Palbociclib (PD0332991) Isethionate

Licensed and Manufactured by Pfizer Catalog No.S1579

Palbociclib (PD0332991) Isethionate Chemical Structure

Molecular Weight(MW): 573.66

Palbociclib (PD0332991) Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

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Cited by 47 Publications

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Biological Activity

Description Palbociclib (PD0332991) Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.
Features The 1st specific inhibitor for CDK4/6 to show promise in multiple 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 exhibits absolute selectivity for CDK4/6 with little or no activity against other CDKs. PD 0332991 is effective at reducing Rb phosphorylation at Ser780 and Ser795 in MDA-MB-435 breast carcinoma cells with IC50 of 66 nM and 63 nM, respectively. PD 0332991 is a potent inhibitor of cell growth and suppresses DNA replication by preventing cells from entering S phase. PD 0332991 inhibits thymidine incorporation into the DNA of Rb-positive human breast (such as MDA-MB-435, MCF-7), colon (H1299), and lung carcinomas (Colo-205) as well as human leukemias (CRRF-CEM and K562), with IC50 values ranging from 0.04-0.17 μM. PD 0332991 significant increases the percentage of MDA-MB-453 in G1 period. [1] PD 0332991 inhibits phosphorylation of Rb in cycling CD138+ primary bone marrow myeloma cells, nontransformed primary B cells, MM1.S and CAG HMCLs cells line with IC50 of <0.1 μM, 0.05 μM, and 60-70 nM, respectively. PD 0332991 treatment also induces G1 arrest of CD138+ primary bone marrow myeloma and nontransformed primary B cells. PD 0332991 induces G1 arrest in MM1.S with IC50 of ~0.05 μM. [2] PD 0332991 preferentially inhibits proliferation of luminal estrogen receptor-positive (including HER2-positive) human breast cancer cell lines. PD 0332991 increases gene expression of pRb and cyclin D1 and decreases gene expression of CDKN2A (p16) in most sensitive lines. PD 0332991 enhances sensitivity to tamoxifen in cell lines with conditioned resistance to ER blockade. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
H157 M1LwN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYGwMVExOCEQvF2= MmOyO|IhcA>? Ml70TWM2OD17IN88US=> MWOyOlM6ODN2Mh?=
H2170 NVnDN3J3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPINE0yODBizszN MYC3NkBp Ml\6TWM2OD13IN88US=> M4fTSVI3OzlyM{Sy
H520 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFT2[G0xNTFyMDFOwG0> MVi3NkBp NUT0bldUUUN3ME2wMlc{KM7:TR?= NXnPb29uOjZ|OUCzOFI>
H596 NFezVWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXINE0yODBizszN MYG3NkBp M2[zOWlEPTB;MUKg{txO NHOy[I8zPjN7MEO0Ni=>
IMR-32 MmH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzle5VZPDkEoHi= M{nHc2ROW09? NVTacWJ4UUN3ME2yOlEhdk1? NIi4dlUzPjJ{NUGyNy=>
SH-SY5Y NUX0RnFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVG0POKhcA>? M4XXd2ROW09? NX2wV4l6UUN3ME22O|Yhdk1? NV7BbGxzOjZ{MkWxNlM>
NGP MoDOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3POFjDqGh? Mo\BSG1UVw>? MnzXTWM2OD1{LkC3O{DPxE1? MV[yOlIzPTF{Mx?=
SH-EP M2fUUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWm0POKhcA>? MWLEUXNQ NF3XbYhKSzVyPUKuNlEyKM7:TR?= NW\LZ2FrOjZ{MkWxNlM>
IMR-32 NE\wS25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1WyT|Eh|ryP MmLVNlQhcA>? NFLPW5dFVVOR MkDXbY5lfWOnczDHNUBienKnc4S= NGj5[XczPjJ{NUGyNy=>
SH-SY5Y MlfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1SwelEh|ryP M2r2NFI1KGh? Ml3uSG1UVw>? NFXreoVqdmS3Y3XzJGcyKGG{cnXzeC=> NFLm[4kzPjJ{NUGyNy=>
NGP NEjMRXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DaVVEh|ryP MXKyOEBp MXnEUXNQ NXLjbmxscW6mdXPld{BIOSCjcoLld5Q> NVjMPYR3OjZ{MkWxNlM>
SH-EP M4fHNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfHNUDPxE1? NHvkUoYzPCCq MkPhSG1UVw>? NGDrZ|lqdmS3Y3XzJGcyKGG{cnXzeC=> NFK4OokzPjJ{NUGyNy=>
NGP M3;lfGZ2[3Srb36gRZN{[Xl? MV:wMVEh|ryP NHHVVGkzPCCq M3jidWROW09? MoH2doVlfWOnczD0bIUh\XiycnXzd4lwdiCxZtMgWG9ROkFuwrDDR25GOixiYX7kxsBVUzIEoHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M1;uVlI3OjJ3MUKz
IMR-32 MVjGeYN1cW:wIFHzd4F6 NHv6NHkxNTFizszN NUfqUWc3OjRiaB?= M3jyT2ROW09? M3nxUpJm\HWlZYOgeIhmKGW6cILld5Nqd25ib3dCpHRQWDKDLNMgR2NPTTJuIHHu[OKhXEtzwrDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NEfWXXozPjJ{NUGyNy=>
U-CH2 NXvoR5Y5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXLXFF3OC1zIN88US=> M3[4cFczKGh? NIrQWGpKSzVyPUWwMlIhdk1? MWWyOlE5Ozl{NR?=
U-CH3 NVTufFFpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\pNE0yKM7:TR?= M3PwcVczKGh? MnfRTWM2OD13MjDuUS=> NVXvZZU2OjZzOEO5NlU>
U-CH6 MnvlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDHdlZEOC1zIN88US=> NF20[I44OiCq NHf3VotKSzVyPUmwJI5O M{T0RlI3OTh|OUK1
U-CH7 NV;YWlJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnH3NE0yKM7:TR?= NH;3b4M4OiCq MoruTWM2OD17ODDuUS=> M3qw[VI3OTh|OUK1
U-CH11 MnjhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTN[oMxNTFizszN M4HZUFczKGh? M17Qe2lEPTB;M{SwJI5O Mly0NlYyQDN7MkW=
MCF7 NFnGT3ZHfWO2aX;uJGF{e2G7 M4fFOFIvPS1{NUCgcm0> NFnmUGozPCCq MUDy[YR2[2W|IGLiJJBpd3OyaH;yfYxifGmxbh?= NUn6VJpHOjV7OUG4NVc>
MV4-11 NHW5OWxCeG:ydH;zbZMhSXO|YYm= M{[1flAvPSEQvF2= Mnv2NlQhcA>? MVHlcohidmOnczDhdI9xfG:|aYOgbY5lfWOnZDDifUB{d3KjZnXubYIh[W6mIFHDNlIx NHf3dmQzPTR6N{mxOy=>
MOLM13 NXPaWZRpSXCxcITvd4l{KEG|c3H5 MkTBNE42KM7:TR?= MnHhNlQhcA>? M4nIXIVvcGGwY3XzJIFxd3C2b4Ppd{BqdmS3Y3XkJIJ6KHOxcnHm[Y5q[iCjbnSgRWMzOjB? MXWyOVQ5PzlzNx?=
MOLM13-ITD alone NF\nPHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkn5TWM2OD1yLkC4PUDDuSByLkCwPUDPxE1? NHuyNnQzPTR6N{mxOy=>
MV4-11-ITD alone MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkm5TWM2OD1yLkC5NkDDuSByLkCwPEDPxE1? M{fxT|I2PDh5OUG3
MOLM13-ITD/D835Y MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTBwMUG0JOKyKDBwMEGxJO69VQ>? MWiyOVQ5PzlzNx?=
MV4-11-ITD/D835V Mn7xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTBwMUG2JOKyKDBwMEGxJO69VQ>? M3PHZVI2PDh5OUG3
MV4-11-ITD/D835V NWDk[4VzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTBwMUCyJOKyKDBwMEC2JO69VQ>? NUH2RpdGOjV2OEe5NVc>
MV4-11-ITD/F691L NHTXZWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXuwR4lLUUN3ME2wMlEyOiEEsTCwMlAyPSEQvF2= MmfvNlU1QDd7MUe=
MV4-11-ITD/N841K MornS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHETWM2OD1yLkGxN{DDuSByLkCwNkDPxE1? NEjJV|IzPTR6N{mxOy=>
U937-FLT3 WT NH7jXpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\tTWM2OD1yLkGwNkDDuSByLkCxN{DPxE1? M{L5R|I2PDh5OUG3

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
RB1 (pT821) / RB1 (pS780); 

PubMed: 30300583     


Immunoblots showing dose-dependent impact of 72 hr palbociclib treatment on indicated protein levels in Kasumi-1 and SKNO-1 cells.

pAMPKα(T172) / AMPKα; 

PubMed: 28453226     


Dose-dependent response of palbociclib on AMPK‐related molecules. HCC cells were treated with different concentrations of palbociclib for 24 h. The phosphorylation of the indicated proteins was determined by western blotting. 

pULK1(S317) / ULK1; 

PubMed: 28453226     


Dose-dependent response of palbociclib on AMPK‐related molecules. HCC cells were treated with different concentrations of palbociclib for 24 h. The phosphorylation of the indicated proteins was determined by western blotting. 

c-Jun / p-c-Jun / NFκB(p50); 

PubMed: 26540629     


The expression of c-Jun and phosphorylated c-Jun was assessed using western blot after the cells were treated with palbociclib. 

p38 / p-P38 / JNK / p-JNK; 

PubMed: 26540629     


MAPK pathway-related proteins, p38, ERK, JNK expression levels were detected.

30300583 28453226 26540629
Growth inhibition assay
Cell viability; 

PubMed: 28453226     


Dose- and time-dependent effects of palbociclib on cell viability in three HCC cell lines. Hep3B, Huh7, and PLC5 cells were treated with palbociclib at the indicated concentrations for 24 or 48 h and assayed by MTT. The solvent (DMSO) concentration in each sample is equal (0.7%).

IC50; 

PubMed: 27099147     


Dose-response curve of ITD+ (red) or control (black) leukemic cells with CDK4/6 inhibitor palbociclib. Cells were incubated with increasing concentrations for 72 hours. Cell viability and proliferation were assessed by using the CTG assay. IC50 values were calculated by using GraphPad Prism software. Error bars indicate ± SEM.

28453226 27099147
Immunofluorescence
γH2AX(Ser139); 

PubMed: 29669860     


Representative maximum‐intensity projections of MCF7 cells treated with the 1 μM palbociclib and/or 7.5 nM bortezomib. Note that 7.5 nM bortezomib inhibits proteasome only partially. Fixed and permeabilized cells were stained with Alexa Fluor 488‐conjugated Ki67 antibody, Alexa Fluor 647‐conjugated phospho‐Histone H2A.X (γH2AX) (pSer139) antibody, and DAPI. All images were acquired with the same magnification, and scale bar is 20 μm.

LC3B; 

PubMed: 28453226     


LC3B immunofluorescence in palbociclib‐treated Hep3B cells. Arrowheads indicate LC3‐positive autophagosomes. Nuclei were counterstained with DAPI (blue). 

29669860 28453226
ELISA
PGE2; 

PubMed: 26540629     


The supernatant of control and 7.5 μM palbociclib-treated cells was collected and stored at −80°C. PGE2 secretion was detected using ELISA.

26540629
In vivo PD 0332991(150 mg/kg) produces rapid Colo-205 colon carcinoma xenografts regressions and a corresponding tumor growth delay. PD 0332991 (150 mg/kg) induces complete tumor stasis and cell kill in MDA-MB-435 breast carcinoma. PD 0332991 (150 mg/kg) also induces significant tumor regression in mice bearing the SF-295 glioblastoma xenografts, and in ZR-75-1 breast and PC-3 prostate tumor models (complete suppression of tumor growth). PD 0332991 (150 mg/kg) suppresses Rb Ser780 phosphorylation in MDA-MB-435 breast carcinoma over the full 24-hour period. PD 0332991 (150 mg/kg) down-regulates expression of four E2F-regulated genes CDC2, CCNE2, TK1, and TOP2A in Colo-205 carcinoma xenografts. [1] PD 0332991 also rapidly inhibits myeloma tumor growth. [2]

Protocol

Kinase Assay:[4]
+ Expand

CDK activity assays:

CDK assays for IC50 determinations and kinetic evaluation 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 reaction volume 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) containing 0.25 μCi of [γ-32P]ATP, 20 ng of enzyme, 1 μg of GST•RB-Cterm, and appropriate dilutions of inhibitor. All components except the [γ-32P]ATP are added to the wells, and placed on a plate mixer for 2 min. The reaction is started by adding the [γ-32P]ATP, and incubated at 25℃ for 15 min. The reaction is terminated by addition of 0.1 mL of 20% trichloroacetic acid, and the plate is kept at 4 ℃ for at least 1 hr to allow the substrate to precipitate. The wells are then washed five times with 0.2 mL of 10% trichloroacetic acid, and radioactive incorporation is determined with a β plate counter.
Cell Research:[3]
+ Expand
  • Cell lines: Human breast cancer cells MDA-MB-435
  • Concentrations: 2 μM
  • Incubation Time: 6 days
  • Method: Cells are seeded in duplicate at 5,000 to 10,000 cells per well in 24-well plates. The day after plating, different concentrations of PD 0332991 are added. Control wells without drug are also seeded. At the end of incubation, cells are trypsinizated and placed in Isotone solution and counted immediately using a Coulter Z2 particle counter.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Human colon carcinoma xenografts Colo-205
  • Formulation: Solution in sodium lactate buffer (50 mM, pH 4.0)
  • Dosages: 150 mg/kg
  • Administration: o.p. injection every day
    (Only for Reference)

Solubility (25°C)

In vitro Water 10 mg/mL warmed (17.43 mM)
DMSO Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
saline (with warming)
For best results, use promptly after mixing.
10mg/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 573.66
Formula

C24H29N7O2.C2H6O4S

CAS No. 827022-33-3
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03870919 Not yet recruiting Drug: Palbociclib|Other: locoregional treatment Breast Cancer Stage IV|Radiotherapy|Surgery UNICANCER|Pfizer October 15 2019 Not Applicable
NCT03900884 Not yet recruiting Drug: Venetoclax|Drug: Palbociclib|Drug: Letrozole Breast Neoplasm Female Peter MacCallum Cancer Centre Australia September 2019 Phase 1
NCT03844997 Recruiting Drug: Palcociclib|Drug: CPX-351 Acute Myeloid Leukemia|AML Aziz Nazha|Case Comprehensive Cancer Center May 31 2019 Phase 1|Phase 2

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.

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Frequently Asked Questions

  • Question 1:

    What is the best vehicle for palbociclib for in vitro and in vivo?

  • Answer:

    You can use water for vitro use and Saline for vivo use.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID