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Abemaciclib

Catalog No. T2381   CAS 1231929-97-7
Synonyms: CDK4/6 dual inhibitor, LY2835219

Abemaciclib (CDK4/6 dual inhibitor) is an effective and specific CDK4/6 inhibitor (IC50: 2/10 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Abemaciclib Chemical Structure
Abemaciclib, CAS 1231929-97-7
Pack Size Availability Price/USD Quantity
5 mg In stock $ 48.00
25 mg In stock $ 78.00
50 mg In stock $ 97.00
100 mg In stock $ 126.00
200 mg In stock $ 158.00
500 mg In stock $ 288.00
1 g In stock $ 427.00
1 mL * 10 mM (in DMSO) In stock $ 77.00
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Purity: 99.87%
Purity: 99.46%
Purity: 99.43%
Purity: 99.39%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Abemaciclib (CDK4/6 dual inhibitor) is an effective and specific CDK4/6 inhibitor (IC50: 2/10 nM).
Targets&IC50 CDK4:2 nM, CDK6:10 nM
In vitro LY2835219 reduces cell viability with the IC50 values ranging from 0.5 μM to 0.7 μM, inhibits Akt and ERK signaling but not mTOR activation at head and neck squamous cell carcinoma (HNSCC) cells[1]. LY2835219 shows inhibition on A375R1-4, M14R, and SH4R with EC50 values ranging from 0.3 to 0.6 μM; LY2835219 inhibits the proliferation of the parental A375 and resistant A375RV1 and A375RV2 cells with similar potencies with IC50 values of 395, 260, and 463 nM, respectively[2]. LY2835219 inhibits CDK4 and CDK6 with low nanomolar potency, inhibits Rb phosphorylation resulting in a G1 arrest and inhibition of proliferation, and its activity is specific for Rb-proficient cells[3].
In vivo LY2835219 (45 mg/kg, p.o.) in combination with everolimus causes a cooperative antitumor effect in HNSCC xenograft tumor[1]. LY2835219 (45 or 90 mg/kg, p.o.) shows significant tumor growth inhibition in an A375 xenograft model[2].
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)

TargetMolReferences and Literature

1. Ku B M , Yi S Y , Koh J , et al. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma[J]. Oncotarget, 2016, 7(12):14803-14813. 2. 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. 3. 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.

TargetMolCitations

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:
Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Pediatric Drug Library Kinase Inhibitor Library Drug-induced Liver Injury (DILI) Compound Library CNS-Penetrant Compound Library NO PAINS Compound Library Human Metabolite Library

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Keywords

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

 

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