SCH900776
Based on 17 publication(s) in Google Scholar
SCH900776 (MK-8776) is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with an IC50 of 3 nM. SCH900776 shows 50- and 500-fold selectivity over CDK2 and Chk2, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.89%
- CAS. Nr.: 891494-63-6
- Formel: C15H18BrN7
- Molecular Weight:376.25
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) SCH900776
More- Nat Commun. 2025 Jun 2;16(1):5126. [Abstract]
- Nat Chem Biol. 2025 Aug;21(8):1182-1193. [Abstract]
- Sci Transl Med. 2021 Jan 20;13(577):eaba7401. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Sci Adv. 2022 Jan 21;8(3):eabj8357. [Abstract]
- Blood Cancer J. 2021 Jul 31;11(7):137. [Abstract]
- Cell Chem Biol. 2026 Jun 18;33(6):767-784.e7. [Abstract]
- Cell Rep. 2025 Jul 23;44(8):116019. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- Mol Cancer Ther. 2018 Dec;17(12):2676-2688. [Abstract]
- Hum Reprod. 2023 Sep 5;38(9):1769-1783. [Abstract]
- Cancer Biol Ther. 2022 Dec 31;23(1):69-82. [Abstract]
- Biomed Rep. 2025 Aug 26;23(5):169. [Abstract]
- J Radiat Res. 2023 May 25;64(3):520-529. [Abstract]
- Anticancer Drugs. 2024 Jan 1;35(1):46-54. [Abstract]
- bioRxiv. 2026 Apr 27.
- bioRxiv. 2025 February 22.
Customer Validation & Images
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WB
Biologische Aktivität
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Chk1 3 nM (IC50) |
Chk2 1500 nM (IC50) |
CDK2 160 nM (IC50) |
SCH900776 (300 nM) shows potent inhibitory activities against phosphorylation at ser296-Chk1. SCH900776 (1 μM) causes a 30-fold decrease in the IC50 for NSC-32065 in MDA-MB-231 cells[1]. The Kd value of SCH 900776 for the CHK1 kinase domain is 2 nM. SCH 900776 exhibits an approximate EC50 of 60 nM in cells exposure to NSC-32065. SCH 900776 induces dose-dependent suppression of CHK1 pS296 and concomitant accumulation of phospho-RPA signal in U2OS cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 891494-63-6
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Appearance Solid
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Molecular Weight 376.25
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Formel C15H18BrN7
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SMILES
NC1=C(Br)C([C@H]2CNCCC2)=NC3=C(C4=CN(C)N=C4)C=NN13
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Synonyms
MK-8776
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (17)
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Journal Impact Factor
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Most Recent
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Nat Commun
Selective targeting of genome amplifications and repeat elements by CRISPR-Cas9 nickases to promote cancer cell death. [Abstract]2025 Jun 2;16(1):5126. PMID: 40456709 -
Nat Chem Biol
2025 Aug;21(8):1182-1193. PMID: 39809895 -
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 -
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 -
Sci Adv
2022 Jan 21;8(3):eabj8357. PMID: 35061527 -
Blood Cancer J
High-throughput drug screening identifies the ATR-CHK1 pathway as a therapeutic vulnerability of CALR mutated hematopoietic cells. [Abstract]2021 Jul 31;11(7):137. PMID: 34333533 -
Cell Chem Biol
The cytotoxic effect of prexasertib is a consequence of dual inhibition on both CHK1 and AMPK. [Abstract]2026 Jun 18;33(6):767-784.e7. PMID: 42061410 -
Cell Rep
2025 Jul 23;44(8):116019. PMID: 40705605 -
Cell Syst
A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]2018 Apr 25;6(4):424-443.e7. PMID: 29655704 -
Mol Cancer Ther
mTORC1/2 and Protein Translation Regulate Levels of CHK1 and the Sensitivity to CHK1 Inhibitors in Ewing Sarcoma Cells. [Abstract]2018 Dec;17(12):2676-2688. PMID: 30282812
SCH900776 purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2018 Dec;17(12):2676-2688. [Abstract]
EW8 cells are treated with 50 nM LY 188011 in combination with increasing doses of Prexasertib, LY2603618, or MK-8776 for 6 hours. Cell lysates are then collected and blotted for p-CHK1- 296.
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Hum Reprod
Inhibition of checkpoint kinase prevents human oocyte apoptosis induced by chemotherapy and allows enhanced tumour chemotherapeutic efficacy. [Abstract]2023 Sep 5;38(9):1769-1783. PMID: 37451671 -
Cancer Biol Ther
Repeated treatments of Capan-1 cells with PARP1 and Chk1 inhibitors promote drug resistance, migration and invasion. [Abstract]2022 Dec 31;23(1):69-82. PMID: 35000525 -
Biomed Rep
Impact of the ATM/Chk2 pathway and cell cycle phase on radiation-induced senescence in A549 human lung cancer cells. [Abstract]2025 Aug 26;23(5):169. PMID: 40927689 -
J Radiat Res
DAP3-mediated cell cycle regulation and its association with radioresistance in human lung adenocarcinoma cell lines. [Abstract]2023 May 25;64(3):520-529. PMID: 37023702 -
Anticancer Drugs
2024 Jan 1;35(1):46-54. PMID: 37449977 -
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Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (265.78 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (6.64 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 (6.64 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.
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.
Protokoll
The Kinase Profiler service is used to generate general selectivity data for SCH 900776 against a broad range of serine/threonine and tyrosine kinases. Assays are typically run at two concentrations of SCH 900776 (0.5 and 5 μM), at a fixed (10 μM) concentration of ATP.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
For cell growth assays, cells are seeded at low density (500-1000 cells) in 96-well plates and then incubated with drug for 24 h (8 wells per concentration). Following treatment, cells are washed and grown in fresh media for 5-7 days at 37°C. Prior to attaining confluence, cells are washed, lysed, and stained with Hoechst 33258. Fluorescence is read on a microplate spectrofluorometer. Results are expressed as mean and standard error for the concentration of drug that inhibited growth by 50%.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
For tumor implantation, specific cell lines are grown in vitro, washed once with PBS and resuspended in 50% Matrigel in PBS to a final concentration of 4×107 to 5×107 cells per mL. Nude mice are injected with 0.1 mL of this suspension subcutaneously in the flank region. Tumor length (L), width (W), and height (H) are measured by a caliper twice a week on each mouse and then used to calculate tumor volume using the formula: (L×W×H)/2. Animals (N=10) are randomized to treatment groups and treated intraperitoneally with either SCH 900776 (formulated in 20% hydroxypropyl β-cyclodextrin) or individual chemotherapeutic agents, formulated as recommended. Tumor volumes and body weights are measured during and after the treatment periods. Data are recorded as means±SEM before being normalized to starting volume. Time to progression to 10x starting volume (TTP 10x) is monitored in some experiments. For pharmacodynamic marker analyses in mice, tumors and adjacent skin are collected at necropsy, fixed overnight in 10% formalin, and washed/stored in 70% ethanol. For skin punch biopsies, an area of approximately 4 square inches is shaved. Rats are anesthetized using inhaled isofluorane and dogs are locally anesthetized using subcutaneous administration of lidocaine. Samples are collected using a 4 mm biopsy punch. Skin punches are fixed in 10% formalin overnight before washing/storage in 70% ethanol.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (283 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Montano R, et al. Preclinical development of the novel Chk1 inhibitor SCH900776 in combination with DNA-damaging agents and antimetabolites. Mol Cancer Ther. 2012 Feb;11(2):427-38. [Content Brief]
[2]. Guzi TJ, et al. Targeting the replication checkpoint using SCH 900776, a potent and functionally selective CHK1 inhibitor identified via high content screening. Mol Cancer Ther. 2011 Apr;10(4):591-602. [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 | 2.6578 mL | 13.2890 mL | 26.5781 mL | 66.4452 mL |
| 5 mM | 0.5316 mL | 2.6578 mL | 5.3156 mL | 13.2890 mL | |
| 10 mM | 0.2658 mL | 1.3289 mL | 2.6578 mL | 6.6445 mL | |
| 15 mM | 0.1772 mL | 0.8859 mL | 1.7719 mL | 4.4297 mL | |
| 20 mM | 0.1329 mL | 0.6645 mL | 1.3289 mL | 3.3223 mL | |
| 25 mM | 0.1063 mL | 0.5316 mL | 1.0631 mL | 2.6578 mL | |
| 30 mM | 0.0886 mL | 0.4430 mL | 0.8859 mL | 2.2148 mL | |
| 40 mM | 0.0664 mL | 0.3322 mL | 0.6645 mL | 1.6611 mL | |
| 50 mM | 0.0532 mL | 0.2658 mL | 0.5316 mL | 1.3289 mL | |
| 60 mM | 0.0443 mL | 0.2215 mL | 0.4430 mL | 1.1074 mL | |
| 80 mM | 0.0332 mL | 0.1661 mL | 0.3322 mL | 0.8306 mL | |
| 100 mM | 0.0266 mL | 0.1329 mL | 0.2658 mL | 0.6645 mL |
SCH900776 Related Classifications
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