NCVkeHUh?=
RERF-LC-MS NH;xPXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NISzPFlKSzVyPUOyMlgzOzFizszN M1fWe3NCVkeHUh?=
M14 M{jOcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXkTWM2OD1|Mj65O|Y1KM7:TR?= NFXaN3lUSU6JRWK=
HPAF-II MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHWb4xKSzVyPUOzMlUxOTFizszN M3nofHNCVkeHUh?=
NCI-H1755 NIDSW|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnNdYh[UUN3ME2zOE4{OzB3IN88US=> NXfYVoJyW0GQR1XS
D-392MG NFfVN4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPMVFFjUUN3ME2zOU45Pjd2IN88US=> MVXTRW5ITVJ?
A704 NHLLTJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTN4LkC0Nlch|ryP M1fDNHNCVkeHUh?=
CP50-MEL-B NWrrfWJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfOTWM2OD1|Nj6xPVEyKM7:TR?= MnixV2FPT0WU
EW-18 NEX1SYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEG0dJJKSzVyPUO2MlQ2OiEQvF2= M3fU[nNCVkeHUh?=
WM-115 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvsdZA1UUN3ME2zOk45ODl7IN88US=> MWXTRW5ITVJ?
LU-65 M1;p[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnjTWM2OD1|Nz6xOFE4KM7:TR?= NGX5XWNUSU6JRWK=
NCI-H1563 NYr2W21FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLpTWM2OD1|Nz6yOFg1KM7:TR?= NGPwcVNUSU6JRWK=
DBTRG-05MG NUi5WIpiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF36XY1KSzVyPUO4MlA3QTFizszN NHLOXXFUSU6JRWK=
NCI-H630 NF\td|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTN6LkS3NVQh|ryP MX\TRW5ITVJ?
NCI-H1155 NYXIUoFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jBcGlEPTB;M{muNlQzKM7:TR?= M{mzbHNCVkeHUh?=
OVACR-3 MnLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTN7LkmxPVUh|ryP MmfFV2FPT0WU
OAW-42 Mn32S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXOSY1xUUN3ME20NE41OjV6IN88US=> NGjKSHZUSU6JRWK=
JVM-2 NX2zW3RXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\xTWM2OD12MT6yOFE2KM7:TR?= NVu2cIVvW0GQR1XS
C3A MoLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnCTWM2OD12MT6zOFQ4KM7:TR?= M4TSVHNCVkeHUh?=
HT55 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjXTWM2OD12Mj6yPFQyKM7:TR?= NInmeHBUSU6JRWK=
OVCAR-4 Ml\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTR{LkK5O|Qh|ryP M3;MUnNCVkeHUh?=
MEG-01 NELzeJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTR{LkS2NVYh|ryP NWW5dmZlW0GQR1XS
NCI-H82 M3;LWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGOwdIZKSzVyPUSzMlk5QTJizszN M4LEd3NCVkeHUh?=
JEG-3 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLCTWM2OD12ND65OFch|ryP M{\CWHNCVkeHUh?=
BPH-1 M3K3OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUey[IZxUUN3ME20Ok4{QTl6IN88US=> MV7TRW5ITVJ?
MPP-89 NV;jPHluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzITWM2OD12Nz6yPFk5KM7:TR?= NWW4foI2W0GQR1XS
ALL-PO NHu2XWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmn5TWM2OD12Nz60NVg5KM7:TR?= M3H3fXNCVkeHUh?=
HT NEn3dHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW[1RpJNUUN3ME20O{41QTJizszN NXv4VoRxW0GQR1XS
NCI-H2347 NGDqd21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknNTWM2OD12OD6wO|E2KM7:TR?= NWq1Z3pqW0GQR1XS
A2780 NGfp[ZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEK1ZXdKSzVyPUS5MlQzOjhizszN NVzVOGJ4W0GQR1XS
KARPAS-299 NHy2SoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4e0XmlEPTB;NEmuOVEyQSEQvF2= NW\rRpQxW0GQR1XS
NCI-H1651 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHBWndOUUN3ME20PU45QDJzIN88US=> M{X5ZXNCVkeHUh?=

... Click to View More Cell Line Experimental Data

In vivo PD 0332991 indicates complete tumor stasis in a MDA-MB-435 xenograft at 150 mg/kg. PD 0332991 also shows broad-spectrum antitumor activity in multiple human tumor xenografts by eliminating phospho-Rb and the proliferative marker Ki-67 from tumor tissue and down-regulation of genes under the transcriptional control of E2F. [1]

Protocol

Kinase Assay:

[1]

+ Expand

Cdk Assays:

A stock solution of PD0332991 is prepared in DMSO. CDK assays are performed in 96-well filter plates. All CDK-cyclin kinase complexes are expressed in insect cells through baculovirus infection and purified. The substrate for the assays is a fragment (amino acids 792–928) of pRb fused to GST (GST·RB-Cterm). The total volume in each well is 0.1 mL containing a final concentration of 20 mM Tris-HCl, pH 7.4, 50 mM NaCl, 1 mM dithiothreitol, 10 mM MgCl2, 25 μM ATP (for CDK4-cyclin D1, CDK6-cyclin D2, and CDK6-cyclin D3) or 12 μM ATP (for CDK2-cyclin E, CDK2-cyclin A, and CDC2-cyclin B) containing 0.25 μCi of [γ-32P]ATP, 20 ng of enzyme, 1 μg of GST·RB-Cterm, and PD 0332991 (0.001-0.1μM). All components except the [γ-32P]ATP are added to the wells, and the plate is placed on a plate mixer for 2 min. The reaction is started by adding the [γ-32P]ATP and the plate is incubated at 25 °C for 15 min. The reaction is terminated by addition of 0.1 mL of 20% trichloroacetic acid and the plate is kept at 4  °C for at least 1 hour to allow the substrate to precipitate. The wells are then washed 5 times with 0.2 mL of 10% trichloroacetic acid and radioactive incorporation is determined with a β plate counter.
Cell Research:

[1]

+ Expand
  • Cell lines: Tumor cell lines including MDA-MB-435, ZR-75-1, T-47D, MCF-7, H1299, Colo-205, MDA-MB-468, H2009, CRRF-CEM and K562
  • Concentrations: 0.01-1 μM
  • Incubation Time: 24 hours
  • Method:

    Cells are seeded at 2 × 104 per well in a 96-well plate and incubated overnight. PD 0332991 (0.01-1 μM) is added to the wells and incubated at 37 °C for another 24 hours. [14C]Thymidine (0.1 μCi) is added to each well and incorporation of the radiolabel is allowed to proceed for 72 hours. Incorporated radioactivity is determined with a β plate counter.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Advanced stage human tumor xenografts including Colo-205, MDA-MB-435 breast, SF-295 glioblastoma, ZR-75-1 breast, PC-3 prostate, H125 lung, SW-620 colon, H23 lung and MDA-MB-468 breast (Rb negative) are established in severe combined immunodeficient mice.
  • Formulation: Dissolved in sodium lactate buffer (50 mM, pH 4.0)
  • Dosages: 0-150 mg/kg
  • Administration: Given by gavage
    (Only for Reference)

Solubility (25°C)

In vitro Water 30 mg/mL (61.98 mM)
DMSO 3 mg/mL warmed (6.19 mM)
Ethanol Insoluble
In vivo Add solvents individually and in order:
Saline
20 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 483.99
Formula

C24H29N7O2.HCl

CAS No. 827022-32-2
Storage powder
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03007979 Not yet recruiting Breast Cancer|Breast Carcinoma|Cancer of Breast|Malignant Tumor of Breast Washington University School of Medicine February 28, 2017 Phase 2
NCT02907918 Not yet recruiting Breast Cancer|Cancer of Breast|Breast Carcinoma Washington University School of Medicine|Pfizer February 28, 2017 Phase 2
NCT01209598 Completed Sarcoma|Liposarcoma Memorial Sloan Kettering Cancer Center|Pfizer September 23, 2010 Phase 2
NCT03054363 Not yet recruiting Breast Cancer University of Colorado, Denver March 2017 Phase 1|Phase 2
NCT03024489 Not yet recruiting Head and Neck Cancer|Locally Advanced|Unresectable Mahidol University February 2017 Phase 1|Phase 2
NCT02947685 Not yet recruiting HER-2 Positive Breast Cancer|Estrogen Receptor Positive Breast Cancer Alliance Foundation Trials, LLC.|Pfizer|German Breast Group (GBG)|Fondazione Michelangelo|PrECOG, LLC.|The Australia and New Zealand Breast Cancer Trials Group (ANZBCTG)|Alliance Foundation Trials Biorepository - Washington State University|Alliance Foundation Trials Central Imaging Core Lab - Ohio State University|Mastering Breast Cancer Initiative, LLC|Mayo Clinic Statistics and Data Center|INC Research|SOLTI Breast Cancer Research Group February 2017 Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    There are two kind of Palbociclibs available: the isethionate salt or the HCl salt. I would like to know which is the main difference between them and what are they more suitable for in terms of experiment type (cell culture or in vivo animals experiments).

  • Answer:

    This two compounds are different Palbociclib salt. S1579 is the Isethionate salt, and the S1116 is the HCl salt. you can use S1116 for oral administration while S1579 is more suitable for I.P. administration.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID