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Home >> Signaling Pathways >> Cell Cycle/Checkpoint >> Chk >> MK-8776 (SCH-900776)
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MK-8776 (SCH-900776)Chk1 inhibitor,potent and selective

MK-8776 (SCH-900776)

Catalog No. A8477
Size Price Stock Qty
10mM (in 1mL DMSO) $121.00 In stock
5mg $110.00 In stock
10mg $160.00 In stock
50mg $450.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

MK-8776(SCH-900776)

Biological Activity

Description SCH 900776 is a selective inhibitor of Chk1 with an IC50 value of 3 nM.
Targets Chk1 CDK2 Chk2      
IC50 3 nM 0.16 μM 1.5 μM      

Protocol

Cell experiment [1]:

Cell lines

U2OS cells

Preparation method

The solubility of this compound in DMSO is >18.8mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

2h

Applications

In U2OS cells, SCH 900776 induced a dose-dependent loss of DNA replication capability 24 hours after hydroxyurea exposure. SCH 900776 enhanced apoptosis for at least 48 hours following release from hydroxyurea blockade.

Animal experiment [1]:

Animal models

BALB/c mice bearing A2780 xenografts

Dosage form

4-32 mg/kg

Application

SCH-900776 (8 mg/kg) led to enhanced tumor pharmacodynamic and regression responses. SCH 900776 (16 and 32 mg/kg) induced incremental improvements in tumor response.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Guzi T J, Paruch K, Dwyer M P, et al. Targeting the replication checkpoint using SCH 900776, a potent and functionally selective CHK1 inhibitor identified via high content screening[J]. Molecular cancer therapeutics, 2011, 10(4): 591-602.

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Chemical Properties

Cas No. 891494-63-6 SDF Download SDF
Chemical Name (R)-6-bromo-3-(1-methyl-1H-pyrazol-4-yl)-5-(piperidin-3-yl)pyrazolo[1,5-a]pyrimidin-7-amine
Canonical SMILES BrC(C([C@@H]1CCCNC1)=N2)=C(N)N3C2=C(C4=CN(C)N=C4)C=N3
Formula C15H18BrN7 M.Wt 376.25
Solubility >18.8mg/mL in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

SCH 900776 is a potent and selective inhibitor of cell cycle checkpoint kinase 1 (Chk1), Chk2 and Cdk3 with IC50 value of 3 nM, 1.5µM and 0.16 µM, respectively.

Chk is s serine/threonine kinase that senses signal of DNA damage and stalls DNA replication, and also plays an essential role in the maintenance of replication fork viability during exposure to DNA antimetabolites.

In vitro, SCH 900776 blocked accumulation of the Chk1 pS296 autophosphorylation in a dose-dependent manner. Treatment of proliferating WS1 cells with SCH 900776 was found to be associated with rapid, dose-dependent accumulation of Chk1 pS345, indicating that cycling populations of normal cells induce Chk1 pS345 in response to the inhibition of SCH 900776 as part of a futile cycle 1.

In BALB/c mice, administration of SCH 900776 at a dosage of 8mg/kg after gemcitabine treatment can sufficiently induce enhanced tumor pharmacodynamic and regression responses as compared to gemcitabine or SCH 900776 alone 1.

Reference:
1.   Guzi TJ, Paruch K, Dwyer MP, et al. Targeting the replication checkpoint using SCH 900776, a potent and functionally selective CHK1 inhibitor identified via high
content screening. Molecular cancer therapeutics. 2011;10(4):591-602.