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Abemaciclib metabolite M20

Cat. No. M13600
Abemaciclib metabolite M20 Structure
Synonym:

LSN3106726

Size Price Availability
5mg USD 350  USD350 Out of stock
10mg USD 550  USD550 Out of stock
25mg USD 990  USD990 Out of stock
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Quality Control & Documentation
Biological Activity

Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor for the treatment of cancer.

Chemical Information
Molecular Weight 522.59
CAS Number 2138499-06-4
Solubility (25°C) DMSO 5 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Ariana Soledad Poetto, et al. J Chromatogr B Analyt Technol Biomed Life Sci. "A new LC-MS/MS method for the simultaneous quantification of abemaciclib, its main active metabolites M2 and M20, and letrozole for therapeutic drug monitoring"

[2] Alejandra Martnez-Chvez, et al. Pharmacol Res. ABCB1 and ABCG2 limit brain penetration and, together with CYP3A4, total plasma exposure of abemaciclib and its active metabolites

[3] Alejandra Martnez-Chvez, et al. J Pharm Biomed Anal. Simultaneous quantification of abemaciclib and its active metabolites in human and mouse plasma by UHPLC-MS/MS

[4] Stefanie L Groenland, et al. Clin Pharmacokinet. Clinical Pharmacokinetics and Pharmacodynamics of the Cyclin-Dependent Kinase 4 and 6 Inhibitors Palbociclib, Ribociclib, and Abemaciclib

[5] P Kellie Turner, et al. Drug Metab Dispos. Abemaciclib Does Not Have a Clinically Meaningful Effect on Pharmacokinetics of CYP1A2, CYP2C9, CYP2D6, and CYP3A4 Substrates in Patients with Cancer

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  Catalog
Abmole Inhibitor Catalog




Keywords: Abemaciclib metabolite M20, LSN3106726 supplier, CDK, inhibitors, activators


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