Home Tools

Abemaciclib

Catalog No. T2381 CAS 1231929-97-7

Synonyms: CDK4/6 dual inhibitor, LY2835219

Abemaciclib (LY2835219) is a dual inhibitor of CDK4/6 (IC50=2/10 nM) with selectivity and specificity. Abemaciclib has antitumor activity and is used to treat advanced or metastatic breast cancer.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Abemaciclib, CAS 1231929-97-7

Pack Size	Availability	Price/USD
5 mg	In stock	$ 48.00
10 mg	In stock	$ 59.00
25 mg	In stock	$ 78.00
50 mg	In stock	$ 97.00
100 mg	In stock	$ 123.00
200 mg	In stock	$ 156.00
500 mg	In stock	$ 288.00
1 mL * 10 mM (in DMSO)	In stock	$ 67.00

Bulk Inquiry

Select Batch

Purity: 99.87%

Purity: 99.46%

Purity: 99.43%

Purity: 99.39%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Abemaciclib (LY2835219) is a dual inhibitor of CDK4/6 (IC50=2/10 nM) with selectivity and specificity. Abemaciclib has antitumor activity and is used to treat advanced or metastatic breast cancer.
Targets&IC50	CDK4:2 nM, CDK6:10 nM
In vitro	METHODS: HNSCC cell lines OSC-19, FaDu and YD-10B were treated with Abemaciclib (0.01-10 μM) for 72 h, and cell viability was measured by Cell Counting Kit. RESULTS: Abemaciclib treatment decreased the cell viability of HNSCC cells with IC50 values ranging from 0.5 μM to 0.7 μM. [1] METHODS: AML cells MV4-11 were treated with Abemaciclib (0.04-5 μM) for 24 h. The cell cycle was detected using Flow Cytometry. RESULTS: Abemaciclib induced G1 phase block in MV4-11 cells. The G1-phase block was maximized when the concentration was ≥320 nmol/L. The RESULTS showed that Abemaciclib induced G1-phase block in MV4-11 cells. [2]
In vivo	METHODS: To assay antitumor activity in vivo, Abemaciclib (45-90 mg/kg in 1% HEC in 20 mM phosphate buffer (pH 2.0)) was administered by gavage to BALB/c mice bearing human tongue squamous carcinoma tumors OSC-19 once daily for fourteen days. RESULTS: Abemaciclib significantly reduced tumor growth in OSC-19 xenografts during treatment. abemaciclib treatment decreased AKT phosphorylation but had no effect on mTOR activation. [1] METHODS: To assay antitumor activity in vivo, Abemaciclib (22.5-90 mg/kg in 1% HEC in 25 mmol/L PB pH2) was administered by gavage to athymic nude mice harboring melanoma A375 once a day for twenty-one days. RESULTS: Statistically significant tumor growth inhibition was observed with Abemaciclib at 45 or 90 mg/kg dosing regimens. abemaciclib treatment significantly reduced pS780-Rb and pS10-Histone H3 levels, suggesting that CDK4/6 inhibition resulted in cell cycle inhibition and reduced tumor cell proliferation. [3]
Kinase Assay	Cells (5×103) are plated in 96 well plates. Cells are treated the next day for 24 to 48 hours and then assessed for caspase-3 activity by Caspase-Glo-3/7 Assay, as per manufacturer's instructions and a luminescence plate reader.
Cell Research	LY2835219 is dissolved in DMSO to a 10 mM concentration.? Cells are seeded in a 96-well plate, allowed to adhere overnight, and treated with DMSO control (0.1% v/v) or the indicated compounds for 72 h. Cell viability and proliferation are determined using a Cell Counting Kit according to the manufacturer's instructions. The interaction between LY2835219 and mTOR inhibitor is determined using CompuSyn. Combination index (CI) values of 1 indicates and additive drug interaction, whereas a CI of <1 is synergistic and a CI of >1 is antagonistic.

Synonyms	CDK4/6 dual inhibitor, LY2835219
Molecular Weight	506.59
Formula	C27H32F2N8
CAS No.	1231929-97-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10mg/mL(19.74mM)

Ethanol: 5.06mg/mL (10mM)

References and Literature

1. Ku BM, et al. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma. Oncotarget. 2016 Mar 22;7(12):14803-13. 2. Gelbert LM, et al. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine. Invest New Drugs. 2014 Oct;32(5):825-37. 3. Yadav V, et al. The CDK4/6 inhibitor LY2835219 overcomes vemurafenib resistance resulting from MAPK reactivation and cyclin D1 upregulation. Mol Cancer Ther. 2014 Oct;13(10):2253-63.

Citations

1. Ni J, Kabraji S, Xie S, et al. p16INK4A-deficiency predicts response to combined HER2 and CDK4/6 inhibition in HER2+ breast cancer brain metastases. Nature Communications. 2022, 13(1): 1-8. 2. Liu X, Hu Q, Wang W, et al. A protein-fragment complementation assay reveals that celastrol and gambogic acid suppress ERα mutants in breast cancer. Biochemical Pharmacology. 2021, 188: 114583. 3. Jiang L, Yu Y, Li Z, et al.BMS-265246, a Cyclin-Dependent Kinase Inhibitor, Inhibits the Infection of Herpes Simplex Virus Type 1.Viruses.2023, 15(8): 1642. 4. Quan C, Wu Z, Xiong J, et al.Upregulated PARP1 confers breast cancer resistance to CDK4/6 inhibitors via YB-1 phosphorylation.Experimental Hematology & Oncology.2023, 12(1): 1-21.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library EMA Approved Drug Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Aging Compound Library Targeted Therapy Drug Library Anti-COVID-19 Compound Library

Related Products

Related compounds with same targets

(R)-CR8 trihydrochloride TBB CDK4/6/1 Inhibitor Ribociclib succinate CDK4/6-IN-3 Ganoderic acid H CP-10 CDK9-IN-27

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Abemaciclib 1231929-97-7 Cell Cycle/Checkpoint CDK inhibit CDK4/6 dual inhibitor LY 2835219 LY2835219 Inhibitor LY-2835219 Cyclin dependent kinase inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.