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1mg |
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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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250mg |
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Purity: ≥98%
Pyridostatin Trifluoroacetate (RR82; RR 82; RR-82; PDS; Pyridostatin TFA), the Trifluoroacetate (TFA) salt of Pyridostatin, is a G-quadruplexe stabilizer with potential antineoplastic activity. In a test without cells, it stabilizes G-quadruplexe at a Kd of 490 nM. Pyridostatin targets Bcl-2, K-ras, and c-kit, among other proto-oncogenes. Pyridostatin induces cell-cycle arrest by activating DNA damage checkpoints and exhibits strong anti-proliferative activity in vitro against a variety of cancer cell lines, including MRC-5-SV40 cells. Pyridostatin interacts with G-quadruplex motifs in SRC to decrease SRC-dependent cell motility in MDA-MB-231 cells as well.
Targets |
G-quadruplexe ( Kd = 490 nM )
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ln Vitro |
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ln Vivo |
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Cell Assay |
After plating the cells at equal confluence, they are either left untreated or continuously treated with 2 μM pyridostatin for the specified amount of time before being harvested. Trypsinization and counting of individual plate cells are done using a Coulter counter. The error bars on graphs show the s.e.m. and the total number of cells at each time interval. The three separate experiments are represented by the data.
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Animal Protocol |
CB17‐SCID mice
7.5 mg/kg i.v. |
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References |
Molecular Formula |
C37H35F9N8O11
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Molecular Weight |
938.72
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Elemental Analysis |
C, 47.34; H, 3.76; F, 18.21; N, 11.94; O, 18.75
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CAS # |
1472611-44-1
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Related CAS # |
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Appearance |
White solid powder
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SMILES |
O=C(C1=NC(C(NC2=NC3=CC=CC=C3C(OCCN)=C2)=O)=CC(OCCN)=C1)NC4=NC5=CC=CC=C5C(OCCN)=C4.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F
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InChi Key |
CYYZQGUDHAKBIQ-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C31H32N8O5.3C2HF3O2/c32-9-12-42-19-15-24(30(40)38-28-17-26(43-13-10-33)20-5-1-3-7-22(20)36-28)35-25(16-19)31(41)39-29-18-27(44-14-11-34)21-6-2-4-8-23(21)37-29;3*3-2(4,5)1(6)7/h1-8,15-18H,9-14,32-34H2,(H,36,38,40)(H,37,39,41);3*(H,6,7)
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Chemical Name |
-(2-aminoethoxy)-N2,N6-bis(4-(2-aminoethoxy)quinolin-2-yl)pyridine-2,6-dicarboxamide tris(2,2,2-trifluoroacetate)
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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 |
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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) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.0653 mL | 5.3264 mL | 10.6528 mL | |
5 mM | 0.2131 mL | 1.0653 mL | 2.1306 mL | |
10 mM | 0.1065 mL | 0.5326 mL | 1.0653 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.
Pyridostatin inhibits growth of BRCA2‐deficient DLD1 xenograft tumours and inflicts repairable DNA damage in BRCA2‐deficient cells. EMBO Mol Med . 2022 Mar 7;14(3):e14501. td> |
Pyridostatin activates innate immune responses in BRCA2‐deficient cells. EMBO Mol Med . 2022 Mar 7;14(3):e14501. td> |
Pyridostatin impairs growth of PARPi‐resistant BRCA1‐deficient tumours and triggers DNA damage and innate immune responses in BRCA1‐deficient PARPi‐resistant cells. EMBO Mol Med . 2022 Mar 7;14(3):e14501. td> |
Pyridostatin-induced transcription- and replication-dependent DNA damage. Nat Chem Biol . 2012 Feb 5;8(3):301-10. td> |
Visual analysis of pyridostatin targets. Nat Chem Biol . 2012 Feb 5;8(3):301-10. td> |
Pyridostatin and hPif1 targeted overlapping sites in cells. Nat Chem Biol . 2012 Feb 5;8(3):301-10. td> |