TAI-1
目录号 : GC17559
TAI-1 是一种口服活性抗癌剂，是一种高效的一流 Hec1 抑制剂，在 K562 细胞中的 GI50 为 13.48 nM。
Cas No.:1334921-03-7
Sample solution is provided at 25 µL, 10mM.
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TAI-1 is a highly potent, first-in-class inhibitor of Hec1 with IC50 of
TAI-1 has a GI50 of 13.48 nM (K562 cells), which is close to 1000 times improvement in potency compared to INH1 (GI50 =11.7 μM). TAI-1 showed strong inhibition across a broad spectrum of tumor cells. TAI-1 interrupted Hec1-Nek2 protein interaction, led to Nek2 degradation, induced significant chromosomal misalignment in metaphase, and induced apoptotic cell death. TAI-1 was orally active in in vivo animal models of triple negative colon cancer, breast cancer and liver cancer. Preliminary toxicity shows no effect on the organ weights, body weights and blood indices at efficacious doses. TAI-1 shows high specificity to cancer cells and to target and had no effect on the cardiac channel hERG. TAI-1 is synergistic with topotecan, doxorubicin and paclitaxel in breast, leukemia and liver cancer cells. Sensitivity to TAI-1 was associated with the status of P53 and RB gene. Knockdown of P53 and RB in cancer cells increased sensitivity to TAI-1.
References:
[1]. Huang LY, Lee YS, Huang JJ et al. Characterization of the biological activity of a potent small molecule Hec1 inhibitor TAI-1. J Exp Clin Cancer Res. 2014 Jan 9;33:6. doi: 10.1186/1756-9966-33-6.
| Cas No. | 1334921-03-7 | SDF | |
| 化学名 | 4-(4-(4-methoxyphenoxy)-2,6-dimethylphenyl)-N-(1-(pyridin-4-yl)vinyl)thiazol-2-amine | ||
| Canonical SMILES | COC1=CC=C(OC2=CC(C)=C(C3=CSC(NC(C4=CC=NC=C4)=C)=N3)C(C)=C2)C=C1 | ||
| 分子式 | C24H21N3O3S | 分子量 | 431.51 |
| 溶解度 | ≥ 43.2mg/mL 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 | 2.3174 mL | 11.5872 mL | 23.1744 mL |
| 5 mM | 0.4635 mL | 2.3174 mL | 4.6349 mL |
| 10 mM | 0.2317 mL | 1.1587 mL | 2.3174 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet