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Prexasertib

Cat. No. M13622
Prexasertib Structure
Synonym:

LY2606368

Size Price Availability Quantity
5mg USD 127  USD127 In stock
25mg USD 395  USD395 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 365.39
Formula C18H19N7O2
CAS Number 1234015-52-1
Form Solid
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] 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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Keywords: Prexasertib, LY2606368 supplier, Checkpoint, inhibitors, activators


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