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MK-8776 (SCH-900776)

Chk1 inhibitor,potent and selective CAS# 891494-63-6

MK-8776 (SCH-900776)

Catalog No. BCC3817----Order now to get a substantial discount!

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MK-8776 (SCH-900776): 5mg $127 In Stock
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Chemical structure

MK-8776 (SCH-900776)

3D structure

Chemical Properties of MK-8776 (SCH-900776)

Cas No. 891494-63-6 SDF Download SDF
PubChem ID 46239015 Appearance Powder
Formula C15H18BrN7 M.Wt 376.25
Type of Compound N/A Storage Desiccate at -20°C
Synonyms MK-8776
Solubility DMSO : ≥ 100 mg/mL (265.78 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 6-bromo-3-(1-methylpyrazol-4-yl)-5-[(3R)-piperidin-3-yl]pyrazolo[1,5-a]pyrimidin-7-amine
SMILES CN1C=C(C=N1)C2=C3N=C(C(=C(N3N=C2)N)Br)C4CCCNC4
Standard InChIKey GMIZZEXBPRLVIV-SECBINFHSA-N
Standard InChI InChI=1S/C15H18BrN7/c1-22-8-10(6-19-22)11-7-20-23-14(17)12(16)13(21-15(11)23)9-3-2-4-18-5-9/h6-9,18H,2-5,17H2,1H3/t9-/m1/s1
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.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of MK-8776 (SCH-900776)

DescriptionSCH 900776 is a selective inhibitor of Chk1 with an IC50 value of 3 nM.
TargetsChk1CDK2Chk2   
IC503 nM0.16 μM1.5 μM    

Protocol

Kinase Assay [2]
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.

Cell Assay [1]
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%.

Animal Administration [2]
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.

References:
[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. [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.

MK-8776 (SCH-900776) Dilution Calculator

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MK-8776 (SCH-900776) Molarity Calculator

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Preparing Stock Solutions of MK-8776 (SCH-900776)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.6578 mL 13.289 mL 26.5781 mL 53.1561 mL 66.4452 mL
5 mM 0.5316 mL 2.6578 mL 5.3156 mL 10.6312 mL 13.289 mL
10 mM 0.2658 mL 1.3289 mL 2.6578 mL 5.3156 mL 6.6445 mL
50 mM 0.0532 mL 0.2658 mL 0.5316 mL 1.0631 mL 1.3289 mL
100 mM 0.0266 mL 0.1329 mL 0.2658 mL 0.5316 mL 0.6645 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

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The Ohio State University

University of Zurich

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Yale University

Worcester Polytechnic Institute

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Universidade da Beira Interior

The Institute of Cancer Research

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University of Amsterdam

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The University of Michigan
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DRURY University
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Jilin University
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Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
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Deemed University
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Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on MK-8776 (SCH-900776)

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.

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Description

SCH900776 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.

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