AZD-7762
Based on 26 publication(s) in Google Scholar
AZD-7762 is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.60%
- No. CAS: 860352-01-8
- Fòrmula: C17H19FN4O2S
- Peso molecular:362.42
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
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Publications Citing Use of MedChemExpress (MCE) AZD-7762
More- Cell. 2025 Jun 26;188(13):3405-3421.e27. [Abstract]
- Nat Nanotechnol. 2021 Jul;16(7):830-839. [Abstract]
- Cell Metab. 2022 Mar 1;34(3):424-440.e7. [Abstract]
- Nat Immunol. 2024 Apr;25(4):659-670. [Abstract]
- Nat Commun. 2023 Nov 22;14(1):7631. [Abstract]
- Exp Hematol Oncol. 2025 Jan 12;14(1):5. [Abstract]
- Sci Transl Med. 2021 Jan 20;13(577):eaba7401. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Arch Toxicol. 2023 Dec;97(12):3209-3226. [Abstract]
- Acta Pharmacol Sin. 2021 May;42(5):814-823. [Abstract]
- Cell Rep. 2023 Dec 11;42(12):113555. [Abstract]
- Cancer Cell Int. 2021 Jun 5;21(1):291. [Abstract]
- Mol Cancer Ther. 2026 Jul 15:10.1158/1535-7163.MCT-26-0182.
- Int Immunopharmacol. 2026 Feb 15:171:116126. [Abstract]
- Inflammation. 2021 Aug;44(4):1529-1539. [Abstract]
- Int J Cancer. 2025 Jan 15;156(2):417-430. [Abstract]
- Eur J Cell Biol. 2026 Apr 17;105(3):151540. [Abstract]
- Immunol Lett. 2021 May:233:42-47. [Abstract]
- FEBS Lett. 2019 Jul;593(14):1827-1836. [Abstract]
- PLoS One. 2019 Jan 10;14(1):e0209224. [Abstract]
- PLoS One. 2017 Jan 18;12(1):e0170308. [Abstract]
- Anticancer Drugs. 2024 Jan 1;35(1):46-54. [Abstract]
- Data Brief. 2021 May 21:37:107168. [Abstract]
- Research Square Preprint. 2024 Nov 06.
- Research Square Print. September 27th, 2022.
- Oncotarget. 2016 Aug 2;7(31):49800-49818. [Abstract]
Customer Validation & Images
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In Vivo Efficacy Study
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Histological Imaging/Staining
Actividad biológica
Descripciòn
IC50 & Target
[1]|
Chk1 5 nM (IC50) |
Chk2 5 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | GI50 |
0.236 μM
Compound: AZD7762
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Antiproliferative activity against human HEK293 cells after 72 hrs by MTS assay
Antiproliferative activity against human HEK293 cells after 72 hrs by MTS assay
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[PMID: 29684894] |
| HT-29 | EC50 |
0.01 μM
Compound: 4, AZD-7762
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Inhibition of CHK1 in human HT29 cells assessed as abrogation of camptothecin induced check point
Inhibition of CHK1 in human HT29 cells assessed as abrogation of camptothecin induced check point
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[PMID: 22551018] |
| HT-29 | EC50 |
0.28 μM
Compound: 4, AZD-7762
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Inhibition of CHK1 in human HT29 cells assessed as check point abrogation
Inhibition of CHK1 in human HT29 cells assessed as check point abrogation
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[PMID: 22551018] |
| HT-29 | EC50 |
0.62 μM
Compound: AZD7762
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Induction of cell cycle arrest in human HT-29 cells incubated for 20 hrs by phH3 staining based analysis
Induction of cell cycle arrest in human HT-29 cells incubated for 20 hrs by phH3 staining based analysis
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[PMID: 18790776] |
| HT-29 | EC50 |
10 nM
Compound: AZD7762
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Inhibition of camptothecin induced DNA damage in human HT-29 cells assessed as G2 checkpoint abrogation measured after 20 hrs presence of nocodazole by pHH3 staining based analysis
Inhibition of camptothecin induced DNA damage in human HT-29 cells assessed as G2 checkpoint abrogation measured after 20 hrs presence of nocodazole by pHH3 staining based analysis
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[PMID: 18790776] |
| HT-29 | GI50 |
0.167 μM
Compound: AZD7762
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Antiproliferative activity against human HT-29 cells after 72 hrs by MTS assay
Antiproliferative activity against human HT-29 cells after 72 hrs by MTS assay
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[PMID: 29684894] |
| MDA-MB-231 | GI50 |
0.15 μM
Compound: AZD7762
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Growth inhibition of human MDA-MB-231 cells expressing p53 mutant assessed as reduction in cell growth incubated for 48 hrs in presence of topotecan
Growth inhibition of human MDA-MB-231 cells expressing p53 mutant assessed as reduction in cell growth incubated for 48 hrs in presence of topotecan
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[PMID: 18790776] |
| SW-620 | GI50 |
1.08 nM
Compound: AZD7762
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Growth inhibition of human SW620 cells expressing p53 mutant assessed as reduction in cell growth incubated for 48 hrs in presence of gemcitabine
Growth inhibition of human SW620 cells expressing p53 mutant assessed as reduction in cell growth incubated for 48 hrs in presence of gemcitabine
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[PMID: 18790776] |
In Vitro
AZD-7762 (AZD7762) is an equally potent inhibitor of Chk1 and Chk2 in vitro. AZD-7762 potently inhibits Chk1 and Chk2, abrogates DNA damage-induced S and G2 checkpoints, enhances the efficacy of NSC 613327 and SKF 104864A, and modulates downstream checkpoint pathway proteins. AZD-7762 potently inhibits Chk1 phosphorylation of a cdc25C peptide with an IC50 of 5 nM as measured by a scintillation proximity assay. The Ki for AZD-7762 is determined to be 3.6 nM. Kinetic characterization suggests that AZD-7762 binds in the ATP-binding site of Chk1 and is thought to compete directly for ATP binding in a reversible manner. AZD-7762 is shown to abrogate the G2 arrest induced by Camptothecin with an average EC50 of 10 nM (n=12) and maximal abrogation in the range of 100 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 860352-01-8
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Appearance Solid
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Peso molecular 362.42
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Fòrmula C17H19FN4O2S
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Color White to yellow
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SMILES
O=C(N[C@@H]1CNCCC1)C2=C(C=C(S2)C3=CC=CC(F)=C3)NC(N)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (26)
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Journal Impact Factor
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Most Recent
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Cell
Extrachromosomal DNA replication and maintenance couple with DNA damage pathway in tumors. [Abstract]2025 Jun 26;188(13):3405-3421.e27. PMID: 40300601 -
Nat Nanotechnol
Therapeutically reprogrammed nutrient signalling enhances nanoparticulate albumin bound drug uptake and efficacy in KRAS-mutant cancer. [Abstract]2021 Jul;16(7):830-839. PMID: 33958764 -
Cell Metab
Imatinib and methazolamide ameliorate COVID-19-induced metabolic complications via elevating ACE2 enzymatic activity and inhibiting viral entry. [Abstract]2022 Mar 1;34(3):424-440.e7. PMID: 35150639 -
Nat Immunol
2024 Apr;25(4):659-670. PMID: 38499799
AZD-7762 purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2024 Apr;25(4):659-670. [Abstract]
AZD-7762 (25 mg/kg). Mean tumor growth curve of LLC tumor-bearing mice.
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Nat Commun
2023 Nov 22;14(1):7631. PMID: 37993427
AZD-7762 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Nov 22;14(1):7631. [Abstract]
Pan-γH2AX-positive cells in AMBRA1 knockdown, AMBRA1 WT and single mutant overexpression U2OS cells. Cells were treated with DMSO or 100 nM AZD7762 for 24 h, then harvested for immunofluorescence.
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Exp Hematol Oncol
Combinatorial functionomics identifies HDAC6-dependent molecular vulnerability of radioresistant head and neck cancer. [Abstract]2025 Jan 12;14(1):5. PMID: 39800760
AZD-7762 purchased from MedChemExpress. Usage Cited in: Exp Hematol Oncol. 2025 Jan 12;14(1):5. [Abstract]
Representative immunoblots of cleaved caspase 3 and its downstream target cleaved PARP upon treatment with Pano and/or AZD7762 (150 nM), for 48 h.
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Sci Transl Med
Small-molecule screen reveals synergy of cell cycle checkpoint kinase inhibitors with DNA-damaging chemotherapies in medulloblastoma. [Abstract]2021 Jan 20;13(577):eaba7401. PMID: 33472956
AZD-7762 purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2021 Jan 20;13(577):eaba7401. [Abstract]
Results of the interaction between four CHK inhibitors (AZD-7762) and the MB chemotherapy drug (4-HPC).
AZD-7762 purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2021 Jan 20;13(577):eaba7401. [Abstract]
AZD-7762 (30 mg/kg). Representative immunohistochemical (IHC) images of γH2AX or phosphorylated (p) CDC2 Tyr 15 in medulloblastoma (MB) tissues from Smo mice.
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Arch Toxicol
SIRT3-dependent mitochondrial redox homeostasis mitigates CHK1 inhibition combined with gemcitabine treatment induced cardiotoxicity in hiPSC-CMs and mice. [Abstract]2023 Dec;97(12):3209-3226. PMID: 37798514 -
Acta Pharmacol Sin
Activation of unfolded protein response overcomes Ibrutinib resistance in diffuse large B-cell lymphoma. [Abstract]2021 May;42(5):814-823. PMID: 32855532 -
Cell Rep
Cell stretching activates an ATM mechano-transduction pathway that remodels cytoskeleton and chromatin. [Abstract]2023 Dec 11;42(12):113555. PMID: 38088930 -
Cancer Cell Int
Construction of a prognostic model with histone modification-related genes and identification of potential drugs in pancreatic cancer. [Abstract]2021 Jun 5;21(1):291. PMID: 34090418 -
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Int Immunopharmacol
CHK1 inhibition by prexasertib sensitizes cisplatin-resistant malignant tumor cells via checkpoint abrogation and STAT1-driven PD-L1 upregulation. [Abstract]2026 Feb 15:171:116126. PMID: 41477994 -
Inflammation
2021 Aug;44(4):1529-1539. PMID: 33624224 -
Int J Cancer
Enhanced pharmacological activities of AKR1C3-activated prodrug AST-3424 in cancer cells with defective DNA repair. [Abstract]2025 Jan 15;156(2):417-430. PMID: 39243400 -
Eur J Cell Biol
MDC1 promotes nuclear localization of Beclin-1 and supports its role in ATM pathway in response to oxidative stress. [Abstract]2026 Apr 17;105(3):151540. PMID: 42013721 -
Immunol Lett
2021 May:233:42-47. PMID: 33741379 -
FEBS Lett
Fbxo6 confers drug-sensitization to cisplatin via inhibiting the activation of Chk1 in non-small cell lung cancer. [Abstract]2019 Jul;593(14):1827-1836. PMID: 31140586 -
PLoS One
2019 Jan 10;14(1):e0209224. PMID: 30629587 -
PLoS One
DNA Double-Strand Breaks Induce the Nuclear Actin Filaments Formation in Cumulus-Enclosed Oocytes but Not in Denuded Oocytes. [Abstract]2017 Jan 18;12(1):e0170308. PMID: 28099474
AZD-7762 purchased from MedChemExpress. Usage Cited in: PLoS One. 2017 Jan 18;12(1):e0170308. [Abstract]
Inhibition of nuclear actin filament formation by Chek1/2 inhibitor, AZD7762 (AZD). No nuclear actin filament formation is observed upon treatment of CEOs with AZD alone.
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Anticancer Drugs
2024 Jan 1;35(1):46-54. PMID: 37449977 -
Data Brief
2021 May 21:37:107168. PMID: 34113705 -
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Oncotarget
Inhibition of RNA polymerase I transcription initiation by CX-5461 activates non-canonical ATM/ATR signaling. [Abstract]2016 Aug 2;7(31):49800-49818. PMID: 27391441
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (275.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% HP-β-CD in Saline water
Solubility: 10 mg/mL (27.59 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
Cell Assay[1]
SW620 (5.5×103 per well) or MDA-MB-231 (5×103 per well) cells are seeded in 96-well plates and incubated overnight. Cells are dosed for 24 h with a 9-point titration of NSC 613327 ranging from 0.01 to 100 nM with or without a constant dose of AZD-7762 (300 nM). Control wells are dosed with vehicle alone (0.1% DMSO) or 300 nM AZD-7762. After 24 h, medium is removed and AZD-7762 alone is added back to the wells treated previously with AZD-7762 for an additional 24 h. Cells are then incubated in drug-free medium for an additional 72 h. The effect on cell proliferation is determined by MTS assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice and Rats[1]
Male NCr mice and male rnu rats are used. For xenograft models in mice, tumor cells are harvested, pelleted by centrifugation for 5 min, and resuspended in sterile PBS. Cells (3×103-6×106) are implanted s.c. into the right flank of the mice in a volume of 0.1 to 0.2 mL using a 25-gauge needle. Tumors are allowed to grow to the designated size of 100 to 200 mm3 before the administration of compound. For xenograft models in rats, Cells are harvested, pelleted by centrifugation for 5 min, and resuspended in 50% sterile PBS and 50% Matrigel. Rats receive a 5 Gy whole-body radiation dose 5 days before cell implantation to improve tumor growth. H460-DNp53 cells (1×107) are implanted s.c., into the right flank of the rats in a volume of 0.2 mL using a 25-gauge needle. Tumors are allowed to grow to the designated size of 100 to 200 mm3 before the administration of AZD-7762. AZD-7762 (10 and 20 mg/kg) is administered by i.v. injection via the tail vein. Cyclic schedules are used and treatment ranged from three to five cycles. Each cycle includes administration of a standard agent (NSC 613327 or CPT-11) every 3 days follow by delivery of AZD-7762. Tumor volumes are measured with electronic calipers and calculated.
Mice [2]
C57Bl/6 mice are intravenously injected with 2×105 Eμ-Myc B-lymphoma cells in PBS and treated with pharmacological inhibitors from 8 days post-injection. Treatment of mice is continued until an ethical end-point is reached; hunched posture, ruffled fur, enlarged lymph nodes, laboured breathing, weight loss greater than 20% of start body weight and limited mobility or paralysis. AZD7762 is delivered intraperitoneally in 10.3% -hydroxypropyl-β-cyclodextrin in 0.9% saline at 20 mg/kg daily on weekdays.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Zabludoff SD, et al. AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies. Mol Cancer Ther. 2008 Sep;7(9):2955-66. [Content Brief]
[2]. Quin J, et al. Inhibition of RNA polymerase I transcription initiation by CX-5461 activates non-canonical ATM/ATR signaling. Oncotarget. 2016 Aug 2;7(31):49800-49818. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7592 mL | 13.7961 mL | 27.5922 mL | 68.9804 mL |
| 5 mM | 0.5518 mL | 2.7592 mL | 5.5184 mL | 13.7961 mL | |
| 10 mM | 0.2759 mL | 1.3796 mL | 2.7592 mL | 6.8980 mL | |
| 15 mM | 0.1839 mL | 0.9197 mL | 1.8395 mL | 4.5987 mL | |
| 20 mM | 0.1380 mL | 0.6898 mL | 1.3796 mL | 3.4490 mL | |
| 25 mM | 0.1104 mL | 0.5518 mL | 1.1037 mL | 2.7592 mL | |
| 30 mM | 0.0920 mL | 0.4599 mL | 0.9197 mL | 2.2993 mL | |
| 40 mM | 0.0690 mL | 0.3449 mL | 0.6898 mL | 1.7245 mL | |
| 50 mM | 0.0552 mL | 0.2759 mL | 0.5518 mL | 1.3796 mL | |
| 60 mM | 0.0460 mL | 0.2299 mL | 0.4599 mL | 1.1497 mL | |
| 80 mM | 0.0345 mL | 0.1725 mL | 0.3449 mL | 0.8623 mL | |
| 100 mM | 0.0276 mL | 0.1380 mL | 0.2759 mL | 0.6898 mL |
AZD-7762 Related Classifications
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