Palbociclib isethionate (Synonyms: PD 0332991 isethionate)

Name: Palbociclib isethionate
Brand: MedChemExpress
SKU: HY-A0065
Rating: 5.0 (167 reviews)

Cat. No.: HY-A0065 Purity: 99.99%: FAQs
Data Sheet SDS COA Handling Instructions

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Palbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC₅₀ values of 11 and 16 nM, respectively. Palbociclib isethionate 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 isethionate Chemical Structure

CAS No. : 827022-33-3

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 76	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 76	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 84	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 108	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 156	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 192	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 396	In-stock	Estimated Time of Arrival: December 31
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Based on 167 publication(s) in Google Scholar

Other Forms of Palbociclib isethionate:

157 Publications Citing Use of MCE Palbociclib isethionate

IHC

: Palbociclib isethionate 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 isethionate 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 isethionate 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 isethionate 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 isethionate 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 isethionate 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 isethionate 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 isethionate 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 isethionate 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 isethionate 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]

Cdk4/cyclin D3

9 nM (IC₅₀)

Cdk4/cyclin D1

11 nM (IC₅₀)

Cdk6/cyclin D2

16 nM (IC₅₀)

DYRK1A

2000 nM (IC₅₀)

MAPK

8000 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 isethionate (oral adminstration, 75 or 150 mg/kg, daily for 14 days) produces rapid tumor regressions and delays tumor growth^[1].
Palbociclib isethionate (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 isethionate (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

573.66

Formula

C₂₆H₃₅N₇O₆S

CAS No.

827022-33-3

Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(C1=C(N2C3CCCC3)N=C(NC4=NC=C(N5CCNCC5)C=C4)N=C1)=C(C(C)=O)C2=O.OCCS(O)(=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

In Vitro:

H₂O : 50 mg/mL (87.16 mM; Need ultrasonic)

DMSO : 10 mg/mL (17.43 mM; Need ultrasonic; 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	1.7432 mL	8.7160 mL	17.4319 mL
5 mM	0.3486 mL	1.7432 mL	3.4864 mL
10 mM	0.1743 mL	0.8716 mL	1.7432 mL

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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* 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.

Molarity Calculator
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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (1.74 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.99%

Select Batch:

Data Sheet (286 KB) SDS (479 KB)

COA (257 KB) HNMR (266 KB) RP-HPLC (242 KB) LCMS (93 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	1.7432 mL	8.7160 mL	17.4319 mL	43.5798 mL
	5 mM	0.3486 mL	1.7432 mL	3.4864 mL	8.7160 mL
	10 mM	0.1743 mL	0.8716 mL	1.7432 mL	4.3580 mL
	15 mM	0.1162 mL	0.5811 mL	1.1621 mL	2.9053 mL
H₂O	20 mM	0.0872 mL	0.4358 mL	0.8716 mL	2.1790 mL
	25 mM	0.0697 mL	0.3486 mL	0.6973 mL	1.7432 mL
	30 mM	0.0581 mL	0.2905 mL	0.5811 mL	1.4527 mL
	40 mM	0.0436 mL	0.2179 mL	0.4358 mL	1.0895 mL
	50 mM	0.0349 mL	0.1743 mL	0.3486 mL	0.8716 mL
	60 mM	0.0291 mL	0.1453 mL	0.2905 mL	0.7263 mL
	80 mM	0.0218 mL	0.1089 mL	0.2179 mL	0.5447 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 isethionate 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:

Palbociclib827022-33-3PD 0332991PD0332991PD-0332991CDKCyclin dependent kinaseBreast cancerhepatocellular carcinomaHCCestrogen receptorERHER2cell cycleInhibitorinhibitorinhibit

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Palbociclib isethionate (Synonyms: PD 0332991 isethionate)

Customer Review

Other Forms of Palbociclib isethionate:

Palbociclib isethionate Related Antibodies

157 Publications Citing Use of MCE Palbociclib isethionate

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All CDK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Palbociclib isethionate Related Antibodies

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Complete Stock Solution Preparation Table

Palbociclib isethionate Related Classifications

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