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

Prexasertib dihydrochloride (Synonyms: LY2606368 (dihydrochloride))

Cat. No.: HY-18174A Purity: 99.41%
Handling Instructions

Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a potent and selective ATP competitive inhibitor of the Chk1 protein kinase, with IC50s of <1 nM and 8 nM for CHK1 and CHK2, respectively, and a Ki of 0.9 nM against purified CHK1.

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

Prexasertib dihydrochloride Chemical Structure

Prexasertib dihydrochloride Chemical Structure

CAS No. : 1234015-54-3

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Based on 3 publication(s) in Google Scholar

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Description

Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a potent and selective ATP competitive inhibitor of the Chk1 protein kinase, with IC50s of <1 nM and 8 nM for CHK1 and CHK2, respectively, and a Ki of 0.9 nM against purified CHK1.

IC50 & Target[1]

Chk1

0.9 nM (Ki)

Chk1

<1 nM (IC50)

Chk2

8 nM (IC50)

In Vitro

Prexasertib (LY2606368) is a potent and selective ATP competitive inhibitor of Chk1, with an IC50 of <1 nM, and also inhibits CHK2, with an IC50 of 8 nM. Prexasertib has an EC50 of 1 nM for CHK1 activity through autophosphorylation of serine 296 and <31 nM for HT-29 CHK2 autophosphorylation (S516). Prexasertib potently abrogates the G2-M checkpoint activated by doxorubicin in p53-deficient HeLa cells with an EC50 of 9 nM. However, 100 nM Prexasertib does not inhibit PMA-stimulated RSK but instead weakly stimulates phosphorylation of S6 on serines 235/236. Prexasertib is broadly antiproliferative with IC50s of 3 nM, 3 nM, 10 nM, 37 nM, and 68 nM against U-2 OS, Calu-6, HT-29, HeLa, and NCI-H460 cell lines, respectively. Prexasertib (4 nM) 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 (LY2606368; 25 μM) exhibits inhibitory activities against proliferation of AGS and MKN1 cells. Prexasertib (20 nM) inhibits HR repair capacity DR-GFP cells. Prexasertib (5 nM) in combination with PARP inhibitor BMN673, displays synergistic anticancer effects in gastric cancer cells[2].

In Vivo

Prexasertib (LY2606368; 15 mg/kg, s.c.) significantly inhibits tumor growth in xenograft tumor models with less animal weight loss[1]. Prexasertib (LY2606368; 2 mg/kg, s.c.) and BMN673 combination has synergistic anticancer effect in gastric cancer PDX model, and the effect is higher than that of one drug alone[2].

Clinical Trial
Molecular Weight

438.31

Formula

C₁₈H₂₁Cl₂N₇O₂

CAS No.

1234015-54-3

SMILES

NCCCOC(C=CC=C1OC)=C1C2=CC(NC3=NC=C(C#N)N=C3)=NN2.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 31 mg/mL (70.73 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2815 mL 11.4075 mL 22.8149 mL
5 mM 0.4563 mL 2.2815 mL 4.5630 mL
10 mM 0.2281 mL 1.1407 mL 2.2815 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

Proliferation inhibition effect of Chk1 ablation, IR sensitivity, anticancer effect of BMN673 and Prexasertib are detected by MTS Cell Proliferation Colorimetric Assay Kit. Cells are seeded into 96 wells cell culture plate, then treated with indicated experiment conditions, then added 20 μL MTS reagent to each well subsequently, after incubated for 2 hours, cell viability of each well is detected on microplate reader at a wavelength of 490 nM[2].

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

Animal Administration
[1]

Female CD-1 nu-/nu- mice (26-28 g) are used for this study. Tumor growth is initiated by subcutaneous injection of 1×106 Calu-6 cells in a 1:1 mixture of serum-free growth medium and Matrigel in the rear flank of each subject animal. When tumor volumes reach approximately 150 mm3 in size, the animals are randomized by tumor size and body weight, and placed into their respective treatment groups. Vehicle consisting of 20% Captisol pH4 or Prexasertib is administered by subcutaneous injection in a volume of 200 μL. Four, eight, 12, 24, and 48 hours after drug administration, blood for plasma drug exposure is extracted via cardiac puncture and assayed on a Sciex API 4000 LC/MS-MS system. The xenograft tissue is promptly removed and prepared. Lysates are analyzed by immunoblot analysis for protein phosphorylation levels. Group means, SEs and P values are calculated using Kronos.

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

References

Purity: 99.41%

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Prexasertib dihydrochloride
Cat. No.:
HY-18174A
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