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SCH900776

Catalog No. T2517 CAS 891494-63-6

Synonyms: MK 8776, MK-8776

SCH900776 (MK-8776) is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities.

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SCH900776, CAS 891494-63-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 48.00
2 mg	In stock	$ 71.00
5 mg	In stock	$ 117.00
10 mg	In stock	$ 171.00
25 mg	In stock	$ 297.00
50 mg	In stock	$ 486.00
100 mg	In stock	$ 695.00
1 mL * 10 mM (in DMSO)	In stock	$ 126.00

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Purity: 99.6%

Purity: 99.45%

Purity: 98.35%

Purity: 98%

Purity: 96.69%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	SCH900776 (MK-8776) is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities.
Targets&IC50	Chk1:3 nM, CDK2:0.16 μM
In vitro	Administering 4 mg/kg of SCH 900776 30 minutes after gemcitabine triggers the γ-H2AX biomarker, while a dose of 8 mg/kg of SCH 900776 boosts tumor pharmacodynamics and degradation response. Incremental increases to 16 mg/kg and 32 mg/kg of SCH 900776 further improve tumor response. Notably, within BALB/c mice, the dose of SCH 900776 correlates with strong biomarker activation, independent of gemcitabine's intensified hematologic toxicity.
In vivo	After 24 hours of exposure to hydroxyurea, SCH 900776 induces a dose-dependent loss of DNA replication capacity. SCH 900776 enhances the response of γ-H2AX to hydroxyurea, 5-fluorouracil, and cytarabine. By combining with antimetabolites, SCH 900776 triggers the accumulation of γ-H2AX within 2 hours, indicating replication fork collapse and subsequent double-strand DNA breaks. Additionally, SCH 900776 inhibits the accumulation of Chk1 pS296 autophosphorylation in a dose-dependent manner. SCH 900776 is a weak inhibitor of Chk2 and CDK2, with IC50 values of 1.5 μM and 0.16 μM, respectively. SCH 900776 does not significantly inhibit human liver microsomal cytochrome P450 subtypes 1A2, 2C9, 2C19, 2D6, and 3A4.
Kinase Assay	The Millipore 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. Data are provided as percent activity remaining, relative to uninhibited controls.
Cell Research	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%.

Synonyms	MK 8776, MK-8776
Molecular Weight	376.25
Formula	C15H18BrN7
CAS No.	891494-63-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (265.78 mM)

References and Literature

1. Guzi TJ, et al. Mol Cancer Ther, 2011, 10(4), 591-602. 2. Montano R, et al. Mol Cancer Ther, 2012, 11(2), 427-438. 3. Schenk EL, et al. Clin Cancer Res, 2012, 18(19), 5364-5373. 4. Ou J, Li H, Qiu P, et al. CDK9 modulates circadian clock by attenuating REV-ERBα activity[J]. Biochemical and biophysical research communications. 2019 Jun 11;513(4):967-973.

Citations

1. Ou J, Li H, Qiu P, et al. CDK9 modulates circadian clock by attenuating REV-ERBα activity. Biochemical and Biophysical Research Communications. 2019 Jun 11;513(4):967-973

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Anti-Cancer Drug Library Highly Selective Inhibitor Library Anti-Cancer Clinical Compound Library Inhibitor Library Drug Repurposing Compound Library Cell Cycle Compound Library Bioactive Compounds Library Max Bioactive Compound Library NO PAINS Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

SCH900776 891494-63-6 Cell Cycle/Checkpoint Chk CDK SCH-900776 Inhibitor MK 8776 SCH 900776 Checkpoint Kinase (Chk) inhibit MK-8776 MK8776 inhibitor

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