Palbociclib (PD0332991)

SKU: orb1307454

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Description

Palbociclib is an orally bioavailable, potent inhibitor of CDK4 and CDK6 (IC50 11/16 nM) with anti-tumor activity. It is widely investigated in preclinical in vitro and in vivo studies for ER-positive, HER2-negative breast cancer and other cyclin D-driven malignancies.

Research Area

Cell Biology, Immunology & Inflammation

Images & Validation

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Key Properties

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CAS Number	571190-30-2
MW	447.53
Purity	>98%
Formula	C₂₄H₂₉N₇O₂
SMILES	O=C1N(C=2C(C(C)=C1C(C)=O)=CN=C(NC3=CC=C(C=N3)N4CCNCC4)N2)C5CCCC5
Target	Kinase
Solubility	Soluble in DMSO (up to 2 mg/ml with warming)

Bioactivity

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Target IC50	MAPK:8000 nM\|DYRK1A:2000 nM\|CDK4:11 nM\|ICNI cells:8 µM\|CDK6:16 nM\|KB-C2 cells:22.573 µM\|CDK4-CyclinD3:9 nM\|CDK6-CyclinD2:16 nM\|CDK4-CyclinD1:11 nM
In Vivo	METHODS: To detect antitumor activity in vivo, Palbociclib (12.5-150 mg/kg, sodium lactate buffer (50 mmol/L, pH 4.0)) was administered orally to immunodeficient mice harboring the tumors Colo-205 or MDA-MB-435 once daily for fourteen days. RESULTS: Palbociclib showed significant anti-tumor efficacy in multiple human tumor xenograft models. In Colo-205 tumors, PD 0332991 administered for 14 days produced rapid tumor regression. METHODS: To assay antitumor activity in vivo, Palbociclib (150 mg/kg, sodium lactate buffer (50 mM, pH = 4.0)) was administered once daily for two weeks by gavage to nu/nu BALB/c mice bearing esophageal squamous cell carcinoma (ESCC) tumors EC109 or KYSE150. RESULTS: Palbociclib effectively inhibited ESCC tumor growth and lung metastasis. Read more...
In Vitro	METHODS: Malignant rhabdomyosarcoma cells G401, MP-MRT-AN (AN), KP-MRT-RY (RY), KP-MRT-NS (NS), and KP-MRT-YM (YM) were treated with Palbociclib (0-1 mM) for 24 h, and cell viability was assayed by WST. RESULTS: Palbociclib effectively inhibited AN, RY, G401 and NS cell lines in a concentration-dependent manner, with IC50s of 0.01 μM, 0.01 μM, 0.06 μM and 0.6 μM, respectively; on the contrary, the YM cell line was resistant to Palbociclib, with an IC50 >10 μM. METHODS: Human breast cancer cells MDA-MB-453 were treated with Palbociclib (0.02-10 μmol/L) for 24 h, and the cell cycle was examined by Flow Cytometry. RESULTS: Palbociclib caused G1 phase block. Read more...
Cell Research	Palbociclib (PD) is prepared in DMSO and stored ( 80°C), and then diluted with appropriate media before use. MRT cell lines, G401, MP-MRT-AN (AN), KP-MRT-RY (RY), KP-MRT-NS (NS), and KP-MRT-YM (YM) cell lines are seeded in normal growth medium into 96-well cell plates. After 24 h, the culture medium is replaced with culture medium containing Palbociclib (0.05 or 1 μM) or DMSO. Cells are cultured and treated in triplicate. Cell proliferation is determined 8 days after the treatment by WST-8 assay using a Cell Counting Kit-8. Read more...

Storage & Handling

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Storage	-20°C
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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PD-332991

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Compound Identifiers

PubChem CID

5330286 ↗

Key Properties

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No computed properties available.

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