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SM-164 (XIAP抑制剂) |
产品编号: SC0114-10mM
产品包装: 10mM×0.2ml
产品价格: 725.00元 |
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产品简介
产品简介:
化学信息:
化学名 |
(3S,6S,10aS)-N-[(S)-[1-[4-[4-[4-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino )propanoyl]amino]-5-oxo-2,3,6,7,8,9, 10,10a-octahydro-1H-pyrrolo[1,2-a] azocine-3-carbonyl] amino]-phenylme thyl]triazol-1-yl]butyl]phenyl]butyl ]triazol-4-yl]-phenylmethyl]-6-[[(2S) |
简称 |
SM-164 |
别名 |
SM 164, SM164 |
中文名 |
N/A |
化学式 |
C62H84N14O6 |
分子量 |
1121.42 |
CAS号 |
957135-43-2 |
纯度 |
- |
溶剂/溶解度 |
DMSO 12mg/ml |
溶液配制 |
5mg加入0.45ml DMSO,或者每11.21mg加入1ml DMSO,配制成10mM溶液。SC0002-10mM用DMSO配制。 |
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生物信息:
产品描述 |
SM-164 is a potent cell-permeable and bivalent Smac mimetic which bind to a XIAP protein with a Ki value of 0.56nM, and binds to cIAP-1 and cIAP-2 proteins with Ki values of 0.31 and 1.1nM, respectively |
信号通路 |
Apoptosis |
靶点 |
XIAP |
cIAP-1 |
cIAP-2 |
- |
- |
IC50 |
0.56nM(Ki) |
0.31nM(Ki) |
1.1nM(Ki) |
- |
- |
体外研究 |
SM-164 induced complete cIAP-1 degradation, it displayed weak inhibitory effects on the viability of HCC cells. Nevertheless, SM-164 considerably potentiated Apo2 ligand or TNF-related apoptosis-inducing ligand (APO2L/TRAIL)- and Doxorubicin-mediated anticancer activity in HCC cells. Mechanistic studies demonstrated that SM-164 in combination with chemotherapeutic agents resulted in enhanced activation of caspases-9, -3 and cleavage of poly ADP-ribose polymerase (PARP), and also led to decreased AKT activation. Although SM-164 is modestly more effective than SM-122 in induction of cIAP-1/2 degradation, SM-164 is 1,000 times more potent than SM-122 as an inducer of apoptosis in tumor cells, which is attributed to its much higher potency in binding to and antagonizing XIAP. SM-164 radiosensitization in sensitive cells was associated with NF-κB activation and TNFα secretion, followed by activation of caspase-8 and -9, leading to enhanced apoptosis. |
体内研究 |
SM-164 induces rapid cIAP-1 degradation and strong apoptosis in the MDA-MB-231 xenograft tumor tissues and achieves tumor regression, but has no toxicity in normal mouse tissues. SM-164 also radiosensitized human tumor xenograft while causing minimal toxicity. |
临床实验 |
N/A |
特征 |
N/A |
相关实验数据(此数据来自于公开文献,碧云天并不保证其有效性):
细胞系 |
N/A |
浓度 |
N/A |
处理时间 |
N/A |
方法 |
N/A |
动物模型 |
N/A |
配制 |
N/A |
剂量 |
N/A |
给药方式 |
N/A |
参考文献:
1.Zhang S, et al. Smac mimetic SM-164 potentiates APO2L/TRAIL-and doxorubicin-mediated anticancer activity in human hepatocellular carcinoma cells. PLoS One. 2012; 7(12):e51461.
2.Lu J, et al. SM-164: a novel, bivalent Smac mimetic that induces apoptosis and tumor regression by concurrent removal of the blockade of cIAP-1/2 and XIAP. Cancer Res. 2008 Nov 15; 68(22):9384-93.
3.Yang J, et al. Radiosensitization of head and neck squamous cell carcinoma by a SMACmimetic compound, SM-164, requires activation of caspases. Mol Cancer Ther. 2011 Apr; 10(4):658-69.
包装清单:
产品编号 |
产品名称 |
产品包装 |
SC0114-10mM |
SM-164 (XIAP抑制剂) |
10mM×0.2ml |
SC0114-5mg |
SM-164 (XIAP抑制剂) |
5mg |
SC0114-25mg |
SM-164 (XIAP抑制剂) |
25mg |
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说明书 |
1份 |
保存条件:
-20℃保存,至少一年有效。如果溶于非DMSO溶剂,建议分装后-80℃保存,预计6个月内有效。
注意事项:
本产品仅限于专业人员的科学研究用,不得用于临床诊断或治疗,不得用于食品或药品,不得存放 于普通住宅内。
为了您的安全和健康,请穿实验服并戴一次性手套操作。
使用说明
使用说明:
1. 收到产品后请立即按照说明书推荐的条件保存。使用前可以在2,000-10,000g离心数秒,以使液体或粉
末充分沉降至管底后再开盖使用。
2. 对于10mM溶液,可直接稀释使用。对于固体,请根据本产品的溶解性及实验目的选择相应溶剂配制成
高浓度的储备液(母液)后使用。
3. 具体的最佳工作浓度请参考本说明书中的体外、体内研究结果或其它相关文献,或者根据实验目的,
以及所培养的特定细胞和组织,通过实验进行摸索和优化。
4. 不同实验动物依据体表面积的等效剂量转换表请参考如下网页:
http://www.beyotime.com/animal-dose.htm
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