Prexasertib (Synonyms: LY2606368)

Name: Prexasertib
Brand: MedChemExpress
SKU: HY-18174
Rating: 5.0 (33 reviews)

Cat. No.: HY-18174 Purity: 99.64%: Data Sheet
COA

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Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a K_i of 0.9 nM and an IC₅₀ of <1 nM. Prexasertib inhibits CHK2 (IC₅₀=8 nM) and RSK1 (IC₅₀=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity.

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

CAS No. : 1234015-52-1

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 33 publication(s) in Google Scholar

Other Forms of Prexasertib:

33 Publications Citing Use of MCE Prexasertib

Cell Proliferation/Viability Assay

Flow Cytometry

In Vivo Efficacy Study

Apoptosis Analysis

RT-PCR

: Prexasertib purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2021 Jul;125(1):101-111. [Abstract]; Full length and cleaved PARP protein expressions are determined by western blot in Hepa1-6 cells and Huh-7 cells induced by prexasertib with dose of 1 µM and 5 nM for 24 h, respectively.

: Prexasertib purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2021 Jul;125(1):101-111. [Abstract]; Representative image of FACS analysis of late apoptotic Hepa1-6 cell rate treated by DMSO or prexasertib with dose of 1 µM for 24 h are shown.

: Prexasertib purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2021 Jul;125(1):101-111. [Abstract]; Tumour growth curves (Mean ± SEM) of murine HCC model treated by vehicle (n = 8) or prexasertib (10mg/kg, subcutaneous injection, 2 of 7 days, n = 8) are shown.

: Prexasertib purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2021 Jul;125(1):101-111. [Abstract]; Prexasertib (10mg/kg, subcutaneous injection, 2 of 7 days). Representative images of TUNEL assay for cellular apoptosis (green staining) in tumours are shown.

: Prexasertib purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2021 Jul;125(1):101-111. [Abstract]; Prexasertib (10mg/kg, subcutaneous injection, 2 of 7 days, n = 8). PD-L1 mRNA expression is determined by qPCR in tumours treated by prexasertib or vehicle.

: Prexasertib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Aug 2;10(1):3485. [Abstract]; Viability of mock control and Myc-activated CRISPRa cells upon treatment with 40 nM prexasertib for 96 h (n = 3).

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Chk1 Chk2 BUBR1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Chk1

0.9 nM (Ki)

Chk1

<1 nM (IC₅₀)

Chk2

8 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	40 nM Compound: Chemical probe: LY2606368	Cytotoxicity against human A2780 cells assessed as reduction in cell viability after 3 days by XTT assay Cytotoxicity against human A2780 cells assessed as reduction in cell viability after 3 days by XTT assay	[PMID: 28881656]
CHO	IC₅₀	20 μM Compound: 4; LY2606368	Inhibition of human ERG expressed in CHO cells at -80 mV holding potential by automated patch clamp assay Inhibition of human ERG expressed in CHO cells at -80 mV holding potential by automated patch clamp assay	[PMID: 30986571]
HEK293	IC₅₀	385.98 nM Compound: 4; LY2606368	Inhibition of recombinant human C-terminal His-tagged FLT3 (M1 to N541 residues) expressed in HEK293 cells using biotin-labelled STK substrate-1 as substrate incubated for 60 mins by HTRF assay Inhibition of recombinant human C-terminal His-tagged FLT3 (M1 to N541 residues) expressed in HEK293 cells using biotin-labelled STK substrate-1 as substrate incubated for 60 mins by HTRF assay	[PMID: 30986571]
JeKo-1	IC₅₀	0.004 μM Compound: 4; LY2606368	Inhibition of human JeKo1 cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay Inhibition of human JeKo1 cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay	[PMID: 30986571]
MV4-11	IC₅₀	0.004 μM Compound: 4; LY2606368	Inhibition of human MV411 cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay Inhibition of human MV411 cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay	[PMID: 30986571]
OVCAR-3	IC₅₀	12 nM Compound: Chemical probe: LY2606368	Cytotoxicity against human OVCAR-3 cells assessed as reduction in cell viability after 3 days by XTT assay Cytotoxicity against human OVCAR-3 cells assessed as reduction in cell viability after 3 days by XTT assay	[PMID: 28881656]
OVCAR-5	IC₅₀	3 nM Compound: Chemical probe: LY2606368	Cytotoxicity against human OVCAR-5 cells assessed as reduction in cell viability after 3 days by XTT assay Cytotoxicity against human OVCAR-5 cells assessed as reduction in cell viability after 3 days by XTT assay	[PMID: 28881656]
OVCAR-8	IC₅₀	10 nM Compound: Chemical probe: LY2606368	Cytotoxicity against human OVCAR-8 cells assessed as reduction in cell viability after 3 days by XTT assay Cytotoxicity against human OVCAR-8 cells assessed as reduction in cell viability after 3 days by XTT assay	[PMID: 28881656]
RPMI-8226	IC₅₀	0.048 μM Compound: 4; LY2606368	Inhibition of human RPMI8226 cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay Inhibition of human RPMI8226 cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay	[PMID: 30986571]
Ramos	IC₅₀	0.004 μM Compound: 4; LY2606368	Inhibition of human Ramos cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay Inhibition of human Ramos cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay	[PMID: 30986571]
SK-OV-3	IC₅₀	10 nM Compound: Chemical probe: LY2606368	Cytotoxicity against human SK-OV-3 cells assessed as reduction in cell viability after 3 days by XTT assay Cytotoxicity against human SK-OV-3 cells assessed as reduction in cell viability after 3 days by XTT assay	[PMID: 28881656]
Z-138	IC₅₀	0.033 μM Compound: 4; LY2606368	Inhibition of human Z138 cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay Inhibition of human Z138 cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay	[PMID: 30986571]

In Vitro

Prexasertib (LY2606368) 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 (33, 100 nM; for 7 hours) results in DNA damage during S-phase in HeLa cells^[1].
Prexasertib (8-250 nM; pre-treated for 15 minutes) inhibits CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) in HT-29 cells^[1].
Prexasertib (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 (33 nM; for 12 hours) causes chromosomal fragmentation in HeLa cells. Prexasertib (100 nM; 0.5 to 9 hours) induces replication stress and depletes the pool of available RPA2 for binding to DNA^[1].

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

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

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

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
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 was 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.

Molecular Weight

365.39

Formula

C₁₈H₁₉N₇O₂

CAS No.

1234015-52-1

Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 16.67 mg/mL (45.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.64%

Select Batch:

Data Sheet (284 KB) SDS (393 KB)

COA (256 KB) HNMR (266 KB) RP-HPLC (263 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. King C, et al. LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms. Mol Cancer Ther. 2015 Sep;14(9):2004-1 [Content Brief]

[2]. Yin Y, et al. Chk1 inhibition potentiates the therapeutic efficacy of PARP inhibitor BMN673 in gastric cancer. Am J Cancer Res. 2017 Mar 1;7(3):473-483. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.7368 mL	13.6840 mL	27.3680 mL	68.4200 mL
	5 mM	0.5474 mL	2.7368 mL	5.4736 mL	13.6840 mL
	10 mM	0.2737 mL	1.3684 mL	2.7368 mL	6.8420 mL
	15 mM	0.1825 mL	0.9123 mL	1.8245 mL	4.5613 mL
	20 mM	0.1368 mL	0.6842 mL	1.3684 mL	3.4210 mL
	25 mM	0.1095 mL	0.5474 mL	1.0947 mL	2.7368 mL
	30 mM	0.0912 mL	0.4561 mL	0.9123 mL	2.2807 mL
	40 mM	0.0684 mL	0.3421 mL	0.6842 mL	1.7105 mL

Prexasertib Related Classifications

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Prexasertib (Synonyms: LY2606368)

Customer Review

Other Forms of Prexasertib:

Prexasertib Related Antibodies

33 Publications Citing Use of MCE Prexasertib

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View All Checkpoint Kinase (Chk) Isoform Specific Products:

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References

Customer Review

Prexasertib Related Antibodies

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Complete Stock Solution Preparation Table

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