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Pyridostatin HCl (RR82) is a G-quadruplexe stabilizer with Kd of 490 nM in a cell-free assay, which targets a series of proto-oncogenes including c-kit, K-ras and Bcl-2. Pyridostatin induces cell-cycle arrest by activating DNA damage checkpoints, which reduces the proliferation of MRC-5-SV40 cells and other cancer cell lines. 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 |
Pyridostatin (RR82) hydrochloride (10 μM; 48 hours) induces cell cycle arrest[1].
Pyridostatin hydrochloride is a small molecule that selectively binds to G-quadruplex DNA, forming a complex that stabilizes the G-quadruplex structure. Neurite retraction, synaptic loss, and dose-dependent neuronal death are brought on by pyridostatin hydrochloride. Pyridostatin hydrochloride induces the formation of DNA double-strand breaks in primary neurons in culture. The BRCA1 protein, which protects and fixes the neuronal genome, is remarkably downregulated at the transcriptional level by pyridogallostatin hydrochloride (1–5 μM, overnight)[3]. |
| Cell Assay |
Cell Line: Over 60 different cancer cell lines
Concentration: 10 μM Incubation Time: 48 hours Result: Predominantly accumulated in the G2 phase of the cell cycle over 60 different cancer cell lines. |
| References |
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| Molecular Formula |
C₃₁H₃₇CL₅N₈O₅
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|---|---|
| Molecular Weight |
778.94
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| Exact Mass |
778.130005
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| CAS # |
1781882-65-2
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| Related CAS # |
Pyridostatin;1085412-37-8;Pyridostatin TFA;1472611-44-1
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| Appearance |
solid
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| SMILES |
C1=CC=C2C(=C1)C(=CC(=N2)NC(=O)C3=CC(=CC(=N3)C(=O)NC4=NC5=CC=CC=C5C(=C4)OCCN)OCCN)OCCN.Cl.Cl.Cl.Cl.Cl
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| InChi Key |
SRIZPFGTXSQRFM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H32N8O5.5ClH/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;;;;;/h1-8,15-18H,9-14,32-34H2,(H,36,38,40)(H,37,39,41);5*1H
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| Chemical Name |
4-(2-aminoethoxy)-2-N,6-N-bis[4-(2-aminoethoxy)quinolin-2-yl]pyridine-2,6-dicarboxamide;pentahydrochloride
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| Synonyms |
RR82 hydrochloride; Pyridostatin hydrochloride
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| 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)
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| Solubility (In Vitro) |
H2O: ~50 mg/mL (~64.2 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (128.38 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2838 mL | 6.4190 mL | 12.8380 mL | |
| 5 mM | 0.2568 mL | 1.2838 mL | 2.5676 mL | |
| 10 mM | 0.1284 mL | 0.6419 mL | 1.2838 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.
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