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SCH900776(S-isomer)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SCH900776(S-isomer)图片
CAS NO:891494-64-7
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
50 mg电议
100 mg电议

产品名称
SCH900776 S-isomer
MK-8776 S-isomer
产品介绍
SCH900776 S-isomer 是SCH900776的S型同分异构体。

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).

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.

Cas No.

891494-64-7

分子式

C15H18BrN7

分子量

376.262

别名

SCH900776 S-isomer;MK-8776 S-isomer

储存和溶解度

DMSO:100 mg/mL (265.78 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years