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SCH900776 S-isomer (MK-8776 S-isomer) is an effective, specific and orally bioavailable inhibitor of checkpoint kinase Chk1 (IC50: 3 nM). It also inhibitors Chk2 (IC50: 1500 nM) and cyclin-dependent kinase CDK2 (IC50: 160 nM).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $45 | In Stock | In Stock | |
| 2 mg | $64 | In Stock | In Stock | |
| 5 mg | $97 | In Stock | In Stock | |
| 10 mg | $157 | In Stock | In Stock | |
| 25 mg | $278 | - | In Stock | |
| 50 mg | $447 | Inquiry | Inquiry | |
| 100 mg | $659 | Inquiry | Inquiry | |
| 1 mL x 10 mM (in DMSO) | $116 | In Stock | In Stock |
| Description | SCH900776 S-isomer (MK-8776 S-isomer) is an effective, specific and orally bioavailable inhibitor of checkpoint kinase Chk1 (IC50: 3 nM). It also inhibitors Chk2 (IC50: 1500 nM) and cyclin-dependent kinase CDK2 (IC50: 160 nM). |
| Targets&IC50 | CDK2:160 nM, Chk2:1500 nM, Chk1:3 nM |
| In vitro | SCH 900776 does not significantly inhibit HLMs CYP450 isoforms 1A2, 2C9, 2C19, 2D6, and 3A4. SCH 900776 induces a dose-dependent loss of DNA replication capability 24 hours after hydroxyurea exposure. In combination with an antimetabolite, SCH 900776 induces accumulation of γ-H2AX within 2 hours, indicative of replication fork collapse and double-stranded DNA breaks. SCH 900776 also dose-dependently suppresses accumulation of the Chk1 pS296 autophosphorylation. |
| In vivo | After pretreatment 30 minutes with gemcitabine, SCH 900776 (4 mg/kg) is sufficient to induce the γ-H2AX biomarker while 8 mg/kg leads to enhanced tumor pharmacodynamic and regression responses relative to gemcitabine or SCH 900776 alone. SCH 900776 (16/32 mg/kg) dose-dependently induces improvements in tumor response. Doses of SCH 900776 associate with robust biomarker activation and improved tumor response are not associated with enhanced toxicity of gemcitabine on hematological parameters in BALB/c mice. |
| Synonyms | SCH900776 S-isomer, MK-8776 S-isomer |
| Molecular Weight | 376.25 |
| Formula | C15H18BrN7 |
| Cas No. | 891494-64-7 |
| Smiles | Cn1cc(cn1)-c1cnn2c(N)c(Br)c(nc12)[C@H]1CCCNC1 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (265.78 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (10.63 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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