SCH900776|891494-63-6|(MK-8776)-陌孚医药/Medlife

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SCH900776 (Synonyms: MK-8776)

目录号: PL13954 纯度: ≥99%

CAS No. :891494-63-6

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中文名称	SCH900776
中文别名	6-溴-3-(1-甲基-1H-吡唑-4-基)-5-(3R)-3-哌啶基吡唑并[1,5-A]嘧啶-7-胺;6-溴-3-(1-甲基-1H-吡唑-4-基)-5-(3R)-3-哌啶基吡唑并[1,5-a]嘧啶-7-胺
英文名称	SCH900776
英文别名	SCH900776;MK-8776 (SCH 900776);(R)-6-Bromo-3-(1-methyl-1H-pyrazol-4-yl)-5-(piperidin-3-yl)pyrazolo[1,5-a]pyrimidin-7-amine;6-BroMo-3-(1-Methyl-1H-pyrazol-4-yl)-5-(3R)-3-piperidinylpyrazolo[1,5-a]pyriMidin-7-aMine;MK-8776;SCH-900776;SCH900776(SCH-900776);MK-8776 (SCH-900776);6-bromo-3-(1-methyl-1H-pyrazol-4-yl)-5-(piperidin-3-yl)pyrazolo[1,5-a]pyrimidin-7-amine;GTPL7943;HMS3656J19;BCP02883;BDBM50334854;MK 8776;BCP0726000317;J3.517.083I;Q27086899;6-bromo-3-(1-methylpyrazol-4-yl)-5-[(3S)-piperidin-3-yl]pyrazolo[1,5-a]pyrimidin-7-amine;6-bromo-3-(1-methylpyrazol-4-;6-Bromo-3-(1-methyl-1H-pyrazol-4-yl)-5-(3R)-3-piperidinylpyrazolo[1,5-a]pyrimidin-7-amine (ACI);Sch 900776
Cas No.	891494-63-6
分子式	C₁₅H₁₈BrN₇
分子量	376.25
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

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。

生物活性

SCH900776 (MK-8776) is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with an IC 50 of 3 nM. SCH900776 shows 50- and 500-fold selectivity over CDK2 and Chk2, respectively.

性状

Solid

IC50 & Target[1][2]

Chk1 3 nM (IC50) Chk2 1500 nM (IC50

体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Montano R, et al. Preclinical development of the novel Chk1 inhibitor SCH900776 in combination with DNA-damaging agents and antimetabolites. Mol Cancer Ther. 2012 Feb;11(2):427-38.
[2]. Guzi TJ, et al. Targeting the replication checkpoint using SCH 900776, a potent and functionally selective CHK1 inhibitor identified via high content screening. Mol Cancer Ther. 2011 Apr;10(4):591-602.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (265.78 mM)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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