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.

Size Price Stock Quantity  
USD 147 In stock
USD 270 In stock
USD 370 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 21 Publications

Purity & Quality Control

Choose Selective CDK Inhibitors

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 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHRNE0yODBizszN NG\FVo84OiCq Mn:wTWM2OD17IN88US=> MUWyOlM6ODN2Mh?=
H2170 NVrCPXhyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX[wMVExOCEQvF2= MUm3NkBp MoDFTWM2OD13IN88US=> NH3mUlAzPjN7MEO0Ni=>
H520 MmLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEmwSnIxNTFyMDFOwG0> MYK3NkBp NHqwNINKSzVyPUCuO|Mh|ryP MVeyOlM6ODN2Mh?=
H596 NIXL[lBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zVPFAuOTByIN88US=> NGC3fJE4OiCq M2nhemlEPTB;MUKg{txO NYHmbXN2OjZ|OUCzOFI>
IMR-32 MmG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLiSHQ1QMLiaB?= MXzEUXNQ NFTPeIRKSzVyPUK2NUBvVQ>? NEnC[VEzPjJ{NUGyNy=>
SH-SY5Y NHHWRo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUW0POKhcA>? MYXEUXNQ NWHMSG52UUN3ME22O|Yhdk1? NIiycZMzPjJ{NUGyNy=>
NGP M4PhWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF22c5c1QMLiaB?= M3[4cmROW09? NEC5OFNKSzVyPUKuNFc4KM7:TR?= MVOyOlIzPTF{Mx?=
SH-EP MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rBb|Q5yqCq NWLCW49GTE2VTx?= NXfq[YVzUUN3ME2yMlIyOSEQvF2= NHrpXnMzPjJ{NUGyNy=>
IMR-32 M3KxU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vJS|Eh|ryP NXry[mxXOjRiaB?= NXrNSIp3TE2VTx?= M1zoPYlv\HWlZYOgS|Eh[XK{ZYP0 MWiyOlIzPTF{Mx?=
SH-SY5Y MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXmNUDPxE1? NHrySmUzPCCq MnizSG1UVw>? MYfpcoR2[2W|IFexJIFzemW|dB?= MkLnNlYzOjVzMkO=
NGP NVnRc2RiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjNWXoyKM7:TR?= NHjtRZQzPCCq MY\EUXNQ NH3wc5pqdmS3Y3XzJGcyKGG{cnXzeC=> NFzYNVEzPjJ{NUGyNy=>
SH-EP MoixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX[xJO69VQ>? NWLwbZNUOjRiaB?= NH\qU2ZFVVOR MVHpcoR2[2W|IFexJIFzemW|dB?= MmnnNlYzOjVzMkO=
NGP MnH6SpVkfGmxbjDBd5NigQ>? NUTncIx4OC1zIN88US=> Mo[0NlQhcA>? M1jwZ2ROW09? NXS3VmNFemWmdXPld{B1cGViZYjwdoV{e2mxbjDv[uKhXE:SMlGsxsBES06HMjygZY5lyqCWS{JCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MljUNlYzOjVzMkO=
IMR-32 NUfpZYk6TnWldHnvckBCe3OjeR?= NWjheo01OC1zIN88US=> MWSyOEBp M17ZZWROW09? NIjDS25z\WS3Y3XzJJRp\SCneIDy[ZN{cW:wIH;mxsBVV1B{QT|CpGNEVkV{LDDhcoTDqFSNMdMgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MnLFNlYzOjVzMkO=
U-CH2 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETnT2oxNTFizszN MkTSO|IhcA>? M3S2[WlEPTB;NUCuNkBvVQ>? M373c|I3OTh|OUK1
U-CH3 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\aSIlOOC1zIN88US=> NVvPZldiPzJiaB?= NVzDRY5ZUUN3ME21NkBvVQ>? NV32TI5nOjZzOEO5NlU>
U-CH6 M325XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljZNE0yKM7:TR?= MVK3NkBp NWnBbHduUUN3ME25NEBvVQ>? MUOyOlE5Ozl{NR?=
U-CH7 MkDFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHuenptOC1zIN88US=> M4DDXFczKGh? MnzOTWM2OD17ODDuUS=> NUXFdGNvOjZzOEO5NlU>
U-CH11 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1K1d|AuOSEQvF2= NXrK[Hh7PzJiaB?= MlnLTWM2OD1|NECgcm0> NVjXe2tWOjZzOEO5NlU>
MCF7 M3LUcmZ2[3Srb36gRZN{[Xl? M13JRVIvPS1{NUCgcm0> Mmr2NlQhcA>? Ml\UdoVlfWOnczDSZkBxcG:|cHjvdplt[XSrb36= MVOyOVk6OThzNx?=
MV4-11 NWPoW3V4SXCxcITvd4l{KEG|c3H5 NVHrTop5OC53IN88US=> NV\FbXJTOjRiaB?= MXjlcohidmOnczDhdI9xfG:|aYOgbY5lfWOnZDDifUB{d3KjZnXubYIh[W6mIFHDNlIx MUOyOVQ5PzlzNx?=
MOLM13 MnfxRZBweHSxc3nzJGF{e2G7 MUmwMlUh|ryP NVq0bZp3OjRiaB?= MX7lcohidmOnczDhdI9xfG:|aYOgbY5lfWOnZDDifUB{d3KjZnXubYIh[W6mIFHDNlIx M2T4flI2PDh5OUG3
MOLM13-ITD alone NH75fHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{O4N2lEPTB;MD6wPFkhyrFiMD6wNFkh|ryP MonUNlU1QDd7MUe=
MV4-11-ITD alone NWTaS5hsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTBwMEmyJOKyKDBwMEC4JO69VQ>? NEDJOGszPTR6N{mxOy=>
MOLM13-ITD/D835Y Mkm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPYTWM2OD1yLkGxOEDDuSByLkCxNUDPxE1? MWiyOVQ5PzlzNx?=
MV4-11-ITD/D835V M3jwNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7RSJMxUUN3ME2wMlEyPiEEsTCwMlAyOSEQvF2= NI[0cI4zPTR6N{mxOy=>
MV4-11-ITD/D835V NFPwdWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDvWXlKSzVyPUCuNVAzKMLzIECuNFA3KM7:TR?= MlnoNlU1QDd7MUe=
MV4-11-ITD/F691L NF;hbWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjRVlQyUUN3ME2wMlEyOiEEsTCwMlAyPSEQvF2= NILMelkzPTR6N{mxOy=>
MV4-11-ITD/N841K NHrpRndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnaZ5FKSzVyPUCuNVE{KMLzIECuNFAzKM7:TR?= MXGyOVQ5PzlzNx?=
U937-FLT3 WT MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWD0fI5{UUN3ME2wMlExOiEEsTCwMlAyOyEQvF2= MmHWNlU1QDd7MUe=

... 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

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)

  • Mass
    Concentration
    Volume
    Molecular Weight

*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 )

  • C1
    V1
    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):
    C7=C6/X C7: LOG(C7):
    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

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

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
NCT03609047 Not yet recruiting Breast Cancer Stage II|Breast Cancer Stage III European Organisation for Research and Treatment of Cancer - EORTC|Pfizer May 7 2019 Phase 2
NCT03609047 Not yet recruiting Breast Cancer Stage II|Breast Cancer Stage III European Organisation for Research and Treatment of Cancer - EORTC|Pfizer May 7 2019 Phase 2
NCT03820830 Not yet recruiting Breast Cancer Recurrent International Breast Cancer Study Group|Pfizer May 1 2019 Phase 3
NCT03870919 Not yet recruiting Breast Cancer Stage IV|Radiotherapy|Surgery UNICANCER|Pfizer May 15 2019 Not Applicable
NCT03820830 Not yet recruiting Breast Cancer Recurrent International Breast Cancer Study Group|Pfizer May 1 2019 Phase 3
NCT03870919 Not yet recruiting Breast Cancer Stage IV|Radiotherapy|Surgery UNICANCER|Pfizer May 15 2019 Not Applicable

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:

    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.

CDK Signaling Pathway Map

CDK Inhibitors with Unique Features

Related CDK Products5

Tags: buy Palbociclib (PD0332991) Isethionate | Palbociclib (PD0332991) Isethionate supplier | purchase Palbociclib (PD0332991) Isethionate | Palbociclib (PD0332991) Isethionate cost | Palbociclib (PD0332991) Isethionate manufacturer | order Palbociclib (PD0332991) Isethionate | Palbociclib (PD0332991) Isethionate distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID