Palbociclib monohydrochloride

SKU: orb1300948

Description

Research Area

Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	827022-32-2
MW	483.99
Purity	>99.99% (May vary between batches)
Formula	C₂₄H₂₉N₇O₂·HCl
SMILES	Cl.CC(=O)c1c(C)c2cnc(Nc3ccc(cn3)N3CCNCC3)nc2n(C2CCCC2)c1=O
Target	CDK
Solubility	DMSO:5 mg/mL (10.33 mM);H2O:20 mg/mL (41.32 mM)

Bioactivity

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Target IC50	CDK6-CyclinD2:15 nM (cell free)\|CDK4-CyclinD1:11 nM (cell free)\|CDK4-CyclinD3:9 nM (cell free)\|MAPK:8000 nM\|DYRK1A:2000 nM
In Vivo	Oral administration of PD 0332991 to mice bearing the Colo-205 human colon carcinoma produces marked tumor regression. Therapeutic doses of PD 0332991 cause elimination of phospho-Rb and the proliferative marker Ki-67 in tumor tissue and down-regulation of genes under the transcriptional control of E2F . Read more...
In Vitro	PD 0332991 is a highly specific inhibitor of Cdk4 (IC50, 0.011 micromol/L) and Cdk6 (IC50, 0.016 micromol/L). It is a potent antiproliferative agent against retinoblastoma (Rb)-positive tumor cells in vitro, inducing an exclusive G1 arrest, with a concomitant reduction of phospho-Ser780/Ser795 on the Rb protein . In all of the cell lines except KP-MRT-YM, PD 0332991 inhibited cell proliferation >50% (IC50 values 0.01 to 0.6 μM), and induced G1-phase cell cycle arrest. The sensitivity of the MRT cell lines to PD 0332991 was inversely correlated with p16 expression. KP-MRT-YM cells overexpress p16 and were resistant to the growth inhibitory effect of PD 0332991 . Cell lines representing luminal estrogen receptor-positive (ER+) subtype (including those that are HER2 amplified) were most sensitive to growth inhibition by PD 0332991 while nonluminal/basal subtypes were most resistant . Read more...
Cell Research	Cells were seeded at 2 × 10^4 per well in a 96-well Cytostar T plate and incubated overnight to allow cells to attach. Varying concentrations of PD 0332991 were added to the wells and incubated for 24 hours at 37°C. [14C]thymidine (0.1 μCi) was added to each well and incorporation of the radiolabel was allowed to proceed for 72 hours. Incorporated radioactivity was determined with a β plate counter . Read more...
Animal Research	Mice (18–22 g) were randomized and then implanted s.c. with tumor fragments (～30 mg) into the region of the right axilla. Treatment was initiated when tumors reached 100 to 150 mg. PD 0332991 was given according to the schedule and dose indicated in the table and figure legends by gavage as a solution in sodium lactate buffer (50 mmol/L, pH 4.0) based on mean group body weight. In all experiments, there were 12 mice in the control group and 8 mice each in the treated groups. Additional details for each experiment are given in the table legends . Read more...

Storage & Handling

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Storage	keep away from moisture,keep away from direct sunlight \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Cyclin dependent kinase, CDK, CDK6/CyclinD2, CDK4/CyclinD1, CDK4/CyclinD3, cell cycle, Breast cancer, PD0332991 Hydrochloride, PD-0332991 Hydrochloride, PD 0332991 hydrochloride, PD 0332991 Hydrochloride, PD 0332991 monohydrochloride, Palbociclib, Palbociclib (PD-0332991) HCl, Palbociclib hydrochloride, Palbociclib Hydrochloride, Palbociclib monohydrochloride, Palbociclib Monohydrochloride, inhibit, estrogen receptor, Inhibitor, HCC, HER2, hepatocellular carcinoma

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Compound Identifiers

PubChem CID

11431660 ↗

Key Properties

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No computed properties available.

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