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Prexasertib dimesylate

Cat. No. M13623
Prexasertib dimesylate Structure
Synonym:

LY2606368 dimesylate

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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity.

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 557.6
Formula
CAS Number 1234015-58-7
Purity >99%
Solubility DMSO 90 mg/mL
Water 50 mg/mL
Storage 2-8°C, sealed
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  Catalog
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Keywords: Prexasertib dimesylate, LY2606368 dimesylate supplier, Checkpoint, inhibitors

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