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Prexasertib

Catalog No. T4310 CAS 1234015-52-1

Synonyms: LY2606368

Prexasertib (LY2606368) is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.

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Prexasertib, CAS 1234015-52-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 48.00
2 mg	In stock	$ 74.00
5 mg	In stock	$ 123.00
10 mg	In stock	$ 192.00
25 mg	In stock	$ 377.00
50 mg	In stock	$ 552.00
100 mg	In stock	$ 787.00
500 mg	In stock	$ 1,590.00

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Purity: 100%

Purity: 97.28%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Prexasertib (LY2606368) is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.
Targets&IC50	Chk1:<1 nM, Chk2:8 nM
In vitro	LY2606368 potently abrogates the G2-M checkpoint activated by doxorubicin in p53-deficient HeLa cells(EC50=9 nM). LY2606368 is a potent and selective ATP competitive inhibitor of Chk1(IC50 <1 nM), and also inhibits CHK2(IC50=8 nM).
In vivo	In xenograft tumor models, LY2606368 (15 mg/kg, s.c.) significantly inhibits tumor growth with less animal weight loss.
Cell Research	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 (25 μM) exhibits inhibitory activities against proliferation of AGS and MKN1 cells. LY2606368 (20 nM) inhibits HR repair capacity DR-GFP cells.
Animal Research	LY2606368 is formulated in vehicle consisting of 20% Captisol.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.

Synonyms	LY2606368
Molecular Weight	365.39
Formula	C18H19N7O2
CAS No.	1234015-52-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. King C, et al. LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms. Mol Cancer Ther. 2015 Sep;14(9):2004-13 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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Inhibitor Library Drug Repurposing Compound Library Anti-Viral Compound Library Kinase Inhibitor Library Bioactive Compound Library Apoptosis Compound Library Anti-Lung Cancer Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Prexasertib 1234015-52-1 Apoptosis Cell Cycle/Checkpoint Chk SIK Checkpoint Kinase (Chk) HT-29 S296 DNA double-stranded inhibit autophosphorylation LY-2606368 H2AX ATP-competitive HeLa MELK RSK1 CDK2 Inhibitor S516 ARK5 replication BRSK2 LY2606368 CDC25A LY 2606368 inhibitor

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