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PD0332991 Isethionate

(CAS No:827022-33-3)
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.
CAS No:827022-33-3
Molecular Weight(MW):573.66
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 827022-33-3
Molecular formula(MF) C24H29N7O2.C2H6O4S
Molecular Weight(MW): 573.66
Alias
Solubility
In vitro Water 50 mg/mL warmed (87.15 mM)
DMSO <1 mg/mL
Ethanol <1 mg/mL
In vivo Saline 30 mg/mL
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)
CDK2/CyclinE2 [1]
(Cell-free assay)
CDK2/CyclinA [1]
(Cell-free assay)
9 nM 11 nM 15 nM >10 μM >10 μM
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 Growth Inhibition Assay 0-100 μM 72 h IC50=9 μM 26390342
H2170 Growth Inhibition Assay 0-100 μM 72 h IC50=5 μM 26390342
H520 Growth Inhibition Assay 0-100 μM 72 h IC50=0.73 μM 26390342
H596 Growth Inhibition Assay 0-100 μM 72 h IC50=12 μM 26390342
IMR-32 Growth Inhibition Assay 48 h DMSO IC50=261 nM 26225123
SH-SY5Y Growth Inhibition Assay 48 h DMSO IC50=676 nM 26225123
NGP Growth Inhibition Assay 48 h DMSO IC50=2.077 μM 26225123
SH-EP Growth Inhibition Assay 48 h DMSO IC50=2.211 μM 26225123
IMR-32 Growth Inhibition Assay 1 μM 24 h DMSO induces G1 arrest 26225123
SH-SY5Y Growth Inhibition Assay 1 μM 24 h DMSO induces G1 arrest 26225123
NGP Growth Inhibition Assay 1 μM 24 h DMSO induces G1 arrest 26225123
SH-EP Growth Inhibition Assay 1 μM 24 h DMSO induces G1 arrest 26225123
NGP Fuction Assay 0-1 μM 24 h DMSO reduces the expression of TOP2A, CCNE2, and TK1 in a dose-dependent manner 26225123
IMR-32 Fuction Assay 0-1 μM 24 h DMSO reduces the expression of TOP2A, CCNE2, and TK1 in a dose-dependent manner 26225123
U-CH2 Growth Inhibition Assay 0-1 μM 72 h IC50=50.2 nM 26183925
U-CH3 Growth Inhibition Assay 0-1 μM 72 h IC50=52 nM 26183925
U-CH6 Growth Inhibition Assay 0-1 μM 72 h IC50=90 nM 26183925
U-CH7 Growth Inhibition Assay 0-1 μM 72 h IC50=98 nM 26183925
U-CH11 Growth Inhibition Assay 0-1 μM 72 h IC50=340 nM 26183925
MCF7 Fuction Assay 2.5-250 nM 24 h reduces Rb phosphorylation 25991817
MV4-11 Apoptosis Assay 0.5 μM 24 h enhances apoptosis induced by sorafenib and AC220 25487917
MOLM13 Apoptosis Assay 0.5 μM 24 h enhances apoptosis induced by sorafenib and AC220 25487917
MOLM13-ITD alone Growth Inhibition Assay IC50=0.089 ± 0.009 μM 25487917
MV4-11-ITD alone Growth Inhibition Assay IC50=0.092 ± 0.008 μM 25487917
MOLM13-ITD/D835Y Growth Inhibition Assay IC50=0.114 ± 0.011 μM 25487917
MV4-11-ITD/D835V Growth Inhibition Assay IC50=0.116 ± 0.011 μM 25487917
MV4-11-ITD/D835V Growth Inhibition Assay IC50=0.102 ± 0.006 μM 25487917
MV4-11-ITD/F691L Growth Inhibition Assay IC50=0.112 ± 0.015 μM 25487917
MV4-11-ITD/N841K Growth Inhibition Assay IC50=0.113 ± 0.002 μM 25487917
U937-FLT3 WT Growth Inhibition Assay IC50=0.102 ± 0.013 μM 25487917

... Click to View More Cell Line Experimental Data

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]