Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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Other Sizes |
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Targets |
Hec1/Nek2
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ln Vitro |
T-1101 tosylate exhibits significant in vitro antiproliferative activity (IC50: 14.8–21.5 nM)[1].
T-1101 tosylate disrupts the Hec1/Nek2 protein–protein interaction in the cells[1]. T-1101 tosylate (1μM; 3-24 24 hours) decreases the level of Nek2 in a time-dependent manner[1]. T-1101 tosylate (1 M; 24 hours) causes apoptosis[1]. T-1101 tosylate reduces amounts of cell-cycle related proteins cyclin A1, cyclin B1, and cyclin D1[1]. |
ln Vivo |
T-1101 tosylate exhibits good oral bioavailability and thermal stability [1].
Oral co-administration of T-1101 tosylate (2.5 mg/kg; p.o.; twice daily) reduces the dose of sorafenib (25 mg/kg to 12.5 mg/kg) needed to exhibit comparable in vivo activity against Huh-7 xenografts [1]. In mice with various human cancer xenografts, T-1101 tosylate (2.5 mg/kg; p.o.; twice daily) exhibits significant in vivo activity[1]. |
References |
Molecular Formula |
C₃₁H₃₁N₅O₆S₃
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Molecular Weight |
665.80
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Exact Mass |
665.1436
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Elemental Analysis |
C, 55.92; H, 4.69; N, 10.52; O, 14.42; S, 14.45
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CAS # |
2250404-95-4
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Related CAS # |
1438638-83-5;2250404-95-4;
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Appearance |
Solid powder
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SMILES |
CC1=CC=C(C=C1)S(=O)(=O)O.CC1=CC(=CC(=C1C2=CSC(=N2)NC(=O)C3=CC=NC=C3)C)SC4=NC=C(N=C4)OCCOC
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InChi Key |
OUJWEAVKLYQREM-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C24H23N5O3S2.C7H8O3S/c1-15-10-18(34-21-13-26-20(12-27-21)32-9-8-31-3)11-16(2)22(15)19-14-33-24(28-19)29-23(30)17-4-6-25-7-5-17;1-6-2-4-7(5-3-6)11(8,9)10/h4-7,10-14H,8-9H2,1-3H3,(H,28,29,30);2-5H,1H3,(H,8,9,10)
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Chemical Name |
N-[4-[4-[5-(2-methoxyethoxy)pyrazin-2-yl]sulfanyl-2,6-dimethylphenyl]-1,3-thiazol-2-yl]pyridine-4-carboxamide;4-methylbenzenesulfonic acid
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Synonyms |
T-1101 tosylate; TAI-95 tosylate; T1101; TAI95;T1101 tosylate; TAI95 tosylate; T 1101; TAI 95
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: 62.5~100 mg/mL (93.87~150.2 mM)
Ethanol: ~3 mg/mL (~4.5 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.12 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.5020 mL | 7.5098 mL | 15.0195 mL | |
5 mM | 0.3004 mL | 1.5020 mL | 3.0039 mL | |
10 mM | 0.1502 mL | 0.7510 mL | 1.5020 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04685473 | Recruiting | Drug: T-1101 (Tosylate) | Advanced Refractory Solid Tumors | Taivex Therapeutics Corporation | January 7, 2021 | Phase 1 |
NCT03349073 | Completed | Drug: T-1101 (Tosylate) | Advanced Refractory Solid Tumors |
Taivex Therapeutics Corporation | September 14, 2017 | Phase 1 |