Palbociclib dihydrochloride (Synonyms: PD-0332991 dihydrochloride)

Cat. No.: HY-50767B: FAQs
Data Sheet Handling Instructions

Molarity Calculator

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

For research use only. We do not sell to patients.

Palbociclib dihydrochloride Chemical Structure

CAS No. : 1831842-69-3

Size		Stock
MOQ		Minimum order quantity
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote
Other size		Get quote

Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of Palbociclib dihydrochloride:

Palbociclib Palbociclib monohydrochloride Palbociclib isethionate

Other Forms of Palbociclib dihydrochloride:

157 Publications Citing Use of MCE Palbociclib dihydrochloride

IHC

: Palbociclib dihydrochloride purchased from MedChemExpress. Usage Cited in: Life Sciences. 2023 Apr 1, 121652.; Palbociclib (1 µM; 48 h) decreases the expression of PPARγ in SVFs.

: Palbociclib dihydrochloride purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2019 May;43:225-237. [Abstract]; Representative images of immunohistochemical staining for proteins as indicated in A2780 xenografted tumors (n=6 per treatment group) treated with AZD2281 and Palbociclib either as single-agents or in combination for 4 days.

: Palbociclib dihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2018 Oct 9;9(1):4180. [Abstract]; MCF7, MCF7-LEM4, and MCF7-TAMR cells are treated with 5% DCC-FBS (vehicle), 4-OHT (1 μM), PD0332991 (PD) (0.2 μM), or a combination of 4-OHT and PD0332991. Immunoblots of lysates from cells are tested.

: Palbociclib dihydrochloride purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Sep 20;37(1):233. [Abstract]; Western blot of the nine cell cycle-related proteins in C666-1 cells treated with different concentrations of GEM (0.1, 1, and 10 μM) and PAL (0.1, 1, and 5 μM) after 48 h.

: Palbociclib dihydrochloride purchased from MedChemExpress. Usage Cited in: Eur J Cancer. 2018 Oct;102:10-22. [Abstract]; Head-to-head comparison of the effect of Palbociclib and Ribociclib on DNA damage response (DDR) signalling in liver cancer cells.

: Palbociclib dihydrochloride purchased from MedChemExpress. Usage Cited in: Nature. 2017 Jun 15;546(7658):426-430. [Abstract]; In vitro kinase reactions using immunoprecipitated endogenous CDK6 and recombinant PFKP or PKM2 with or without Palbociclib (PALBO). ³²P-PFKP and ³²P-PKM2 denote phosphorylated proteins, IB, immunoblotting.

: Palbociclib dihydrochloride purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049. [Abstract]; Effects of Palbociclib on CDK4/6-Rb pathway. HCC cells are treated with different doses of Palbociclib for 24 h, and then, the cells are subjected to western blot analysis.

: Palbociclib dihydrochloride purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049. [Abstract]; Effects of CDK4/6 inhibitors on AMPK phosphorylation and apoptosis-related signals. After 24 h of drug treatment, the cells are subjected to western blot analysis. AMPK phosphorylation level is quantified by the ratio of band intensities of phospho-AMPKα vs. AMPKα.

: Palbociclib dihydrochloride purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049. [Abstract]; Inhibition of AMPK reverses Palbociclib-induced autophagy and apoptosis. Hep3B cells are incubated with AMPK inhibitor (Compound C, 2.5 μM) for 4 h and then treated with Palbociclib for 24 h. Apoptotic cells are determined by flow cytometry.

: Palbociclib dihydrochloride purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta. 2017 Nov 20;1865(2):354-363. [Abstract]; LAPC-4 cells are grown in charcoal-stripped serum medium (CSS) for 24 hours and then stimulated by R1881 alone or with different doses of Palbociclib (PD). Palbociclib is added 30 min before androgen treatment. Cellular expression of all proteins is detected by immunoblotting analysis. β-actin is included as a control for protein loading.

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All CDK Isoform Specific Products:

View All Isoforms

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Cdk4/cyclin D3

9 nM (IC₅₀)

Cdk4/cyclin D1

11 nM (IC₅₀)

Cdk6/cyclin D2

16 nM (IC₅₀)

In Vitro

Palbociclib dihydrochloride (0-1 μM, 24 h) inhibits Rb Phosphorylation at Ser⁷⁹⁵ in MDA-MB-435 cells with an IC₅₀ value of 0.063 μM, and obtains similar effects on both Ser⁷⁸⁰ and Ser⁷⁹⁵ phosphorylation in the Colo-205 colon carcinoma^[1].
Palbociclib dihydrochloride (0-10 μM, 24 h) arrests MDA-MB-453 cells exclusively in G1 phase^[1].
Palbociclib dihydrochloride (500 nM, 7 days) increases expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells^[2].
Palbociclib dihydrochloride (0-1 μM, 6 days) inhibits growth of several luminal ER-positive as well as HER2-amplified breast cancer cell lines, with IC₅₀ values ranging from 4 nM to 1 μM^[3].
Palbociclib dihydrochloride (0-1 μM, 3 days) inhibits the proliferation of human liver cancer cell lines with IC₅₀ values ranging from 0.01 μM to 3.49 μM, and induces a reversible cell cycle arrest^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[1]

Cell Line:	MDA-MB-453 cells
Concentration:	0-1 μM
Incubation Time:	24 h
Result:	Arrested MDA-MB-453 cells in G1.

Cell Proliferation Assay^[3]

Cell Line:	ER-positive as well as HER2-amplified breast cancer cell lines (MDA-MB-175, ZR-75-30, CAMA-1, etc.)
Concentration:	0-10 μM
Incubation Time:	6 days
Result:	Inhibited growth of luminal ER-positive as well as HER2-amplified breast cancer cell lines.

In Vivo

Palbociclib dihydrochloride (oral adminstration, 75 or 150 mg/kg, daily for 14 days) produces rapid tumor regressions and delays tumor growth^[1].
Palbociclib dihydrochloride (oral adminstration, 90 mg/kg, daily for 12 days) reduces Treg numbers and the Treg:CD8 ratio in the spleen and lymph nodes in tumor-free mice, demonstrating the tumor-independent effects^[2].
Palbociclib dihydrochloride (oral administration, 100 mg/kg, daily for 1 week) has potent antitumour effects in genetically engineered mosaic mouse model of liver cancer^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mice bearing Colo-205 colon carcinoma xenografts (p16 deleted)^[1]
Dosage:	75, 150 mg/kg, daily for 14 days
Administration:	Oral adminstration
Result:	Produced rapid tumor regressions and a corresponding tumor growth delay of ~50 days.

Animal Model:	Tumor-free female FVB mice^[2]
Dosage:	90 mg/kg (diluted in 50 nM sodium D-lactate), daily for 12 days
Administration:	Oral adminstration
Result:	Reduced total thymic mass and immature CD4⁺ and CD8⁺ double-positive thymocytes, and increased the fractions of CD4⁺ and CD8⁺ single-positive thymocytes.

Animal Model:	Genetically engineered mosaic mouse model of liver cancer (Myc;p53-sgRNA)^[4]
Dosage:	100 mg/kg, daily for 1 week.
Administration:	Oral adminstration
Result:	Decreased the luminescence signal in liver and delayed tumour growth.

Clinical Trial

Molecular Weight

520.45

Formula

C₂₄H₃₁Cl₂N₇O₂

CAS No.

1831842-69-3

SMILES

[H]Cl.[H]Cl.O=C1C(C(C)=O)=C(C)C2=CN=C(NC3=NC=C(N4CCNCC4)C=C3)N=C2N1C5CCCC5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. [1] Fry DW, et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38. [Content Brief]

[2]. Goel S, et al. CDK4/6 inhibition triggers anti-tumour immunity. Nature. 2017 Aug 24;548(7668):471-475. [Content Brief]

[3]. Richard S Finn, et al. PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro. Breast Cancer Res. 2009;11(5):R77. [Content Brief]

[4]. Bollard J, et al. Palbociclib (PD-0332991), a selective CDK4/6 inhibitor, restricts tumour growth in preclinical models of hepatocellular carcinoma. Gut. 2017 Jul;66(7):1286-1296. [Content Brief]

Palbociclib dihydrochloride Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Palbociclib1831842-69-3PD-0332991PD0332991PD 0332991CDKCyclin dependent kinaseBreast cancerhepatocellular carcinomaHCCestrogen receptorERHER2cell cycleInhibitorinhibitorinhibit

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社
Product Name			Salutation
Applicant Name *			Email Address *
Phone Number *			Organization Name *
Department *			Requested quantity *
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks