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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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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
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. Science. 2019 Dec 13;366(6471):eaaw2106.
Huh7 and skHep1 cell lines 0.5 μM 14 days Induced cellular senescence, characterized by flat morphology and SAβGAL positivity Gut. 2017 Jul;66(7):1286-1296.
human liver cancer cell lines 1 μM 3 days Suppressed cell proliferation by promoting a reversible cell cycle arrest Gut. 2017 Jul;66(7):1286-1296.
IB115 cells 1-4 μM 72 h Palbociclib reduced Rb phosphorylation, decreased cell growth, and induced apoptosis. J Hematol Oncol. 2017 Jun 19;10(1):123.
IB111 cells 1-4 μM 72 h Palbociclib reduced Rb phosphorylation, decreased cell growth, and induced apoptosis. J Hematol Oncol. 2017 Jun 19;10(1):123.

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 Nat Commun. 2023 Jul 14;14(1):4212.
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 Gut. 2017 Jul;66(7):1286-1296.
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. J Hematol Oncol. 2017 Jun 19;10(1):123.

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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