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- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
MK-8776
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
891494-63-6
- 规格：
10 mM * 1 mL/5 mg/10 mg/25 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1045.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥950.0 |
| 规格： | 10 mg | 产品价格： | ￥1727.0 |
| 规格： | 25 mg | 产品价格： | ￥3800.0 |
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SCH900776
CAS No. : 891494-63-6
MCE 国际站：SCH900776
产品活性：SCH900776 (MK-8776) 是一种有效，选择性，可口服的 Chk1 抑制剂，IC50 值为 3 nM；它比对CDK2 和 Chk2 的选择性分别高 50 和 500 倍。
研究领域：Cell Cycle/DNA Damage
作用靶点：Checkpoint Kinase (Chk)
In Vitro: SCH900776 (300 nM) shows potent inhibitory activities against phosphorylation at ser296-Chk1. SCH900776 (1 μM) causes a 30-fold decrease in the IC50 for NSC-32065 in MDA-MB-231 cells. The Kd value of SCH 900776 for the CHK1 kinase domain is 2 nM. SCH 900776 exhibits an approximate EC50 of 60 nM in cells exposure to NSC-32065. SCH 900776 induces dose-dependent suppression of CHK1 pS296 and concomitant accumulation of phospho-RPA signal in U2OS cells.
In Vivo: SCH 900776 induces the γ-H2AX biomarker at 4 mg/kg (i.p.), and enhances tumor pharmacodynamic and regression responses in A2780 xenograft model. SCH 900776 (16 and 32 mg/kg, i.p.) induces incremental improvements in tumor response. Escalation of SCH 900776 dose to 20 and 50 mg/kg in combination with LY 188011 results in improvements in TTP 10× in the A2780 xenograft systems.
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文献和实验Signal Transduction Inhibitors in Cellular Function
CAAX peptide analogues BZA-5B, L-739, Cys-4-ABA-Met FT1-276, SCH44342, SCH66336 (57 –59) Bisubstrate inhibitors
References: Drews, J. Georgopolous, A., Laber, G., Schütze, E. and Unger, J. (1975) Antimicrobial activities of 81.723 hfu, a new pleuromutilin derivative. Antimicrobial Agents and Chemotherapy, 2, 5, pp 507-516 Kleven, S.H. (1990
(5' to 3') bp Reference 63F 16S CAG GCC TAA CAC ATG CAA GTC 1300 Marchesi et al. 1998 1387R
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