SCH900776
Based on 18 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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.89%
- No. CAS: 891494-63-6
- Fòrmula: C15H18BrN7
- Peso molecular:376.25
-
Almacenamiento: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]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
HY-10992
AZD-7762Chk Inhibitor -
HY-14720
RabusertibCHK1 Inhibitor -
HY-18174
PrexasertibCHK1 Inhibitor -
HY-18958
CCT245737CHK1 Inhibitor -
HY-10032
PF 477736Chk1 Inhibitor -
HY-10993
AdavosertibWee1 Inhibitor -
HY-13263
CHIR-124Checkpoint Kinase (Chk) Inhibitor -
HY-13946
BML-277 -
HY-112167
GDC-0575Chk1 Inhibitor -
HY-14715B
CCT241533 hydrochlorideCHK2 Inhibitor -
HY-18175
CCT244747 -
HY-19323
CeralasertibATR Inhibitor
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]
- EMBO Rep. 2026 Aug;27(16):4855-4878.
- 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
-
Cell Proliferation/Viability Assay
-
WB
-
IF
-
Flow Cytometry
-
Flow Cytometry
Actividad biológica
Descripciòn
IC50 & Target
[2]|
Chk1 3 nM (IC50) |
Chk2 1500 nM (IC50) |
CDK2 160 nM (IC50) |
In Vitro
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. Further protocols information, click here.
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
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 891494-63-6
-
Appearance Solid
-
Peso molecular 376.25
-
Fòrmula C15H18BrN7
-
SMILES
NC1=C(Br)C([C@H]2CNCCC2)=NC3=C(C4=CN(C)N=C4)C=NN13
-
Synonyms
MK-8776
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (18)
-
Journal Impact Factor
-
Most Recent
-
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
SCH900776 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2025 Aug;21(8):1182-1193. [Abstract]
SCH900776 (MK-8776; 0.1, 0.2, 0.4 μM) inhibited cell viability in MSANTD4-deficient U2OS cells.
-
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
SCH900776 purchased from MedChemExpress. Usage Cited in: Blood Cancer J. 2021 Jul 31;11(7):137. [Abstract]
SCH900776 (MK-8776; 1 μM; 24 h) increased the protein expression γH2AX, pRPA2 S33, PPA2 of CALR del61/WT.
SCH900776 purchased from MedChemExpress. Usage Cited in: Blood Cancer J. 2021 Jul 31;11(7):137. [Abstract]
SCH900776 (MK-8776; 1 μM; 6, 24 h) increased the γ-H2AX expression and increased γ-H2AX-positive cells in UT-7/Tpo CALR WT and CALR del61/WT cells.
SCH900776 purchased from MedChemExpress. Usage Cited in: Blood Cancer J. 2021 Jul 31;11(7):137. [Abstract]
SCH900776 (MK-8776; 1 μM; 24 h) induced cell cycle arrest at S-phase in the mutant cells, in the presence or absence of TPO, and nearly all the S-phase CALR-mutated cells were γ-H2AX positive CALR del61/WT cell lines.
SCH900776 purchased from MedChemExpress. Usage Cited in: Blood Cancer J. 2021 Jul 31;11(7):137. [Abstract]
SCH900776 (MK-8776; 1 μM; 72 h) showed that the mutant CALR del61/WT cells became blocked in S-phase and these cells were γ-H2AX positive.
-
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.
-
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 -
-
Solvente y solubilidad
In Vitro:
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.
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 (6.64 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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 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.
Pureza y Documentación
-
Ficha de datos (283 KB)
-
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)
-
Instrucciones de manejo (2659 KB)
Referencias
[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
HY-15532 Related Classifications
Powered by Bioz