TAI-1 |
رقم الكتالوجGC17559
One-Click Copy Product Info
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TAI-1 ، عامل مضاد للسرطان نشط عن طريق الفم ، هو مثبط قوي للغاية الأول في فئته Hec1 ، مع GI50 من 13.48 نانومتر في خلايا K562
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Chemical Name | 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 | ||
| Formula | C24H21N3O3S | M.Wt | 431.51 |
| الذوبان | ≥ 43.2mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3174 mL | 11.5872 mL | 23.1744 mL |
| 5 mM | 463.5 μL | 2.3174 mL | 4.6349 mL |
| 10 mM | 231.7 μL | 1.1587 mL | 2.3174 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)