AZD-7762 hydrochloride
Based on 27 publication(s) in Google Scholar
AZD-7762 hydrochloride is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 98.03%
- CAS No.: 1246094-78-9
- Formule: C17H20ClFN4O2S
- Masse moléculaire:398.88
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) AZD-7762 hydrochloride
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]
- Biomed Pharmacother. 2026 Sep:202:119803.
- Research Square Preprint. 2024 Nov 06.
- Research Square Print. September 27th, 2022.
- Oncotarget. 2016 Aug 2;7(31):49800-49818. [Abstract]
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Activité biologique
Description
IC50 & Target
[1]|
Chk1 5 nM (IC50) |
Chk2 5 nM (IC50) |
In Vitro
AZD-7762 hydrochloride (AZD7762) is an equally potent inhibitor of Chk1 and Chk2 in vitro. AZD-7762 hydrochloride 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 hydrochloride 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 hydrochloride is determined to be 3.6 nM. Kinetic characterization suggests that AZD-7762 hydrochloride binds in the ATP-binding site of Chk1 and is thought to compete directly for ATP binding in a reversible manner. AZD-7762 hydrochloride 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. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1246094-78-9
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Appearance Solid
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Masse moléculaire 398.88
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Formule C17H20ClFN4O2S
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Color White to off-white
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SMILES
O=C(C1=C(NC(N)=O)C=C(C2=CC=CC(F)=C2)S1)N[C@@H]3CNCCC3.Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (27)
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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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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
Solvant et solubilité
In Vitro:
DMSO : 20 mg/mL (50.14 mM; ultrasonic and warming and heat to 60°C; 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 mg/mL (5.01 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 mg/mL (5.01 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
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Fiche technique (280 KB)
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SDS (614 KB)
- English - EN (614 KB)
- Français - FR (614 KB)
- Deutsch - DE (614 KB)
- Norwegian - NO (614 KB)
- Español - ES (614 KB)
- Swedish - SV (614 KB)
- Italian - IT (614 KB)
- Korean - KR (614 KB)
- Portuguese - PT (614 KB)
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Instruction de manipulation (2659 KB)
Références
[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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5070 mL | 12.5351 mL | 25.0702 mL | 62.6755 mL |
| 5 mM | 0.5014 mL | 2.5070 mL | 5.0140 mL | 12.5351 mL | |
| 10 mM | 0.2507 mL | 1.2535 mL | 2.5070 mL | 6.2675 mL | |
| 15 mM | 0.1671 mL | 0.8357 mL | 1.6713 mL | 4.1784 mL | |
| 20 mM | 0.1254 mL | 0.6268 mL | 1.2535 mL | 3.1338 mL | |
| 25 mM | 0.1003 mL | 0.5014 mL | 1.0028 mL | 2.5070 mL | |
| 30 mM | 0.0836 mL | 0.4178 mL | 0.8357 mL | 2.0892 mL | |
| 40 mM | 0.0627 mL | 0.3134 mL | 0.6268 mL | 1.5669 mL | |
| 50 mM | 0.0501 mL | 0.2507 mL | 0.5014 mL | 1.2535 mL |
AZD-7762 hydrochloride Related Classifications
HY-10992A Related Classifications
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