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Prexasertib

Cat. No. M13622
Prexasertib Structure
Synonym:

LY2606368

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

Prexasertib (LY2606368) 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 inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib 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 365.39
Formula
CAS Number 1234015-52-1
Purity >99%
Solubility DMSO 16.67 mg/mL
Storage at -20°C
References

[1] Jason Ostergaard, et al. Br J Haematol. Preclinical efficacy of prexasertib in acute lymphoblastic leukemia

[2] Chenguang Liu, et al. Nat Chem. Automated synthesis of prexasertib and derivatives enabled by continuous-flow solid-phase synthesis

[3] Giulio Evangelisti, et al. Expert Opin Investig Drugs. Prexasertib: an investigational checkpoint kinase inhibitor for the treatment of high-grade serous ovarian cancer

[4] Yoshihito Morimoto, et al. Oncol Rep. Prexasertib increases the sensitivity of pancreatic cancer cells to gemcitabine and S‑1

[5] Gesuino Angius, et al. Cancer Chemother Pharmacol. Prexasertib, a checkpoint kinase inhibitor: from preclinical data to clinical development

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GDC-0575 dihydrochloride

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CCT244747

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  Catalog
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Keywords: Prexasertib, LY2606368 supplier, Checkpoint, inhibitors

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