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Prexasertib

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Prexasertib is a small molecule inhibitor of the serine/threonine-protein kinase CHK1. It functions by inhibiting the activity of CHK1, which plays a critical role in the cell cycle and DNA damage response pathways.

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Lab products found in correlation

Dimethyl sulfoxide (dmso), by Merck Group (3 mentions) Ve 821, by MedChemExpress (2 mentions) Azd7762, by Selleck Chemicals (1 mentions) Mk 1775, by Selleck Chemicals (1 mentions) Prexasertib, by Eli Lilly (1 mentions) Pf 477736, by Selleck Chemicals (1 mentions) Ro 3306, by Selleck Chemicals (1 mentions) Birb 796, by Selleck Chemicals (1 mentions) Cisplatin, by Merck Group (1 mentions) Adavosertib, by Selleck Chemicals (1 mentions) Short tandem repeat multiplex assay, by Thermo Fisher Scientific (1 mentions) Olaparib, by MyBioSource (1 mentions) Fetal bovine serum (fbs), by Harvard Bioscience (1 mentions) Adavosertib, by MedChemExpress (1 mentions) Roswell park memorial institute (rpmi), by Merck Group (1 mentions) Rucaparib, by Selleck Chemicals (1 mentions) Olaparib, by Merck Group (1 mentions) Prexasertib, by Merck Group (1 mentions) Rucaparib, by Merck Group (1 mentions) Adh 1, by Merck Group (1 mentions)

9 protocols using prexasertib

1

Cell Culture Drug Solubilization Protocol

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For cell culture studies, drugs were dissolved in dimethyl sulfoxide (DMSO) to a final stock concentration of 10 mM except for prexasertib (4.5 mM). With the exception of prexasertib (MedChemExpress), all compounds were purchased from Selleckchem.
Dammert M.A., Brägelmann J., Olsen R.R., Böhm S., Monhasery N., Whitney C.P., Chalishazar M.D., Tumbrink H.L., Guthrie M.R., Klein S., Ireland A.S., Ryan J., Schmitt A., Marx A., Ozretić L., Castiglione R., Lorenz C., Jachimowicz R.D., Wolf E., Thomas R.K., Poirier J.T., Büttner R., Sen T., Byers L.A., Reinhardt H.C., Letai A., Oliver T.G, & Sos M.L. (2019). MYC paralog-dependent apoptotic priming orchestrates a spectrum of vulnerabilities in small cell lung cancer. Nature Communications, 10, 3485.
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2

Prexasertib and Cisplatin Resistance Study

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Cisplatin was purchased from Sigma (St. Louis, MO, USA). Prexasertib was provided by Eli Lilly or purchased from MedChemExpress (Monmouth Junction, NJ, USA). The Prexasertib provided by Eli Lilly was used to establish acquired‐resistant cell lines, evaluate the characteristics of the resistant cell lines, do the inhibition experiments by Wee1 inhibitor and detect the downstream proteins. All other experiments were performed with Prexasertib purchased from MedChemExpress. Several experiments were performed using both drugs with superimposable results. AZD7762, PF477736, RO3306, K3861, THZ1, BIRB796 and MK1775 were purchased from Selleckchem (Houston, TX, USA).
Zhao X., Kim I., Kallakury B., Chahine J.J., Iwama E., Pierobon M., Petricoin E., McCutcheon J.N., Zhang Y., Umemura S., Chen V., Wang C, & Giaccone G. (2021). Acquired small cell lung cancer resistance to Chk1 inhibitors involves Wee1 up‐regulation. Molecular Oncology, 15(4), 1130-1145.
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3

Combination Therapy for Acute Lymphoblastic Leukemia

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Prexasertib (PX) and VE-821 were purchased from Medchemexpress and were dissolved in dimethyl sulfoxide (DMSO, Sigma-Aldrich, St. Louis, MO, USA) as 10-mM stocks and stored at −20 °C. Dox was kindly provided by the Oncology Pharmacy Unit, IRCCS Istituto Romagnolo per lo Studio dei Tumori “Dino Amadori”, Meldola, Italy. Dox stock solution (2 mg/ml) was stored at 4 °C and diluted directly in culture medium. Dox effect in single agent was evaluated seeding ALL cell lines at 0.5 × 106 cell/ml and treating them with increasing drug concentrations (RPMI-8402 from 5 to 0.25 μM, dilution 1:2; SUP-B15 and REH from 1 to 0.05 μM, dilution 1:2). In the combination studies, ALL cell lines were seeded at 0.5 × 106 cells/ml and were treated with Dox (RPMI-8402: 0.1 μM; SUP-B15 and REH: 0.05 μM) for 48 h. After that, cells were reseeded at 0.5 × 106 cells/ml and treated with different doses of PX or VE-821 (or DMSO, as negative control), for additional 3 or 24 h depending on the experimental design.
Ghelli Luserna Di Rorà A., Ghetti M., Ledda L., Ferrari A., Bocconcelli M., Padella A., Napolitano R., Fontana M.C., Liverani C., Imbrogno E., Bochicchio M.T., Paganelli M., Robustelli V., Sanogo S., Cerchione C., Fumagalli M., Rondoni M., Imovilli A., Musuraca G., Martinelli G, & Simonetti G. (2021). Exploring the ATR-CHK1 pathway in the response of doxorubicin-induced DNA damages in acute lymphoblastic leukemia cells. Cell Biology and Toxicology, 39(3), 795-811.
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4

HNSCC Cell Line Culturing and Inhibitor Treatments

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All cell lines were grown in RPMI (Sigma-Aldrich, St. Louis, MO, USA) supplemented with 10% fetal bovine serum (FBS) (Biochrom AG, Berlin, Germany) at 37°C, 5% CO2 and 100% humidification. HPV-positive HNSCC cells UD-SCC-2, UM-SCC-47 and UPCI-SCC-154, UPCI-SCC-90, 93VU-147T, UT-SCC-45, and normal human fibroblasts F184 were described previously (21 (link), 33 (link), 39 (link)). Tumor cell lines were identified by a short tandem repeat multiplex assay (Applied Biosystems, Waltham, MD, USA). PARP inhibition was performed using 1 µM olaparib (MyBiosource, San Diego, CA, USA). Wee1 inhibition was performed using 240 nM adavosertib (Selleckchem, Houston, TX, USA) and combined Wee1/Chk1 inhibition was performed at a dose of 60 nM adavosertib and 1 nM prexasertib (MedChemExpress, Monmouth Junction, NJ, USA) unless stated otherwise. Supplementation with nucleosides (EmbryoMax 100×, Sigma-Aldrich, St. Louis, MO, USA) was performed at a final dilution of 1/12.5.
Hintelmann K., Berenz T., Kriegs M., Christiansen S., Gatzemeier F., Struve N., Petersen C., Betz C., Rothkamm K., Oetting A, & Rieckmann T. (2021). Dual Inhibition of PARP and the Intra-S/G2 Cell Cycle Checkpoints Results in Highly Effective Radiosensitization of HPV-Positive HNSCC Cells. Frontiers in Oncology, 11, 683688.
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5

Preparation and Storage of PARP Inhibitors

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Olaparib (#S1060) and rucaparib (#S1098) were purchased from Selleck Chemicals, Houston, TX. Hydroxyurea (HU; #H8627) was from Sigma-Aldrich. ADH-1 (N-cadherin inhibitor; #HY-13541) and prexasertib (CHK1 inhibitor; #HY-18174) were from MedChemExpress (Monmouth Junction, NJ). 100 mM of Olaparib, 10 mM of rucaparib, HU, ADH-1, and prexasertib were prepared as stocks in dimethyl sulfoxide (DMSO; #S-002-M, Sigma-Aldrich, Saint Louis, MO). All drugs were stored in aliquots at −80 °C until use.
Huang T.T., Burkett S.S., Tandon M., Yamamoto T.M., Gupta N., Bitler B.G., Lee J.M, & Nair J.R. (2022). Distinct roles of treatment schemes and BRCA2 on the restoration of homologous recombination DNA repair and PARP inhibitor resistance in ovarian cancer. Oncogene, 41(46), 5020-5031.
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6

Screening of Chemical Inhibitors for GFP-AZI2 Puncta

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GFP-AZI2 -4OHT cells were seeded in 24-well plates and left overnight before treatment with respective inhibitors. Upon treatment, images of cells were acquired every 2 h with an Incucyte live-cell imaging system (Essen Bioscience) to monitor GFP-AZI2 puncta formation. Inhibitor concentrations used in this screen were; SB203580, 10 µM (MedChemExpress, HY-10256); Tozasertib, 5 µM (MedChemExpress, HY-10161); Chloroquine, 100 µM (Sigma Aldrich, C6628); GDC0994, 5 µM (Cayman Chemical, 21107); Prexasertib, 5 µM (MedChemExpress, HY-18174); LTURM34, 10 µM (MedChemExpress, HY-101667); GSK650394, 5 uM (MedChemExpress, HY-15192); Amlexanox, 100 µM (MedChemExpress, HY-B0713); U0126, 10 µM (Cayman Chemical, 70970); IRAK 1–4 Inhibitor I, 10 µM (MedChemExpress, HY-13329); SP600125, 25 µM (MedChemExpress, HY-12041); SBI0206965, 10 µM (Cayman Chemical, 18477); BMS345541, 10 µM (MedChemExpress, HY-10519); Triciribine, 10 µM (MedChemExpress, HY-15457); Silmitasertib, 10 µM (MedChemExpress, HY-50855); PP242, 5 µM (MedChemExpress, HY-10474); Lys05, 20 µM (provided by Dr. Ravi Amaravadi); Palbociclib, 5 µM (MedChemExpress, HY-50767); and D4476, 50 µM (MedChemExpress, HY-10324). The puncta/image at 24 h were quantified and plotted.
Yeo S.K., Haas M., Manupati K., Hao M., Yang F., Chen S, & Guan J.L. (2023). AZI2 mediates TBK1 activation at unresolved selective autophagy cargo receptor complexes with implications for CD8 T-cell infiltration in breast cancer. Autophagy, 20(3), 525-540.
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7

High-throughput Screening of DNA Damage Response Inhibitors

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Cells were seeded in a 96-well plate at a density of 1,000 cells per well overnight. The next day, drugs including MK-1775, ceralasertib/AZD6738, CCT245737, AZD7762, prexasertib, CHIR-124 (all from MedChemExpress), Debio 0123, ZN-c3, VE-821, PD0166285, and VX-970 (all from Selleckchem) or DMSO was added. Cells were exposed to the drug for 10–15 days, and cell confluency or nuclei count was measured using an IncuCyte S3 (Sartorius).
Yang Y., Badura M.L., O’Leary P.C., Delavan H.M., Robinson T.M., Egusa E.A., Zhong X., Swinderman J.T., Li H., Zhang M., Kim M., Ashworth A., Feng F.Y., Chou J, & Yang L. (2024). Large tandem duplications in cancer result from transcription and DNA replication collisions. medRxiv.
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8

Combination Chemotherapeutic Regimen Evaluation

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4-HPC was purchased from Toronto Research Chemicals, and GEM from Medchem Express. For in vitro assays, drugs were dissolved in DMSO and stored at −80°C, with the exception of CDDP, which was purchased as a 1 mg/mL solution in saline (Hospira). For in vivo administration, CPM (Endoxan, Baxter) was dissolved in saline and 120 mg/kg delivered intraperitoneally (i.p.) once weekly. CDDP and GEM were diluted in phosphate-buffered saline (PBS) and 3 mg/kg (i.p.) or 60 mg/kg (i.v.), respectively, were delivered once weekly. CHK inhibitors were purchased from Medchem Express except for prexasertib (MedKoo Biosciences). AZD7762 was dissolved in 11% cyclodextrin (Sigma) and 30 mg/kg delivered i.v. (22 (link)), MK8776 was dissolved in 20% hydroxypropyl-β-cyclodextrin (Sigma) and 40 mg/kg delivered i.p., and LY2606368-hydrochloride and prexasertib were dissolved in 20% Captisol (Medchem Express) and 20 mg/kg delivered i.v. once per day, or 10 mg/kg delivered s.c. twice in one day 10–12 h apart. LY2603618 was formulated for daily oral dosing (p.o.) at 200 mg/kg in 16.7% Captisol in 25 mM phosphate buffer, pH 4 (59 (link)). Treatment schedules are shown in figures and were repeated weekly for 6 weeks unless tumor-related morbidity or other ill health was observed.
Endersby R., Whitehouse J., Pribnow A., Kuchibhotla M., Hii H., Carline B., Gande S., Stripay J., Ancliffe M., Howlett M., Schoep T., George C., Andradas C., Dyer P., Schluck M., Patterson B., Tacheva-Gigorova S.K., Cooper M.N., Robinson G., Stewart C., Pfister S.M., Kool M., Milde T., Gajjar A., Johns T., Wechsler-Reya R.J., Roussel M.F, & Gottardo N.G. (2021). Small molecule screen reveals synergy of cell cycle checkpoint kinase inhibitors with DNA-damaging chemotherapies in medulloblastoma. Science translational medicine, 13(577), eaba7401.
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9

Combination treatment of ALL cells

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Prexasertib (PX) and VE-821 were purchased from Medchemexpress and were dissolved in dimethyl sulfoxide (DMSO, Sigma-Aldrich, St. Louis, MO, USA) as 10 mM stocks and stored at -20°C. Dox was kindly provided by the Oncology Pharmacy Unit, IRCCS Istituto Romagnolo per lo Studio dei Tumori "Dino Amadori", Meldola, Italy. Dox stock solution (2 mg/ml) was stored at 4°C and diluted directly in culture medium. Dox effect in single agent was evaluated seeding ALL cell lines at 0.5x10 6 cell/ml and treating them with increasing drug concentrations (RPMI-8402 from 5 to 0.25 M dilution 1:2; SUP-B15 and REH from 1 to 0.05 M dilution 1:2). In the combination studies, ALL cell lines were seeded at 0.5x10 6 cells/ml and were treated with Dox (RPMI-8402: 0.1 M; SUP-B15 and REH: 0.05 M) for 48 hrs. After that, cells were reseeded at 0.5x10 6 cells/ml and treated with different doses of PX or VE-821 (or DMSO, as negative control), for additional 3 or 24 hrs depending on the experimental design.
Rorà A.G.L.d., Ghetti M., Ledda L., Ferrari A., Bocconcelli M., Padella A., Napolitano R., Fontana M.C., Liverani C., Imbrogno E., Bochicchio M.T., Paganelli M., Robustelli V., Sanogo S., Cerchione C., Fumagalli M., Rondoni M., Imovilli A., Musuraca G., Martinelli G., & Simonetti G. (2021). Exploring the ATR-CHK1 Pathway in the Response of Doxorubicin-induced DNA Damages in Acute Lymphoblastic Leukemia Cells.
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