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Abemaciclib (LY2835219)

Cat. No. M10347
Abemaciclib (LY2835219) Structure
Synonym:

LY2835219 free base

Size Price Availability Quantity
5mg USD 51.3  USD57 In stock
10mg USD 76.5  USD85 In stock
50mg USD 99  USD110 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Abemaciclib (LY2835219) is a potent and selective inhibitor for CDK4 and CDK6 with IC50 values of 2 nM and 10 nM, respectively. 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. LY2835219 shows inhibition on A375R1-4, M14R, and SH4R with EC50 values ranging from 0.3 to 0.6 μM. Abemaciclib (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. 

In vivo, Abemaciclib (45 mg/kg, p.o.) in combination with RAD001 causes a cooperative antitumor effect in HNSCC xenograft tumor. Abemaciclib (45 or 90 mg/kg, p.o.) shows significant tumor growth inhibition in an A375 xenograft model.

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 506.59
Formula C27H32F2N8
CAS Number 1231929-97-7
Purity >99%
Solubility DMSO 5 mg/mL
Storage 2-8°C, protect from light, sealed
References

The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma
Bo Mi Ku, et al. Oncotarget. 2016 Mar 22;7(12):14803-13. PMID: 26909611.

The CDK4/6 inhibitor LY2835219 overcomes vemurafenib resistance resulting from MAPK reactivation and cyclin D1 upregulation
Vipin Yadav, et al. Mol Cancer Ther. 2014 Oct;13(10):2253-63. PMID: 25122067.

Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine
Lawrence M Gelbert, et al. Invest New Drugs. 2014 Oct;32(5):825-37. PMID: 24919854.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Abemaciclib (LY2835219), LY2835219 free base supplier, CDK, inhibitors

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