| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
TAI-1 (TAI 1; TAI1) is a selective Hec1 (High expression in cancer 1) inhibitor with potential anticancer activity. It inhibits the Hec1-Nek2 protein-protein interaction with a GI50 of 13.48 nM in K562 cells, which is >1000-fold higher than that of INH1 (GI50 =11.7 μM). TAI-1 showed strong anti-proliferative activity in vitro against a broad spectrum of cancer cells.
| ln Vitro |
TAI-1 causes apoptotic cell death, major chromosomal misalignment in metaphase, disruption of the Hec1-Nek2 protein connection, and Nek2 degradation[1]. According to evidence that TAI-1 triggers the activation of apoptotic pathways, it causes cancer cells to die by cleaving the apoptotic proteins Caspase 3 and PARP and degrading the anti-apoptotic protein MCL-1. With GI50 less than 100 nM, TAI-1 is effective against a wide range of cancer cells, including those with chronic myeloid leukemia, cervical cancer, breast cancer, metastatic-pleural, invasive ductal carcinoma, acute myeloid leukemia, myelogenous leukemia, and colorectal carcinoma cells[1].
|
|---|---|
| ln Vivo |
In several cancer xenograft models, TAI-1 (20 mg/kg intravenously IV; 150 mg/kg oral PO/BID) suppresses tumor growth[1].
|
| Animal Protocol |
Animal/Disease Models: CB-17 SCID (severe combined immunodeficient) mouse (6-7 weeks, 21- 24 g)[1].
Doses: 20 mg/kg intravenously (iv)IV/ or 150 mg/kg per oral PO/BID. Route of Administration: QDx28 cycles. Experimental Results: Led to significant tumor growth retardation in Huh-7 and modest tumor inhibition was noted tor the Colo205 and MDA-MB-231 models. Did not lead to any loss in body weight. |
| References |
| Molecular Formula |
C24H21N3O3S
|
|
|---|---|---|
| Molecular Weight |
431.51
|
|
| Exact Mass |
431.13
|
|
| CAS # |
1334921-03-7
|
|
| Related CAS # |
|
|
| PubChem CID |
53389629
|
|
| Appearance |
White to off-white solid powder
|
|
| LogP |
5.948
|
|
| Hydrogen Bond Donor Count |
1
|
|
| Hydrogen Bond Acceptor Count |
6
|
|
| Rotatable Bond Count |
6
|
|
| Heavy Atom Count |
31
|
|
| Complexity |
568
|
|
| Defined Atom Stereocenter Count |
0
|
|
| InChi Key |
NBNNDUZYMXBCOX-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C24H21N3O3S/c1-15-12-20(30-19-6-4-18(29-3)5-7-19)13-16(2)22(15)21-14-31-24(26-21)27-23(28)17-8-10-25-11-9-17/h4-14H,1-3H3,(H,26,27,28)
|
|
| Chemical Name |
N-[4-[4-(4-Methoxyphenoxy)-2,6-dimethylphenyl]-2-thiazolyl]-4-pyridinecarboxamide
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
|
|---|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
