Prexasertib HCl (LY2606368)

Catalog No.S7178

Prexasertib HCl (LY2606368) Chemical Structure

Molecular Weight(MW): 438.31

Prexasertib (LY2606368) is an ATP-competitive CHK1 inhibitor with a Ki value of 0.9 nmol/L. For CHK2 and RSK, its IC50 values are 8 nM and 9 nM respectively in cell-free assay.

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Biological Activity

Description Prexasertib (LY2606368) is an ATP-competitive CHK1 inhibitor with a Ki value of 0.9 nmol/L. For CHK2 and RSK, its IC50 values are 8 nM and 9 nM respectively in cell-free assay.
Targets
Chk1 [1]
(Cell-free assay)
Chk2 [1]
(Cell-free assay)
RSK [1]
(Cell-free assay)
0.9 nM(Ki) 8 nM 9 nM
In vitro

In nonclinical studies, LY2606368 induced DNA damage as measured by replication catastrophe and increases in pH2A.X, a marker of double-stranded DNA breaks[1]. Treatment of cells with LY2606368 results in the rapid appearance of TUNEL and pH2AX-positive double-stranded DNA breaks in the S-phase cell population. In a functional assay, LY2606368 potently abrogated the G2–M checkpoint activated by doxorubicin in p53-deficient HeLa cells with an EC50 of 9 nmol/L. LY2606368 was broadly antiproliferative with IC50 values typically <50 nmol/L in the most sensitive cell lines with a minority of cell lines showing considerable resistance with IC50's >1,000 nmol/L. LY2606368 requires CDC25A and CDK2 to cause DNA damage[2].

In vivo LY2606368 inhibited tumor growth in cancer xenografts as monotherapy and in combination with other agents[1]. In an orthotopic SKOV3 ovarian cancer model, LY2606368 was shown to inhibit the growth of primary tumors and significantly reduce the incidence of metastases and ascites accumulation. LY2606368 also demonstrated efficacy in an SW1990 orthotopic pancreatic cancer model resulting in a 92% inhibition of primary tumor growth and the elimination of metastases to the lymphnode, spleen, and intestine[3].

Protocol

Cell Research:

[2]

+ Expand
  • Cell lines: HeLa cells
  • Concentrations: 33 or 100 nmol/L
  • Incubation Time: 12 h
  • Method:

    HeLa cells were plated onto T25 flasks and allowed to recover for 24 hours. LY2606368 was then added to give final concentrations of 33 or 100 nmol/L. In some experiments, 20μmol/L Z-VAD-FMK was included during the drug treatment. Cells were treated for 12 hours, and during the last 2 hours, colchicine was added to 1 μg/mL. Fixation of nuclei for metaphase spreads was done following the method of Bayani and Squire. Chromosome spreads were done. A 12-μL volume of cell suspension in 3:1 methanol/acetic acid fixative was dropped from a height of 3 cm onto dry glass slides or coverslips. The slides were then heated for 45 seconds on a 43°C metal block, before being removed to allow drying to complete at room temperature. Coverslips were mounted on slides with Vectashield Hard Set mounting medium with DAPI. Slides were examined with a Leica DMR fluorescence microscope and images were captured using a SPOT RT3 Slider camera.


    (Only for Reference)
Animal Research:

[2]

+ Expand
  • Animal Models: Female CD-1 nu-/nu- mice
  • Formulation: 20% Captisol, pH4
  • Dosages: 15 mg/kg
  • Administration: s.c.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 2 mg/mL (4.56 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 438.31
Formula

C18H19N7O2.2HCl

CAS No. 1234015-54-3
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02649764 Active not recruiting Leukemia M.D. Anderson Cancer Center|Eli Lilly and Company May 4 2016 Phase 1
NCT03735446 Not yet recruiting Acute Myeloid Leukemia|Myelodysplastic Syndromes Dana-Farber Cancer Institute|Eli Lilly and Company November 30 2018 Phase 1
NCT02203513 Recruiting Ovarian Cancer|Breast Cancer|Prostate Cancer National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) July 29 2014 Phase 2
NCT02808650 Recruiting Childhood Solid Neoplasm|Recurrent Central Nervous System Neoplasm|Recurrent Malignant Solid Neoplasm|Refractory Central Nervous System Neoplasm|Refractory Malignant Solid Neoplasm Children''s Oncology Group|National Cancer Institute (NCI) February 27 2017 Phase 1
NCT02555644 Recruiting Head and Neck Neoplasms Eli Lilly and Company February 24 2016 Phase 1
NCT02778126 Active not recruiting Advanced Cancer Eli Lilly and Company September 22 2016 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    What is the solubility of LY2606368 in 20% Captisol?

  • Answer:

    S7178 in 20% Captisol is a suspension, which is fine for oral gavage. You can dissolve it in this vehicle to the concentration you need as long as the suspension is homogeneous.

Chk Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID