Palbociclib hydrochloride (Synonyms: PD-0332991 hydrochloride)

Name: Palbociclib hydrochloride
Brand: MedChemExpress
SKU: HY-50767C
Rating: 5.0 (130 reviews)

Cat. No.: HY-50767C Purity: 99.84%: FAQs
Data Sheet SDS COA Handling Instructions

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Palbociclib (PD 0332991) hydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC₅₀ values of 11 and 16 nM, respectively. Palbociclib hydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib hydrochloride 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 hydrochloride Chemical Structure

CAS No. : 571189-11-2

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5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 84	In-stock	Estimated Time of Arrival: December 31
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Based on 130 publication(s) in Google Scholar

Other Forms of Palbociclib hydrochloride:

120 Publications Citing Use of MCE Palbociclib hydrochloride

IHC

: Palbociclib hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

DYRK1A

2000 nM (IC₅₀)

MAPK

8000 nM (IC₅₀)

Cdk4/cyclin D3

9 nM (IC₅₀)

Cdk4/cyclin D1

11 nM (IC₅₀)

Cdk6/cyclin D2

16 nM (IC₅₀)

In Vitro

Palbociclib (0-1 μM, 24 h) hydrochloride inhibits retinoblastoma 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 (0-10 μM, 24 h) hydrochloride arrests MDA-MB-453 cells exclusively in G1 phase^[1].
Palbociclib (500 nM, 7 days) hydrochloride increases expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells^[2].
Palbociclib (0-1 μM, 6 days) hydrochloride 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 (0-1 μM, 3 days) hydrochloride 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 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:	0-1 μM
Incubation Time:	6 days
Result:	Inhibited growth of luminal ER-positive as well as HER2-amplified breast cancer cell lines.

Cell Cycle Analysissup>[1]

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

In Vivo

Palbociclib (oral adminstration, 75 or 150 mg/kg, daily for 14 days) hydrochloride produces rapid tumor regressions and delays tumor growth^[1].
Palbociclib (oral adminstration, 90 mg/kg, daily for 12 days) hydrochloride 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 (oral administration, 100 mg/kg, daily for 1 week) hydrochloride 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
Administration:	Oral administration; daily for 14 days
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
Administration:	Oral administration; daily for 12 days
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
Administration:	Oral administration; daily for 1 week
Result:	Decreased the luminescence signal in liver and delayed tumour growth.

Clinical Trial

Molecular Weight

514.99

Formula

C₂₄H₃₀ClN₇O₂

CAS No.

571189-11-2

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C(C(C)=O)=C(C2=CN=C(N=C2N1C3CCCC3)NC4=CC=C(N5CCNCC5)C=N4)C.Cl.[37/20]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 2 mg/mL (3.88 mM; ultrasonic and warming and heat to 60°C)

DMSO : 1.25 mg/mL (2.43 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9418 mL	9.7089 mL	19.4179 mL
5 mM	---	---	---
10 mM	---	---	---

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.84%

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Data Sheet (284 KB) SDS (252 KB)

COA (254 KB) HNMR (292 KB) LCMS (268 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O

1 mM

1.9418 mL

9.7089 mL

19.4179 mL

48.5446 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Palbociclib hydrochloride Related Classifications

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:

Palbociclib571189-11-2PD-0332991PD0332991PD 0332991CDKCyclin dependent kinaseBreast cancerhepatocellular carcinomaHCCestrogen receptorERHER2cell cycleInhibitorinhibitorinhibit

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Palbociclib hydrochloride (Synonyms: PD-0332991 hydrochloride)

Customer Review

Other Forms of Palbociclib hydrochloride:

Palbociclib hydrochloride Related Antibodies

120 Publications Citing Use of MCE Palbociclib hydrochloride

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All CDK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Palbociclib hydrochloride Related Antibodies

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Complete Stock Solution Preparation Table

Palbociclib hydrochloride Related Classifications

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