All AbMole products are for research use only, cannot be used for human consumption.
AZD7762 is a potent ATP-competitive checkpoint kinase inhibitor with an IC50 of 5 and <10 nM for CHK1 and CHK2 respectively.AZD7762 has been profiled extensively in vitro andin vivo in combination with DNA-damaging agents and has been shown to potentiate response in several different settings where inhibition of checkpoint kinase results in the abrogation of DNA damage-induced cell cycle arrest.
Sci Rep. 2017 Nov 14;7(1):15511.
Targeting a non-oncogene addiction to the ATR/CHK1 axis for the treatment of small cell lung cancer
AZD7762 purchased from AbMole
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Source | Int J Gynecol Cancer (2014). Figure 3. AZD7762 |
| Method | analysis of cell cycle distribution | |
| Cell Lines | Ovarian clear cell carcinoma cells | |
| Concentrations | 50- or 150-nmol/L | |
| Incubation Time | 48 and 72 h | |
| Results | However, after treatment with cisplatin and AZD7762, the proportion of the cells in the G0/G1 and S phases decreased dramatically |
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Source | Int J Gynecol Cancer (2014). Figure 2. AZD7762 |
| Method | Immunofluorescence Studies | |
| Cell Lines | Ovarian clear cell carcinoma cells | |
| Concentrations | 50- or 150-nmol/L | |
| Incubation Time | 24 h | |
| Results | AZD7762 inhibited phosphorylation of Chk1 and Chk2 effectively and stabilized Cdc25A in response to cisplatin. |
| Cell Experiment | |
|---|---|
| Cell lines | H29 cells |
| Preparation method | Checkpoint Abrogation Assay HT29 cells (3 × 105) were seeded in 96-well plates and incubated overnight. Cells were treated for 2 h with camptothecin (topoisomerase I inhibitor; 0.07 μg/mL) to induce the G2 checkpoint. Cells were then treated for 20 h with vehicle (0.5% DMSO) or caffeine (4 mmol/L; positive control) plus nocodazole (1 μg/mL) or a 12-point titration of AZD7762 (12.5 μmol/L to 6 nmol/L) plus nocodazole. Nocodazole alone-treated cells with no camptothecin pretreatment were used to determine the maximum mitotic index. Cells were fixed with 3.7% formaldehyde for 1 h, permeabilized with PBS containing 0.05% Triton X, and incubated with anti-phH3 antibody for 1 h followed by Alexa Fluor 488 anti-rabbit (Molecular Probes) and Hoechst stain for 1 h. Mitotic index was determined on the ArrayScan and expressed as the percentage of cells undergoing mitosis. The EC50 was calculated by concentration-response curve fitting using three-variable logistical equations within XLfit (model 205) with the curve bottom constrained to 0 and the top constrained to 100 by nocodazole alone treatment. |
| Concentrations | 6nM~12.5μM |
| Incubation time | 20 h |
| Animal Experiment | |
|---|---|
| Animal models | athymic mice bearing established H460-DNp53 or SW620 tumors and rnu rats bearing established H460-DNp53 tumors |
| Formulation | formulated in 11.3% hydroxyproplyl-β-cyclodextrin |
| Dosages | 25mg/kg(mouse) and 10 or 20mg/kg (rat) |
| Administration | i.v. injection via the tail vein |
| Molecular Weight | 362.42 |
| Formula | C17H19FN4O2S |
| CAS Number | 860352-01-8 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Checkpoint Products |
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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
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| Rabusertib (LY2603618)
Rabusertib (LY2603618) is an effective and selective Chk1 inhibitor with an IC50 of 7 nM. |
| CHIR-124
CHIR-124 is a novel and potent Chk1 inhibitor with IC50 of 0.3 nM. |
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