SBP-0636457
(Synonyms: SBI-0636457; SB1-0636457) 目录号 : GC63870
SBP-0636457 (SB1-0636457) 是一种 SMAC 模拟物，是 IAP 的拮抗剂。SBP-0636457 以 0.27 μM 的 Ki 与 IAP 蛋白的 BIR 结构域结合。SBP-0636457 可用于实体瘤和血液系统癌症的研究。
Cas No.:1422180-49-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
SBP-0636457 (SB1-0636457) is a SMAC mimetic, and as an IAP antagonist. SBP-0636457 binds to the BIR-domains of the IAP proteins, with a Ki of 0.27 μM. SBP-0636457 can be used for the research of solid tumors and hematologic cancers[1][2].
SBP-0636457 (1-20 μM) demonstrates no cytotoxicity in BT474, BT549, MCF7, and MDA-MB-231 breast cancer cell lines up to a concentration of 20μM[1].SBP-0636457 (10-1000 nM; 20 h) is ef?cacious as TRAIL-sensitizing agents in MDA-MB-231 cells, with an EC50 of 9 nM[1].
[1]. Finlay D, et, al. Small-molecule IAP antagonists sensitize cancer cells to TRAIL-induced apoptosis: roles of XIAP and cIAPs. Mol Cancer Ther. 2014 Jan; 13(1): 5-15.
[2]. Finlay D, et, al. Inducing death in tumor cells: roles of the inhibitor of apoptosis proteins. F1000Res. 2017 Apr 27; 6:587.
| Cas No. | 1422180-49-1 | SDF | Download SDF |
| 别名 | SBI-0636457; SB1-0636457 | ||
| 分子式 | C25H36N4O4 | 分子量 | 456.58 |
| 溶解度 | 储存条件 | 4°C, stored under nitrogen | |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1902 mL | 10.951 mL | 21.902 mL |
| 5 mM | 0.438 mL | 2.1902 mL | 4.3804 mL |
| 10 mM | 0.219 mL | 1.0951 mL | 2.1902 mL |
| 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） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 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GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
体内配方配制方法：取 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 saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
SBP-0636457, a Novel Smac Mimetic, Cooperates with Doxorubicin to Induce Necroptosis in Breast Cancer Cells during Apoptosis Blockage
J Oncol 2022 Jul 11;2022:2390078.PMID:35859663DOI:PMC9293568
Breast cancer (BC) is a common health concern worldwide. Doxorubicin (Dox) is a widely used chemotherapeutic agent to treat various cancers, including BC. However, drug resistance and severe side effects often hinder the clinical application of Dox. Combination therapy is an effective potent strategy to increase chemosensitivity and reduce the adverse effects. Smac is a proapoptotic protein that interacts with inhibitors of apoptosis proteins (IAPs) and thereby promotes cell death. Smac mimetic compounds can mimic its function and can be used to kill cancer cells. In this study, Dox and SBP-0636457, a novel Smac mimetic, were found to have cooperative effects in inducing BC cell death. Dox and SBP-0636457 cotreatment induced necroptosis instead of apoptosis in BC cells. Receptor-interacting serine/threonine-protein kinase 1 or mixed-lineage kinase domain-like silencing could attenuate cell death caused by Dox/SBP-0636457 in BC cells. In addition, this combined treatment caused synergistic induction of TNFα, and TNFα/TNFR signalling is essential for cell death induced by Dox/SBP-0636457 in BC cells. Moreover, both canonical and noncanonical nuclear factor kappa B pathways were found to contribute to TNFα upregulation induced by Dox/SBP-0636457. Therefore, the findings suggest that SBP-0636457 combined with Dox is an alternative strategy for treating BC.