SCH900776 (S-isomer)
作者：齐岳
发布时间：2023-09-13
16:57:27
点击数：
产品名称：SCH900776 (S-isomer)
产品描述：
| 产品描述 | SCH900776 (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). |
| 靶点活性 | Chk1:3 nM, Chk2:1500 nM, CDK2:160 nM |
| 体外活性 | 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. |
| 体内活性 | 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. |
| 别名 | MK-8776 S-isomer, SCH900776 S-isomer |
| 分子量 | 376.25 |
| 分子式 | C15H18BrN7 |
| CAS No. | 891494-64-7 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 100 mg/mL (265.78 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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