1. Cell Cycle/DNA Damage
    Apoptosis
  2. Checkpoint Kinase (Chk)
    Apoptosis
  3. Prexasertib Mesylate Hydrate

Prexasertib Mesylate Hydrate (Synonyms: LY2606368 Mesylate Hydrate; LY2940930)

Cat. No.: HY-18174B
Handling Instructions

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) 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 Mesylate Hydrate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor activity.

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Prexasertib Mesylate Hydrate Chemical Structure

Prexasertib Mesylate Hydrate Chemical Structure

CAS No. : 1234015-57-6

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Description

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) 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 Mesylate Hydrate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor activity[1][2].

IC50 & Target[1]

Chk1

0.9 nM (Ki)

Chk1

<1 nM (IC50)

Chk2

8 nM (IC50)

In Vitro

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) inhibits MELK (IC50=38 nM), SIK (IC50=42 nM), BRSK2 (IC50=48 nM), ARK5 (IC50=64 nM). LY2606368 requires CDC25A and CDK2 to cause DNA damage[1].
Prexasertib Mesylate Hydrate (33, 100 nM; for 7 hours) results in DNA damage during S-phase in HeLa cells[1].
Prexasertib Mesylate Hydrate (8-250 nM; pre-treated for 15 minutes) inhibits CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) in HT-29 cells[1].
Prexasertib Mesylate Hydrate (4 nM; 24 hours) results in a large shift in cell-cycle populations from G1 and G2-M to S-phase with an accompanied induction of H2AX phosphorylation in U-2 OS cells[1].
Prexasertib Mesylate Hydrate (33 nM; for 12 hours) causes chromosomal fragmentation in HeLa cells. Prexasertib Mesylate Hydrate (100 nM; 0.5 to 9 hours) induces replication stress and depletes the pool of available RPA2 for binding to DNA[1].

Cell Cycle Analysis[1]

Cell Line: HeLa cells
Concentration: 33, 100 nM
Incubation Time: For 7 hours
Result: Had an IC50 of 37 nM and resulted in the G2-M population received DNA damage during S-phase but continued to progress through the cell cycle into an early mitosis.

Western Blot Analysis[1]

Cell Line: HT-29 cells
Concentration: 8, 16, 31, 63, 125, 250 nM
Incubation Time: Pre-treated for 15 minutes
Result: Inhibited CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) (IC50 of less than 31 nM) in HT-29 cells.
In Vivo

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate; 1-10 mg/kg; SC; twice daily for 3 days, rest 4 days; for three cycles; for 64 days) causes growth inhibition in tumor xenografts[1].
Prexasertib Mesylate Hydrate (15 mg/kg; SC) causes CHK1 inhibition in the blood and the phosphorylation of both H2AX (S139) and RPA2 (S4/S8)[1].

Animal Model: Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells[1]
Dosage: 1, 3.3, or 10 mg/kg
Administration: SC; twice daily for 3 days, rest 4 days; for three cycles (for 64 days)
Result: Caused statistically significant tumor growth inhibition (up to 72.3%).
Animal Model: Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells[1]
Dosage: 15 mg/kg (Pharmacokinetic Analysis)
Administration: SC (200 μL)
Result: CHK1 is 7 ng/mL at 12 hours and 3 ng/mL by 24 hours in plasma exposures.
Phosphorylation of both H2AX (S139) and RPA2 (S4/S8) was detectable at 4 hours, showing the rapid occurrence of DNA damage.
Clinical Trial
Molecular Weight

479.51

Formula

C₁₉H₂₅N₇O₆S

CAS No.

1234015-57-6

SMILES

N#CC1=NC=C(NC2=NNC(C3=C(OC)C=CC=C3OCCCN)=C2)N=C1.CS(=O)(O)=O.O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

Prexasertib MesylateLY2606368 MesylateLY2940930LY 2940930LY-2940930Checkpoint Kinase (Chk)ApoptosisATP-competitiveRSK1double-strandedDNAreplicationMELKSIKBRSK2ARK5CDC25ACDK2HeLaautophosphorylationS296S516H2AXHT-29Inhibitorinhibitorinhibit

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