Chk2 Inhibitor Ⅱ
货号：
IC3180
品牌：
Jinpan
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产品简介
| MDL | MFCD08276917 |
| 别名 | BML-277 |
| CAS | 516480-79-8 |
| 分子式 | C20H14ClN3O2 |
| 分子量 | 363.8 |
| 储存条件 | -20℃ |
| 纯度 | ≥98% |
| 单位 | 瓶 |
| 生物活性 | 是一种Chk2的ATP竞争性抑制剂，IC50为15 nM。它对Chk2的选择性比对Chk1和Cdk1/B激酶高1000倍以上。Chk2 Inhibitor II (BML-277) 剂量依赖性地保护人CD4(+)和CD8(+)T细胞免受电离辐射导致的凋亡。[1-2] |
| IC50 | Chk2(Cell-free assay): 15 nM [1] |
| In Vitro | CHK2 Inhibitor II对Chk2丝氨酸/苏氨酸激酶的选择性比对Cdk1/B和CK1激酶的选择性高1000倍，是一种有效的、选择性的小分子抑制剂，对人类T细胞具有辐射防护作用。将CHK2 inhibitor II和ERK抑制剂组合给药比其单独给药引起更多的细胞凋亡[2]。 |
| In Vivo | 对SUDHL6 DLBCL移植瘤小鼠每隔一天就腹腔注射一次vehicle、ERK inhibitor (5 mg/kg)、CHK2 inhibitor II (1 mg/kg)或组合给药，连续20天，没有发现致死性队形、显著的体重下降或是明显异常。5 mg/kg ERK inhibitor和1 mg/kg CHK2 inhibitor II可适度地抑制肿瘤生长，但组合给药的效果更加明显[2]。 |
| SMILES | ClC(C=C1)=CC=C1OC(C=C2)=CC=C2C3=NC4=CC(C(N)=O)=CC=C4N3 |
| 靶点 | Checkpoint Kinase (Chk) |
| 动物实验 | Female SCID Beige mice were housed in a pathogen-free environment under controlled conditions of light and humidity and received food and water ad libitum. SUDHL6 cells (1.2×106) were resuspended in 100μl PBS and then mixed with an equal volume of Matrigel. The mixture was s.c. injected into the left and right dorsal flanks of 5- to 7-week-old female SCID mice. When the tumour reached the size of 60–163mm3, the treatment was administered intraperitoneally every other day for a total of 20 days. CHK2 inhibitor II in alcohol was diluted in PBS for a final dose of 1mgkg?1. Injection of the vehicle alone was used as a control. At the moment of death, tumours were collected for further analysis. [2] |
| 数据来源文献 | [1] Arienti KL, et al. J Med Chem. 2005, 48(6):1873-85. [2] Dai B, et al. Nat Commun. 2011, 2:402. |
| 规格 | 10mg |
是一种Chk2的ATP竞争性抑制剂。
