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Prexasertib (LY2606368) is a substrate ATP competitively selective inhibitor of CHK1 and CHK2 with IC50 values of <1 nM and 8 nM against CHK1 and CHK2, respectively. LY2606368 treatment led to TUNEL and pH2AXy positive double-stranded DNA breaks in cells in S phase. LY2606368 effectively cancelled the G2-M checkpoint activated by Doxorubicin in P53-deficient HeLa cells with EC50 of 9 nM. LY2606368 can play an antiproliferative role in a wide range of cells, with IC50s < 50 nM in most sensitive cell lines. Only a few cell lines were resistant to LY2606368, IC50s > 1000 nM.
In vivo studies, LY2606368 can effectively inhibit tumor growth in tumor xenograft model and exert anti-tumor activity. In the SKOV3 ovarian cancer model, LY2606368 inhibited the growth of primary tumor and significantly reduced the rate of metastasis and ascites accumulation. In SW1990 model of pancreatic carcinoma in situ, LY2606368 inhibited the growth of 92% of the primary tumor and prevented its metastasis to lymph node tuberculosis, spleen and intestine.
| Cell Experiment | |
|---|---|
| Cell lines | HeLa cells |
| Preparation method | HeLa cells were plated onto T25 flasks and allowed to recover for 24 hours. LY2606368 was then added to give final concentrations of 33 or 100 nmol/L. In some experiments, 20μmol/L Z-VAD-FMK was included during the drug treatment. Cells were treated for 12 hours, and during the last 2 hours, colchicine was added to 1 μg/mL. Fixation of nuclei for metaphase spreads was done following the method of Bayani and Squire. Chromosome spreads were done. A 12-μL volume of cell suspension in 3:1 methanol/acetic acid fixative was dropped from a height of 3 cm onto dry glass slides or coverslips. The slides were then heated for 45 seconds on a 43°C metal block, before being removed to allow drying to complete at room temperature. Coverslips were mounted on slides with Vectashield Hard Set mounting medium with DAPI. Slides were examined with a Leica DMR fluorescence microscope and images were captured using a SPOT RT3 Slider camera. |
| Concentrations | 33 or 100 nmol/L |
| Incubation time | 12 h |
| Animal Experiment | |
|---|---|
| Animal models | Female CD-1 nu-/nu- mice |
| Formulation | 20% Captisol, pH4 |
| Dosages | 15 mg/kg |
| Administration | s.c. |
| Molecular Weight | 438.31 |
| Formula | C18H19N7O2.2HCl |
| CAS Number | 1234015-54-3 |
| Solubility (25°C) | DMSO 10 mg/mL (Need ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Checkpoint Products |
|---|
| AZD7762
AZD7762 is a potent ATP-competitive checkpoint kinase inhibitor with an IC50 of 5 and <10 nM for CHK1 and CHK2 respectively. |
| BIBR1532
BIBR1532 is a potent and selective telomerase inhibitor with IC50 of 100 nM. BIBR 1532 inhibits the proliferation of JVM13 leukemia cells with an IC50 of 52 μM, and similar effect also occurs in other leukemia cell lines such as Nalm-1, HL-60, and Jurkat. BIBR1532 is also an inhibitor of TERT, the rate-limiting enzyme in the regulation of telomerase activity. |
| PF-477736
PF-477736 is a selective checkpoint kinase 1 (Chk1) inhibitor with Ki values of 0.49 nM and 47 nM for CHK1 and CHK2 respectively. |
| SCH 900776
SCH 900776 (MK-8776) is a highly potent and functionally selective CHK1 inhibitor with IC50 of 3 nM. |
| Rabusertib (LY2603618)
Rabusertib (LY2603618) is an effective and selective Chk1 inhibitor with an IC50 of 7 nM. |
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