MK-8776 (SCH 900776)

MK-8776 (SCH 900776)是一种选择性Chk1抑制剂,无细胞试验中IC50为3 nM,比作用于Chk2选择性高500倍。Phase 2。

MK-8776 (SCH 900776) Chemical Structure

MK-8776 (SCH 900776) Chemical Structure

CAS: 891494-63-6

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1921.21 现货
5mg RMB 1733.35 现货
10mg RMB 3015.42 现货
50mg RMB 7966.05 现货
500mg RMB 16134.3 现货
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客户使用Selleck的MK-8776 (SCH 900776)发表文献67

产品质控

批次: 纯度: 99.98%
99.94

MK-8776 (SCH 900776)相关产品

相关信号通路图

Chk抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
SKOV3 Growth Inhibition Assay 0.3 µM 8 d sensitizes the cell lines to gemcitabine  23548269
BxPC-3 Growth Inhibition Assay 10-1000 nM 24-48h enhances the chemosensitization to gemcitabine 23804422
MiaPaCa-2 Growth Inhibition Assay 10-1000 nM 24-48h enhances the chemosensitization to gemcitabine 23804422
AsPC-1 Growth Inhibition Assay 10-1000 nM 24-48h enhances the chemosensitization to gemcitabine 23804422
H1299 Growth Inhibition Assay 500 nM 24 h enhances the chemosensitization to PMX 24113549
H1993 Growth Inhibition Assay 500 nM 24 h enhances the chemosensitization to PMX 24113549
H1437 Growth Inhibition Assay 500 nM 24 h enhances the chemosensitization to PMX 24113549
H23 Growth Inhibition Assay 500 nM 24 h enhances the chemosensitization to PMX 24113549
AsPC-1 Growth Inhibition Assay 200/2000 nM 24 h decreases the IC50 of Gemcitabine 24359526
TK10 Growth Inhibition Assay 200/2000 nM 24 h decreases the IC50 of Gemcitabine 24359526
A498 Growth Inhibition Assay 200/2000 nM 24 h decreases the IC50 of Gemcitabine 24359526
U20S Growth Inhibition Assay 200/2000 nM 24 h decreases the IC50 of Gemcitabine 24359526
SNB19 Growth Inhibition Assay 200/2000 nM 24 h decreases the IC50 of Gemcitabine 24359526
MDA-MB-435 Growth Inhibition Assay 200/2000 nM 24 h decreases the IC50 of Gemcitabine 24359526
U87 Growth Inhibition Assay 200/2000 nM 24 h decreases the IC50 of Gemcitabine 24359526
HCC2998 Growth Inhibition Assay 200/2000 nM 24 h decreases the IC50 of Gemcitabine 24359526
MDA-MB-231 Growth Inhibition Assay 200/2000 nM 24 h decreases the IC50 of Gemcitabine 24359526
MiaPaCa-2 Growth Inhibition Assay 200/2000 nM 24 h decreases the IC50 of Gemcitabine 24359526
MCF10A Growth Inhibition Assay 200/2000 nM 24 h decreases the IC50 of Gemcitabine 24359526
HCT116 Growth Inhibition Assay 200/2000 nM 24 h decreases the IC50 of Gemcitabine 24359526
IGROV-1 Growth Inhibition Assay 200/2000 nM 24 h decreases the IC50 of Gemcitabine 24359526
SW620 Growth Inhibition Assay 200/2000 nM 24 h decreases the IC50 of Gemcitabine 24359526
HCT115 Growth Inhibition Assay 200/2000 nM 24 h decreases the IC50 of Gemcitabine 24359526
U251 Growth Inhibition Assay 200/2000 nM 24 h decreases the IC50 of Gemcitabine 24359526
OVCAR-8 Growth Inhibition Assay 0.3 µM 8 d sensitizes the cell lines to gemcitabine  23548269
MV-4-11 Apoptosis Assay 100-700 nM 48 h induces apoptosis dose dependently 23536721
U937 Apoptosis Assay 100-700 nM 48 h induces apoptosis dose dependently 23536721
MOLM-13  Apoptosis Assay 100-700 nM 48 h induces apoptosis dose dependently 23536721
A2058  Cell Viability Assay 37.5-300 nM 72 h reduces the MK-1775 EC50 by 5-fold to an average of 45 nM 23148684
H2009 Cell Viability Assay 500 nM 72 h results in G1/S-phase accumulation combined with MK-1775 23148684
Su.86.86 Cell Viability Assay 500 nM 72 h results in G1/S-phase accumulation combined with MK-1775 23148684
HRE Cell Viability Assay 500 nM 72 h results in G1/S-phase accumulation combined with MK-1775 23148684
HMEC Cell Viability Assay 500 nM 72 h results in G1/S-phase accumulation combined with MK-1775 23148684
U2OS  Function Assay 2 µM 0-24 h induces phosphorylation of Chk1 at serine 345 at both concentrations as early as 2 h after administration 22937147
U2OS  Growth Inhibition Assay 0-10 µM 24/48 h inhibits cell growth dose dependently 22937147
U937 Function Assay 100-500 nM 4 h  decreases the cytarabine-induced Chk1 autophosphorylation at Ser296 and prevents Cdc25A downregulation 22869869
U937 Function Assay 100 nM 4 h  reverses the cytarabine-induced inhibition of 3H-thymidine incorporation into DNA 22869869
U937 Function Assay 100-500 nM 4 h  induces increased phosphorylation of H2AX 22869869
HL-60 Apoptosis Assay 30/100/300 nM 24 h enhances cytarabine-induced apoptosis 22869869
ML-1 Apoptosis Assay 25/50/100 nM 24 h enhances cytarabine-induced apoptosis 22869869
HCT116 Function Assay 1 µM 24 h abrogates of cell cycle arrest  22510560
U2OS Function Assay 1 µM 24 h abrogates of cell cycle arrest  22510560
Sf9 Function assay Inhibition of recombinant CDK2/Cyclin A expressed in insect Sf9 cells assessed as inhibition of [33P]-ATP incorporation into biotinylated histone H1 after 1 hr by liquid scintillation counting, IC50 = 0.16 μM. 21094607
点击查看更多细胞系数据

生物活性

产品描述 MK-8776 (SCH 900776)是一种选择性Chk1抑制剂,无细胞试验中IC50为3 nM,比作用于Chk2选择性高500倍。Phase 2。
靶点
Chk1 [1]
(Cell-free assay)
CDK2 [1]
(Cell-free assay)
3 nM 0.16 μM
体外研究(In Vitro)
体外研究活性

SCH 900776是Chk2和CDK2的低效抑制剂,IC50分别为1.5 μM 和 0.16 μM。SCH 900776对细胞色素P450人肝微粒体亚型1A2,2C9,2C19,2D6,和3A4没有显著的抑制作用。羟基脲下暴露24小时后,SCH 900776诱导DNA复制能力剂量依赖性损失。SCH 900776增强γ-H2AX对羟基脲,5-氟尿嘧啶,和阿糖孢苷的响应。与抗代谢物结合,SCH 900776在2小时内诱导γ-H2AX的累积,表明复制叉瓦解,并且双链DNA断裂。此外,SCH 900776以剂量依赖的方式抑制Chk1 pS296自磷酸化的积累。增殖的WS1细胞暴露于SCH 900776,与Chk1 pS345快速的,剂量依赖性聚集相关,表明正常细胞的循环群诱导Chk1 pS345在暴露于SCH 900776后,是一部分无效循环,这也许通过AT-家族激酶和DNA-PK驱动。[1]

实验图片 检测方法 检测指标 实验图片 PMID
Western blot Cyclin E / pY15-CDK / γH2AX p-chk1(ser345) / CDC25A 26595527
体内研究(In Vivo)
体内研究活性

相对于gemcitabine或SCH 900776单独给药,Gemcitabine给药30分钟后,4 mg/kg SCH 900776足以诱导γ-H2AX生物标志物,而8 mg/kg增强肿瘤药效动力学和退化响应。递增剂量的SCH 900776 (16 mg/kg和32 mg/kg)诱导肿瘤响应持续改进。重要的是,在BALB/c 小鼠体内,SCH 900776的剂量与强的生物标志物活化相关,而提高的肿瘤响应与gemcitabine对血液学指标增强的毒性无关。[1]

动物实验 Animal Models 皮下注射A2780 或 MiaPaCa2细胞的额雌性裸鼠
Dosages ~50 mg/kg
Administration 腹腔内注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00779584 Completed
Hodgkin Disease|Lymphoma Non-Hodgkin|Neoplasms
Merck Sharp & Dohme LLC
October 17 2008 Phase 1

化学信息&溶解度

分子量 376.25 分子式

C15H18BrN7

CAS号 891494-63-6 SDF Download MK-8776 (SCH 900776) SDF
Smiles CN1C=C(C=N1)C2=C3N=C(C(=C(N3N=C2)N)Br)C4CCCNC4
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 75 mg/mL ( 199.33 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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常见问题及建议解决方法

问题 1:
I would like to know whether your product S2735 is the optically pure R enantiomer or whether it is a racemic mix.

回答:
Our S2735 MK-8776 (SCH 900776) is R enantiomer.

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