UC 112
(Synonyms: 5-[(苯基甲氧基)甲基]-7-(1-吡咯烷基甲基)-8-喹啉醇) 目录号 : GC16479
UC 112 是一种新型强效 IAP（凋亡抑制剂）抑制剂；有效抑制两种人黑色素瘤（A375 和 M14）和两种人前列腺（PC-3 和 DU145）癌细胞系的细胞生长（IC50\u003d0.7-3.4 uM）。
Cas No.:383392-66-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
UC-112[5-((benzyloxy)methyl)-7-(pyrrolidin-1-ylmethyl)quinolin-8-ol], is inhibitor of inhibitor of apoptosis protein (IAP).[1]
Inhibitor of apoptosis protein (IAP) family is overexpressed in most human cancer cells, but nearly isn’t expressed in adult differentiated tissues. Inhibitor of apoptosis (IAP) proteins are widely considered as promising drug-resistant tumors drug targets. [1,2]
UC-112 strongly activates caspase-3/7 and caspase-9 activities, and selectively reduce surviving level at a concentration as low as 1 mM. Coincubation of UC-112 with a known proteasome inhibitor Z-Leu-Leu-Leu-CHO (MG-132) rescued survivin inhibition. As a single agent, UC-112 strongly inhibits tumor growth and reduces both X chromosomelinked IAP and survivin levels in an A375 human melanoma xenograft model in vivo.[1]
UC-112 inhibits tumor cell growth in several cancer cell lines in vitro and suppresses melanoma tumor growth in vivo. Mechanistic studies indicated that UC-112 selectively inhibits survivin expression and induces strong cancer cell apoptosis. UC-112 could efficiently inhibit tumor cell proliferation by down regulating the level of IAPs, especially survivin protein.[1,2]
References:
[1] Wang J, Li W. Discovery of novel second mitochondria-derived activator of caspase mimetics as selective inhibitor of apoptosis protein inhibitors. J Pharmacol Exp Ther. 2014 May;349(2):319-29.
[2] Xiao M, Wang J, Lin Z, etal. , Design, Synthesis and Structure-Activity Relationship Studies of Novel Survivin Inhibitors with Potent Anti-Proliferative Properties. PLoS One. 2015 Jun 12;10(6):e0129807.
| Cas No. | 383392-66-3 | SDF | |
| 别名 | 5-[(苯基甲氧基)甲基]-7-(1-吡咯烷基甲基)-8-喹啉醇 | ||
| 化学名 | 5-((benzyloxy)methyl)-7-(pyrrolidin-1-ylmethyl)quinolin-8-ol | ||
| Canonical SMILES | OC1=C2C(C=CC=N2)=C(COCC3=CC=CC=C3)C=C1CN4CCCC4 | ||
| 分子式 | C22H24N2O2 | 分子量 | 348.44 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| 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 | 2.8699 mL | 14.3497 mL | 28.6993 mL |
| 5 mM | 0.574 mL | 2.8699 mL | 5.7399 mL |
| 10 mM | 0.287 mL | 1.435 mL | 2.8699 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。