| Name | SCH900776 (S-isomer) |
| 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). |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 100 mg/mL (265.78 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (10.63 mM), Sonication is recommended.
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| Keywords | S-isomer | SCH900776 (S-isomer) | SCH-900776 (S-isomer) | SCH900776 (Sisomer) | SCH900776 (S isomer) | SCH-900776 | SCH900776 | SCH 900776 | Inhibitor | inhibit | Chk2 | Chk1 | CDK2 |
| Inhibitors Related | Ribociclib | (E)-β-Farnesene | Amantadine | 2-Chloropyrazine | Kojic acid | Abemaciclib | 2,4,6-Trihydroxybenzoic acid | Palbociclib | Abemaciclib methanesulfonate | Sodium Oxamate | Seliciclib | Dinaciclib |
| Related Compound Libraries | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Aging Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
