Voreloxin (Synonyms: SNS-595, Voreloxin) |
| Catalog No.GC13544 |
An inhibitor of topoisomerase II
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 175414-77-4
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Voreloxin, formerly known as SNS-595 or AG-7352, is a novel naphthyridine analog, which is structurally related to the quinolone antibiotics, a chemical class not previously used for the treatment
of cancer.
In vitro: In vitro studies demonstrated voreloxin has broad anti-proliferative activity in 11 tumor cell lines, with IC50 values ranging from 0.04 to 0.97 μM. Similar activity was observed in vitro in drug-resistant cell lines, including those that overexpress P-glycoprotein [2].
In vivo: After a single intravenous dose, voreloxin concentrations in tumor were correlated with induction of the apoptosis marker caspase-3. Administration of voreloxin at 20 mg/kg weekly inhibited tumor growth (86%). Voreloxin demonstrated strong dose-dependent tumor growth inhibition (63–88%) in 10 of 11 solid tumor xenograft models [2].
Clinical trial: Voreloxin showed an acceptable safety profile with clinical activity in patients with relapsed/refractory solid tumors. The maxmum tolerence dose was schedule-dependent. Voreloxin is now in clinical studies of ovarian cancer and acute myeloid leukemia [3].
References:
[1] Tsuzuki Y, Tomita K, Shibamori K, Sato Y, Kashimoto S, Chiba K. Synthesis and structure-activity relationships of novel 7-substituted 1,4-dihydro-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acids as antitumor agents. Part 2. J Med Chem. 2004;47(8):2097-109.
[2] Hoch U, Lynch J, Sato Y, Kashimoto S, Kajikawa F, Furutani Y, Silverman JA. Voreloxin, formerly SNS-595, has potent activity against a broad panel of cancer cell lines and in vivo tumor models. Cancer Chemother Pharmacol. 2009;64(1):53-65.
[3] Advani RH, Hurwitz HI, Gordon MS, Ebbinghaus SW, Mendelson DS, Wakelee HA, Hoch U, Silverman JA, Havrilla NA, Berman CJ, Fox JA, Allen RS, Adelman DC. Voreloxin, a first-in-class anticancer quinolone derivative, in relapsed/refractory solid tumors: a report on two dosing schedules. Clin Cancer Res. 2010;16(7):2167-75.
| Cell experiment [1]: | |
|
Cell lines |
SK-BR-3, ScaBER, PANC-1, KB, HCT116, SKOV3, GT3TKB, Hs746T, Calu-6, NCI-H460, PA-1, MES-SA, SBC-3, SBC-3/ETP and PC-14 cells |
|
Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reaction Conditions |
0.04 ~ 1.155 μM; 72 hrs |
|
Applications |
Voreloxin exhibited broad anti-proliferative activity in 15 cell lines, including 4 drug-resistant lines, with the IC50 values ranging from 0.04 to 1.155 μM. |
| Animal experiment [2]: | |
|
Animal models |
Mice implanted with P388 leukemia cells |
|
Dosage form |
3.13, 12.5 or 50 mg/kg; i.p.; on days 1 and 5 after tumor implantation |
|
Applications |
In mice implanted with P388 leukemia cells, Voreloxin (50 mg/kg, i.p.) showed potent antitumor activity. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Hoch U, Lynch J, Sato Y, Kashimoto S, Kajikawa F, Furutani Y, Silverman JA. Voreloxin, formerly SNS-595, has potent activity against a broad panel of cancer cell lines and in vivo tumor models. Cancer Chemother Pharmacol. 2009;64(1):53-65. [2]. Tsuzuki Y, Tomita K, Shibamori K, Sato Y, Kashimoto S, Chiba K. Synthesis and structure-activity relationships of novel 7-substituted 1,4-dihydro-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acids as antitumor agents. Part 2. J Med Chem. 2004;47(8):2097-109. | |
| Cas No. | 175414-77-4 | SDF | |
| Synonyms | SNS-595, Voreloxin | ||
| Chemical Name | 7-[(3S,4S)-3-methoxy-4-(methylamino)pyrrolidin-1-yl]-4-oxo-1-(1,3-thiazol-2-yl)-1,8-naphthyridine-3-carboxylic acid | ||
| Canonical SMILES | CNC1CN(CC1OC)C2=NC3=C(C=C2)C(=O)C(=CN3C4=NC=CS4)C(=O)O | ||
| Formula | C18H19N5O4S | M.Wt | 401.44 |
| Solubility | <4.01 mg/mL in DMSO, <2.51 mg/mL in EtOH, <2.49 mg/mL in Water | 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 | 2.491 mL | 12.4552 mL | 24.9103 mL |
| 5 mM | 0.4982 mL | 2.491 mL | 4.9821 mL |
| 10 mM | 0.2491 mL | 1.2455 mL | 2.491 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 ddH2O, 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%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *