KSI-3716
目录号 : GC33377
KSI-3716是c-Myc的抑制剂。
Cas No.:1151813-61-4
Sample solution is provided at 25 µL, 10mM.
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KSI-3716 is a c-Myc inhibitor.
KSI-3716 blocks c-MYC/MAX from forming a complex with target gene promoters. KSI-3716 effectively blocks complex formation in a dose dependent manner (IC50=0.84 μM). c-MYC mediated transcriptional activity is inhibited by KSI-3716 at concentrations as low as 1 μM. The expression of c-MYC target genes, such as cyclin D2, CDK4 and hTERT, is markedly decreased. KSI-3716 exerts cytotoxic effects on bladder cancer cells by inducing cell cycle arrest and apoptosis[1].
Intravesical instillation of KSI-3716 at a dose of 5 mg/kg significantly suppresses tumor growth with minimal systemic toxicity[1].
[1]. Jeong KC, et al. Intravesical instillation of c-MYC inhibitor KSI-3716 suppresses orthotopic bladder tumor growth. J Urol. 2014 Feb;191(2):510-8.
Cell experiment: | Ku19-19 cells are seeded 1 day before drug treatment and treated with KSI-3716 (5, 10, 15, 20, 25 μM) for (12, 24, 48 hours). Cell survival assays are performed to count viable cells[1]. |
Animal experiment: | Mice[1][1]The control group is administered solvent and the experimental group (5 tumor bearing mice per group) is administered c-MYC inhibitor KSI-3716 (5 mg/kg) intravesically twice weekly for 3 weeks. Luminescence images are obtained twice weekly[1]. |
References: [1]. Jeong KC, et al. Intravesical instillation of c-MYC inhibitor KSI-3716 suppresses orthotopic bladder tumor growth. J Urol. 2014 Feb;191(2):510-8. | |
| Cas No. | 1151813-61-4 | SDF | |
| Canonical SMILES | ClC1=CC=C(Br)C(NC(NC2=CC=C(Cl)C=C2)=C3C(C)=O)=C1C3=O | ||
| 分子式 | C17H11BrCl2N2O2 | 分子量 | 426.09 |
| 溶解度 | DMSO: 5 mg/mL (11.73 mM) | 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 | 2.3469 mL | 11.7346 mL | 23.4692 mL |
| 5 mM | 0.4694 mL | 2.3469 mL | 4.6938 mL |
| 10 mM | 0.2347 mL | 1.1735 mL | 2.3469 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
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet