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LY2835219 mesylate

Cat. No. M2112
LY2835219 mesylate Structure
Synonym:

Abemaciclib, CDK4/6 dual inhibitor

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 46.8  USD52 In stock
10mg USD 72  USD80 In stock
50mg USD 102.6  USD114 In stock
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Quality Control
Biological Activity

LY2835219 mesylate is a potent and selective CDK4/6 dual inhibitor with potential antineoplastic activity. CDK4/6 dual inhibitor LY2835219 has been shown in vitro to be a selective ATP-competitive inhibitor of CDK4/6 that inhibits phosphorylation of the Rb tumor suppressor protein and thereby induces G1 cell cycle arrest. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. LY2835219 is being investigated in a phase I clinical trial and in a clinical trial for the treatment of mantle cell lymphoma.

Product Citations
Customer Product Validations & Biological Datas
Source Cancer Cell (2018). Figure 5. abemaciclib (Abmole Bioscience, Houston, USA)
Method oral gavage
Cell Lines Mice
Concentrations 50 mg/kg
Incubation Time
Results Mice treated with IRN + VCR had stable disease (SD), whereas mice treated with either palbociclib + trametinib or abemaciclib + trametinib exhibited progressive disease.
Source Invest New Drugs (2014). Figure 2. LY2835219
Method flow cytometry
Cell Lines MCF10A cells
Concentrations 5 μM
Incubation Time 24-hour
Results LY2835219 induced a G1 arrest in Rb-proficient MDA-MB-231 breast cancer cells, whereas no such effect was seen in Rb-deficient MDA-MB-468 breast cancer cells at compound concentrations up to 2,500 nmol/L
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 602.7
Formula C27H32F2N8.CH4O3S
CAS Number 1231930-82-7
Purity >99%
Solubility Water 90 mg/mL
DMSO 50 mg/mL
Storage at -20°C
References

Abemaciclib: a CDK4/6 inhibitor for the treatment of HR+/HER2- advanced breast cancer
Silvia Paola Corona, et al. Drυg Des Devel Ther. 2018 Feb 16;12:321-330. PMID: 29497278.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LY2835219 mesylate, Abemaciclib, CDK4/6 dual inhibitor supplier, CDK, inhibitors

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