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Purity: ≥98%
TAS-103 dihydrochloride (also known as BMS-247615) is a potent and dual inhibitor of DNA topoisomerase I/II. In tumor models from mice and humans, this derivative of quinoline exhibits antitumor activity. TAS-103 has an IC50 value of 5 nM and is active on CCRF-CEM cells. In individual CCRF-CEM cells, TAS-103 at 0.1 μM significantly increases levels of topo IIα FITC immunofluorescence. HeLa cell viability is inhibited by TAS-103, with an IC50 of 40 nM. At 10 μM, TAS-103 prevents the formation of signal recognition particle (SRP) complexes and causes SRP14 and SRP19 to become unstable, leading to their eventual degradation. Despite the fact that TAS-103 has been described as a strong topoisomerase II poison. Nonetheless, alternative research has demonstrated that there is no association between topoisomerase II expression and cellular susceptibility to TAS-103.
| Targets |
Topoisomerase II; Topoisomerase I
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| Cell Assay |
Human acute lymphoblastic leukemia cells, designated as CCRF-CEM cells, are cultured in RPMI-1640 medium supplemented with 3 mM l-glutamine, 10% foetal bovine serum, 50 U/mL penicillin, and 40 μg/mL streptomycin. The culture is maintained at 37°C in a humidified environment with 5% CO2. In DMSO, TAS-103, CPT, and DACA are dissolved. Both drugs are applied to exponentially growing cells (approximately 5 × 105) for a duration of 2 hours. After being exposed to drugs, cells are centrifuged twice for three minutes at 400 × g in cold phosphate-buffered saline[1].
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| References |
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| Additional Infomation |
TAS-103 is a quinoline derivative that inhibits both topoisomerase I and II, causing a cytotoxic effect in cancer cells. (NCI)
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| Molecular Formula |
C20H21CL2N3O2
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| Molecular Weight |
406.31
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| Exact Mass |
405.101
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| Elemental Analysis |
C, 59.12; H, 5.21; Cl, 17.45; N, 10.34; O, 7.88
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| CAS # |
174634-09-4
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| Related CAS # |
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| PubChem CID |
135413532
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| Appearance |
Red solid powder
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| Boiling Point |
564ºC at 760mmHg
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| Flash Point |
294.9ºC
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| Vapour Pressure |
9.56E-13mmHg at 25°C
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| LogP |
4.39
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
497
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].Cl[H].O=C1C2=C([H])C([H])=C([H])C([H])=C2C2C3C([H])=C([H])C(=C([H])C=3N=C(C=21)N([H])C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H])O[H]
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| InChi Key |
HAYAYGFVSIWSGQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H19N3O2.2ClH/c1-23(2)10-9-21-20-18-17(13-5-3-4-6-14(13)19(18)25)15-8-7-12(24)11-16(15)22-20;;/h3-8,11,24H,9-10H2,1-2H3,(H,21,22);2*1H
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| Chemical Name |
6-[2-(dimethylamino)ethylamino]-3-hydroxyindeno[2,1-c]quinolin-7-one;dihydrochloride
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| Synonyms |
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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. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 3.57 mg/mL (8.79 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4612 mL | 12.3059 mL | 24.6117 mL | |
| 5 mM | 0.4922 mL | 2.4612 mL | 4.9223 mL | |
| 10 mM | 0.2461 mL | 1.2306 mL | 2.4612 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.
Structures of the chemical compounds and preparation of TAS-1-3383-fixed latex beads.Mol Pharmacol.2008 Mar;73(3):987-94. |
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Affinity purification using TAS-1-3383-fixed beads.Mol Pharmacol.2008 Mar;73(3):987-94. |
Effects of TAS-103 on the interactions between SRP54 and other subunits.Mol Pharmacol.2008 Mar;73(3):987-94. |
 Effects of TAS-103 on the SRP complex.Mol Pharmacol.2008 Mar;73(3):987-94. |
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 Effects of TAS-103 and knockdowns of SRP14 or SRP54 on the translocation of IL-6-FLAG.Mol Pharmacol.2008 Mar;73(3):987-94. |
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