Size | Price | Stock | Qty |
---|---|---|---|
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
1g |
|
||
2g |
|
||
Other Sizes |
|
Purity: ≥98%
Fludarabine (also known as FaraA, Fludarabinum; NSC-118218; F-ara-A, HSDB6964; NSC118218; HSDB-6964) is a potent STAT1 activation inhibitor and a DNA synthesis inhibitor that has been approved as a chemotherapeutic drug for the treatment of leukemia and lymphoma. In order to cause biological activity, the prodrug fludarabine must be phosphorylated in cells to produce nucleoside triphosphate, or F-ara-ATP. It had an impact on several enzymes needed for DNA synthesis, including ribonucleotide reductase, DNA primase, DNA polymerases, DNA ligase I, and the 3'–5' exonuclease activity of DNA polymerases δ and ΰ. Fludarabine decreased Akt phosphorylation and markedly slowed down the growth of human myeloma cell RPMI8226.
Targets |
STAT1
|
||
---|---|---|---|
ln Vitro |
|
||
ln Vivo |
|
||
Cell Assay |
Fludarabine- or control-treated human MM cell lines, RPMI8226 and U266 (5 × 105 cells), that are dexamethasone-sensitive (MM.1S) and -resistant (MM.1R) are fixed with 70% ice-cold ethanol, centrifuged, and suspended in PBS containing 100 μg/mL RNase A. Sampling is done in 25 μg/mL propidium iodide after 30 minutes of incubation at 37 ºC. The FACSCalibur automated system is used to perform flow cytometry. As per the manufacturer's instructions, apoptosis is identified using the Annexin V-FITC apoptosis detection kit. In situ cell death detection kit-assisted flow cytometry is used to analyze cells for the TUNEL (terminal deoxynucleotidyl transferase-mediated deoxyuridine triphosphate nick end labeling) assay.
|
||
Animal Protocol |
|
||
References |
Molecular Formula |
C10H12FN5O4
|
|
---|---|---|
Molecular Weight |
285.23
|
|
Exact Mass |
285.09
|
|
Elemental Analysis |
C, 42.11; H, 4.24; F, 6.66; N, 24.55; O, 22.44
|
|
CAS # |
21679-14-1
|
|
Related CAS # |
|
|
Appearance |
Solid powder
|
|
SMILES |
C1=NC2=C(N=C(N=C2N1[C@H]3[C@H]([C@@H]([C@H](O3)CO)O)O)F)N
|
|
InChi Key |
HBUBKKRHXORPQB-FJFJXFQQSA-N
|
|
InChi Code |
InChI=1S/C10H12FN5O4/c11-10-14-7(12)4-8(15-10)16(2-13-4)9-6(19)5(18)3(1-17)20-9/h2-3,5-6,9,17-19H,1H2,(H2,12,14,15)/t3-,5-,6+,9-/m1/s1
|
|
Chemical Name |
(2R,3S,4S,5R)-2-(6-amino-2-fluoropurin-9-yl)-5-(hydroxymethyl)oxolane-3,4-diol
|
|
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 (8.76 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 25.0 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: ≥ 2.5 mg/mL (8.76 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.5059 mL | 17.5297 mL | 35.0594 mL | |
5 mM | 0.7012 mL | 3.5059 mL | 7.0119 mL | |
10 mM | 0.3506 mL | 1.7530 mL | 3.5059 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 |
NCT03524235 | Active Recruiting |
Drug: Fludarabine Drug: Rituximab |
CLL Leukemia Lymphoma |
Noah Merin | July 18, 2018 | Phase 1 |
NCT00719888 | Active Recruiting |
Drug: Fludarabine Drug: Thiotepa |
Burkitt Lymphoma Myelofibrosis |
Fred Hutchinson Cancer Center |
November 18, 2005 | Phase 2 |
NCT03434769 | Active Recruiting |
Drug: Fludarabine Drug: Cyclophosphamide |
Non-Hodgkin Lymphoma | Benjamin Tomlinson | July 9, 2018 | Phase 1 |
NCT00577278 | Active Recruiting |
Drug: fludarabine phosphate Drug: melphalan |
Leukemia Lymphoma |
City of Hope Medical Center | October 3, 2007 | Phase 2 |
NCT01163357 | Active Recruiting |
Drug: fludarabine phosphate Drug: bortezomib |
Loss of Chromosome 17p Plasma Cell Leukemia |
City of Hope Medical Center | January 28, 2011 | Phase 1 |