Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Prexasertib (LY2606368) is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: < 1 mg/mL (insoluble or slightly soluble)
You can also refer to dose conversion for different animals. More
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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