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

LY2606368 (Synonyms: Prexasertib)

Cat. No.: HY-18174 Purity: 97.91%
Handling Instructions

LY2606368 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.

LY2606368 Chemical Structure

LY2606368 Chemical Structure

CAS No. : 1234015-52-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 238 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 216 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 360 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
25 mg USD 780 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
50 mg USD 1320 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
100 mg USD 2280 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other Forms of LY2606368:

View All Checkpoint Kinase (Chk) Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

LY2606368 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

1 nM (IC50)

Chk2

8 nM (IC50)

In Vitro

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. LY2606368 has an EC50 of 1 nM for CHK1 activity through autophosphorylation of serine 296 and <31 nM for HT-29 CHK2 autophosphorylation (S516). LY2606368 potently abrogates the G2-M checkpoint activated by doxorubicin in p53-deficient HeLa cells with an EC50 of 9 nM. However, 100 nM LY2606368 does not inhibit PMA-stimulated RSK but instead weakly stimulates phosphorylation of S6 on serines 235/236. LY2606368 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. LY2606368 (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]. LY2606368 (25 μM) exhibits inhibitory activities against proliferation of AGS and MKN1 cells. LY2606368 (20 nM) inhibits HR repair capacity DR-GFP cells. LY2606368 (5 nM) in combination with PARP inhibitor BMN673, displays synergistic anticancer effects in gastric cancer cells[2].

In Vivo

LY2606368 (15 mg/kg, s.c.) significantly inhibits tumor growth in xenograft tumor models with less animal weight loss[1]. 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
Solvent & Solubility
In Vitro: 

DMSO : ≥ 60 mg/mL (164.21 mM)

*"≥" means soluble, but saturation unknown.

Preparing
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.
References
Cell Assay
[2]

Proliferation inhibition effect of Chk1 ablation, IR sensitivity, anticancer effect of BMN673 and LY2606368 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 LY2606368 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
Molecular Weight

365.39

Formula

C₁₈H₁₉N₇O₂

CAS No.

1234015-52-1

SMILES

NCCCOC(C=CC=C1OC)=C1C2=CC(NC3=NC=C(C#N)N=C3)=NN2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
LY2606368
Cat. No.:
HY-18174
Quantity:

LY2606368

Cat. No.: HY-18174