CSN5i-3
目录号 : GC34340
CSN5i-3是一种有效的，选择性和口服的CSN5抑制剂;抑制CSN催化的Cul1deneddylationIC50值为5.8nM。
Cas No.:2375740-98-8
Sample solution is provided at 25 µL, 10mM.
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CSN5i-3 is a potent, selective and orally available inhibitor of CSN5; inhibits CSN-catalysed Cul1 deneddylation with an IC50 value of 5.8 nM.
CSN5i-3 traps CRLs in the neddylated state, which leads to inactivation of a subset of CRLs by inducing degradation of their substrate recognition module[1].
CSN5i-3 shows a good pharmacokinetic profile. CSN5i-3 inhibits growth of human xenograft. Treatment with CSN5i-3 triggers the formation of cleaved PARP and cleaved caspase 3 indicative of apoptosis induction[1].
[1]. Schlierf A, et al. Targeted inhibition of the COP9 signalosome for treatment of cancer. Nat Commun. 2016 Oct 24;7:13166.
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Cell experiment: |
Cell viability is measured using the CellTiter-Glo Assay. Cells (THP-1, HCT116, NCI-H2030 and TE-1) are treated with CSN5i-3 (1 nM, 10 nM, 100 nM, 1 μM, 10 μM) for 72 hours[1]. |
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Animal experiment: |
Mice[1]SU-DHL-1 xenografts were grown in SCID-bg mice and dosed by oral administration with either vehicle control or CSN5i-3 at the indicated doses (50 mg/kg BID, 100mg/kg QD) and schedules (3, 7, 10, 14 day). Tumour response is reported as percentage change in tumour volume at the last day of treatment relative to start of treatment. |
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References: [1]. Schlierf A, et al. Targeted inhibition of the COP9 signalosome for treatment of cancer. Nat Commun. 2016 Oct 24;7:13166. |
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| Cas No. | 2375740-98-8 | SDF | |
| Canonical SMILES | O=C(C1=CC(C(F)F)=NN1C(C)C)NC2=CC(C3=CC=CC=C3)=C([C@@H]4N5C(CCC[C@@H]4O)=CN=C5)C=C2 | ||
| 分子式 | C28H29F2N5O2 | 分子量 | 505.56 |
| 溶解度 | DMSO: ≥ 100 mg/mL (197.80 mM) | 储存条件 | Store at -20°C, protect from light, 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 | 1.978 mL | 9.89 mL | 19.78 mL |
| 5 mM | 0.3956 mL | 1.978 mL | 3.956 mL |
| 10 mM | 0.1978 mL | 0.989 mL | 1.978 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。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet