1. Cell Cycle/DNA Damage
  2. Checkpoint Kinase (Chk)

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

Cat. No.: HY-18174B
Handling Instructions

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a potent, selective, ATP competitive CHK1 and CHK2 inhibitor, with a Ki of 0.9 nM for CHK1 and IC50s of <1 nM, 8 nM for CHK1 and CHK2, respectively. Prexasertib Mesylate Hydrate inhibits HT-29 CHK1 autophosphorylation (S296) and HT-29 CHK2 autophosphorylation (S516). Prexasertib Mesylate Hydrate shows potent anti-tumor activity, significantly abrogates the G2/M checkpoint in p53 deficient HeLa cells with an EC50 of 9 nM.

For research use only. We do not sell to patients.

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 potent, selective, ATP competitive CHK1 and CHK2 inhibitor, with a Ki of 0.9 nM for CHK1 and IC50s of <1 nM, 8 nM for CHK1 and CHK2, respectively. Prexasertib Mesylate Hydrate inhibits HT-29 CHK1 autophosphorylation (S296) and HT-29 CHK2 autophosphorylation (S516). Prexasertib Mesylate Hydrate shows potent anti-tumor activity, significantly abrogates the G2/M checkpoint in p53 deficient HeLa cells with an EC50 of 9 nM[1].

IC50 & Target[1]

Chk1

0.9 nM (Ki)

Chk1

<1 nM (IC50)

Chk2

8 nM (IC50)

In Vitro

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is an ATP competitive CHK1 inhibitor, with a Ki of 0.9 nM and an IC50 of <1 nM[1].
Prexasertib (LY2606368) shows high anti-tumor activity against U-2 OS, Calu-6 and HeLa cells (IC50, 3, 3, 37 nM, respectively), causes DNA damage during S-phase requiring CDC25A and CDK2 at 4 μM[1].
Prexasertib (0-20 nM) synergizes with olaparib (0-20 μM) to decrease cell viability in HGSOC cells[2].

References
Animal Administration

Prexasertib (1, 3.3 or 10 mg/kg s.c.) is well tolerated, and significantly inhibits tumor inhibition in mice bearing Calu-6 xenograft tumors[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Prexasertib Mesylate Hydrate
Cat. No.:
HY-18174B
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Prexasertib Mesylate Hydrate

Cat. No.: HY-18174B