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

Prexasertib (Synonyms: LY2606368)

Cat. No.: HY-18174 Purity: 98.22%
Handling Instructions

Prexasertib (LY2606368) is a potent, selective and ATP-competitive checkpoint kinase 1 (Chk1) inhibitor, with an IC50 and a Ki of <1 nM and 0.9 nM, respectively.

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

Prexasertib Chemical Structure

Prexasertib Chemical Structure

CAS No. : 1234015-52-1

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 176 In-stock
Estimated Time of Arrival: December 31
5 mg USD 160 In-stock
Estimated Time of Arrival: December 31
10 mg USD 260 In-stock
Estimated Time of Arrival: December 31
25 mg USD 520 In-stock
Estimated Time of Arrival: December 31
50 mg USD 750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

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Prexasertib (LY2606368) is a potent, selective and ATP-competitive checkpoint kinase 1 (Chk1) inhibitor, with an IC50 and a Ki of <1 nM and 0.9 nM, respectively.

IC50 & Target[1]


0.9 nM (Ki)


<1 nM (IC50)


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 NSC 123127 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









Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (45.62 mM; Need ultrasonic)

Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7368 mL 13.6840 mL 27.3680 mL
5 mM 0.5474 mL 2.7368 mL 5.4736 mL
10 mM 0.2737 mL 1.3684 mL 2.7368 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.67 mg/mL (4.57 mM); Clear solution

*All of the co-solvents are provided by MCE.
Cell Assay

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

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. 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.

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PrexasertibLY2606368LY 2606368LY-2606368Checkpoint Kinase (Chk)Inhibitorinhibitorinhibit

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