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Chemical Structure| 827022-32-2 Chemical Structure| 827022-32-2

Structure of Palbociclib monohydrochloride
CAS No.: 827022-32-2

Chemical Structure| 827022-32-2

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CAS No.: 827022-32-2

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Palbociclib (PD 0332991) monohydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib monohydrochloride exhibits potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which is valuable for research on HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.

Synonyms: PD 0332991 monohydrochloride; PD 0332991 (hydrochloride); Palbociclib

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Product Details of Palbociclib monohydrochloride

CAS No. :827022-32-2
Formula : C24H30ClN7O2
M.W : 483.99
SMILES Code : O=C1C(C(C)=O)=C(C)C2=CN=C(NC3=NC=C(N4CCNCC4)C=C3)N=C2N1C5CCCC5.[H]Cl
Synonyms :
PD 0332991 monohydrochloride; PD 0332991 (hydrochloride); Palbociclib
MDL No. :MFCD22420809
InChI Key :STEQOHNDWONVIF-UHFFFAOYSA-N
Pubchem ID :11431660

Safety of Palbociclib monohydrochloride

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Palbociclib monohydrochloride

Hedgehog

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
IB115 cells 1-4 μM 72 h Palbociclib reduced Rb phosphorylation, decreased cell growth, and induced apoptosis. PMC5477309
Breast cancer cells 500 nM 48 h To test the inhibitory effect of Palbociclib on endogenous CDK4 activity, results showed that Palbociclib did not significantly inhibit the activity of endogenous CDK4 complexes. PMC7592119
Huh7 and skHep1 cell lines 0.5 μM 14 days Induced cellular senescence, characterized by flat morphology and SAβGAL positivity PMC5512174
IB111 cells 1-4 μM 72 h Palbociclib reduced Rb phosphorylation, decreased cell growth, and induced apoptosis. PMC5477309
Human liver cancer cell lines 1 μM 3 days Suppressed cell proliferation by promoting a reversible cell cycle arrest PMC5512174

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Subcutaneous tumor model generated by A549 cells Oral 100 mg/kg Once daily, 5 days/week The combination of GAA and CDK4/6i significantly inhibited tumor growth PMC10349134
Mice Genetically engineered liver cancer model and human HCC xenografts Oral 100 mg/kg Once daily for 1 week or 16 days Suppressed tumour growth and significantly extended survival when used alone or in combination with sorafenib PMC5512174
Rag γ2C?/? mice DDLPS xenograft model Oral gavage 130 mg/kg Five times per week for 3 weeks Palbociclib significantly slowed tumour growth rate and prolonged progression-free survival. PMC5477309

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.07mL

0.41mL

0.21mL

10.33mL

2.07mL

1.03mL

20.66mL

4.13mL

2.07mL

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