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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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 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFy5U48xNTFyMDFOwG0> NFS4Z3Y4OiCq NIjacZlKSzVyPUmg{txO MUiyOlM6ODN2Mh?=
H2170 NFHXR3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHYfnAxNTFyMDFOwG0> M{m3U|czKGh? Mm\NTWM2OD13IN88US=> MWqyOlM6ODN2Mh?=
H520 NHjwbFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;adm4xNTFyMDFOwG0> Mk\3O|IhcA>? NHfLcpJKSzVyPUCuO|Mh|ryP MUGyOlM6ODN2Mh?=
H596 Ml:zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfHbnBQOC1zMECg{txO NWrK[|dNPzJiaB?= NXLWNWdSUUN3ME2xNkDPxE1? Mn3XNlY{QTB|NEK=
IMR-32 M4TXbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYC0POKhcA>? NUHlNmN2TE2VTx?= NHXZeWNKSzVyPUK2NUBvVQ>? Mnz2NlYzOjVzMkO=
SH-SY5Y NYT3RpB1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2[zV|Q5yqCq MVXEUXNQ M2noemlEPTB;Nke2JI5O NVjtdlczOjZ{MkWxNlM>
NGP NUT3ZXBqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUK0POKhcA>? NYX0U2RbTE2VTx?= NITWTXRKSzVyPUKuNFc4KM7:TR?= NUTacVF4OjZ{MkWxNlM>
SH-EP NGDGPZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXK0POKhcA>? NYntV5BUTE2VTx?= Mn\MTWM2OD1{LkKxNUDPxE1? MnrSNlYzOjVzMkO=
IMR-32 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo[5NUDPxE1? NIT4fZkzPCCq MortSG1UVw>? MnzTbY5lfWOnczDHNUBienKnc4S= NIfv[JozPjJ{NUGyNy=>
SH-SY5Y M2PPNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPsOIgyKM7:TR?= M335R|I1KGh? Mnm0SG1UVw>? NXjrW5N{cW6mdXPld{BIOSCjcoLld5Q> MWKyOlIzPTF{Mx?=
NGP NYLTZmVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvVeFUyKM7:TR?= MVuyOEBp M3G5ZmROW09? MnjBbY5lfWOnczDHNUBienKnc4S= MkS4NlYzOjVzMkO=
SH-EP M2TpUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnDNUDPxE1? MW[yOEBp MUDEUXNQ MYfpcoR2[2W|IFexJIFzemW|dB?= MYqyOlIzPTF{Mx?=
NGP M4XnbmZ2[3Srb36gRZN{[Xl? NXLnbmx[OC1zIN88US=> NWTyfW11OjRiaB?= MYnEUXNQ M3\KeZJm\HWlZYOgeIhmKGW6cILld5Nqd25ib3dCpHRQWDKDLNMgR2NPTTJuIHHu[OKhXEtzwrDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NVTYZoplOjZ{MkWxNlM>
IMR-32 NUjoXYhJTnWldHnvckBCe3OjeR?= NFPBUVMxNTFizszN NXrOTZByOjRiaB?= NITP[nRFVVOR NVj4PWJZemWmdXPld{B1cGViZYjwdoV{e2mxbjDv[uKhXE:SMlGsxsBES06HMjygZY5lyqCWS{JCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MoXENlYzOjVzMkO=
U-CH2 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWKwMVEh|ryP NH;BeIw4OiCq MnTmTWM2OD13MD6yJI5O MWSyOlE5Ozl{NR?=
U-CH3 NWWxVmVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnDNE0yKM7:TR?= NHr5VWQ4OiCq MkT2TWM2OD13MjDuUS=> MUeyOlE5Ozl{NR?=
U-CH6 M2XwSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWiwMVEh|ryP MW[3NkBp MlS4TWM2OD17MDDuUS=> NFG0c3ozPjF6M{myOS=>
U-CH7 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPObZUxNTFizszN Mn;CO|IhcA>? MXrJR|UxRTl6IH7N NWm0U49HOjZzOEO5NlU>
U-CH11 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV[wMVEh|ryP M3n5dFczKGh? MmO4TWM2OD1|NECgcm0> MoHDNlYyQDN7MkW=
MCF7 NUPZXI1uTnWldHnvckBCe3OjeR?= MV2yMlUuOjVyIH7N NH;uRo4zPCCq NVjiTJBQemWmdXPld{BT[iCyaH;zdIhwenmuYYTpc44> M4rEPFI2QTlzOEG3
MV4-11 MonJRZBweHSxc3nzJGF{e2G7 MV2wMlUh|ryP MnX2NlQhcA>? Morw[Y5p[W6lZYOgZZBweHSxc3nzJIlv\HWlZXSgZpkhe2:{YX\lcoljKGGwZDDBR|IzOA>? Mo\TNlU1QDd7MUe=
MOLM13 NUDudocySXCxcITvd4l{KEG|c3H5 MYWwMlUh|ryP MWiyOEBp MYjlcohidmOnczDhdI9xfG:|aYOgbY5lfWOnZDDifUB{d3KjZnXubYIh[W6mIFHDNlIx NYnEU4pxOjV2OEe5NVc>
MOLM13-ITD alone M1ToSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGj3[JpKSzVyPUCuNFg6KMLzIECuNFA6KM7:TR?= MnvyNlU1QDd7MUe=
MV4-11-ITD alone NF6wNFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHrVnNKSzVyPUCuNFkzKMLzIECuNFA5KM7:TR?= Ml;ENlU1QDd7MUe=
MOLM13-ITD/D835Y MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrxV2JXUUN3ME2wMlEyPCEEsTCwMlAyOSEQvF2= MXOyOVQ5PzlzNx?=
MV4-11-ITD/D835V MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDnTWM2OD1yLkGxOkDDuSByLkCxNUDPxE1? MUSyOVQ5PzlzNx?=
MV4-11-ITD/D835V Mnm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPVPFhSUUN3ME2wMlExOiEEsTCwMlAxPiEQvF2= MnPhNlU1QDd7MUe=
MV4-11-ITD/F691L MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXPO5AxUUN3ME2wMlEyOiEEsTCwMlAyPSEQvF2= MoS2NlU1QDd7MUe=
MV4-11-ITD/N841K NYL4foU5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fROWlEPTB;MD6xNVMhyrFiMD6wNFIh|ryP MorwNlU1QDd7MUe=
U937-FLT3 WT NXXlcHFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLsTWM2OD1yLkGwNkDDuSByLkCxN{DPxE1? NYPLdYVZOjV2OEe5NVc>

... 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]
- Collapse

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]
- Collapse
  • 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]
- Collapse
  • 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