MK-8776 (SCH-900776)Chk1 inhibitor,potent and selective CAS# 891494-63-6 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
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. |
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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. |
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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. |
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 |
MK-8776 (SCH-900776) Dilution Calculator
MK-8776 (SCH-900776) Molarity Calculator
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. |
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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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