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| 5mg |
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| 10mg |
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| 25mg |
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Purity: ≥98%
GDP366 is a novel, potent, selective small molecule and dual inhibitor of survivin and Op18, it induces cell growth inhibition, cellular senescence and mitotic catastrophe in human cancer cells. Survivin appears to be essential for cell cycle progression as well as cell survival, according to mounting evidence. Op18/stathmin is an oncoprotein that controls the stabilization of microtubules. Op18 and survivin have both been suggested as potential therapeutic targets for cancer. However, only a small number of small molecule survivin and Op18 inhibitors have been reported. GDP366 potently and selectively inhibited the expression of both survivin and Op18. Survivin and Op18 saw a decline in their protein and mRNA levels. Although the levels of p53 and p21 were potently raised by GDP366, this inhibitory effect was not reliant on their health. In vivo (nude mouse model) and in vitro (GDP366), tumor cell growth was markedly inhibited by GDP366 without apoptosis being induced quickly. In several different cancer cell lines, GDP366 induced polyploidy. By decreasing the activity of the telomerase enzyme, GDP366 accelerated chromosomal instability and triggered cellular senescence. According to our findings, GDP366 is a brand-new dual inhibitor of Op18 and Survivin. Additional translational testing of this compound is warranted in light of our findings.
| Targets |
Survivin; Op18
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|---|---|
| ln Vitro |
Survivin and Op18 expression are both potently and specifically inhibited by GDP366. Survivin and Op18 have lower mRNA and protein levels as a result of GDP366. Despite the fact that GDP366 significantly raises the levels of p53 and p21, this inhibitory effect is not reliant on their health. In vitro and in vivo (using a nude mouse model), GDP366 significantly slows the growth of tumor cells without quickly inducing apoptosis. Multiple kinds of cancer cell lines are induced to become polyploid by GDP366. By decreasing telomerase activity, GDP366 causes chromosomal instability to increase and accelerates cellular senescence[1].
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| References |
| Molecular Formula |
C20H17N5OS
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|---|---|
| Molecular Weight |
375.44688
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| Exact Mass |
375.115
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| Elemental Analysis |
C, 63.98; H, 4.56; N, 18.65; O, 4.26; S, 8.54
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| CAS # |
501698-03-9
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| Related CAS # |
501698-03-9
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| PubChem CID |
6539985
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
27
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| Complexity |
513
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DZSUJUOJJJCWGG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H17N5OS/c1-12-3-2-4-15(9-12)25-20(26)24-14-7-5-13(6-8-14)16-10-27-19-17(16)18(21)22-11-23-19/h2-11H,1H3,(H2,21,22,23)(H2,24,25,26)
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| Chemical Name |
1-[4-(4-aminothieno[2,3-d]pyrimidin-5-yl)phenyl]-3-(3-methylphenyl)urea
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| Synonyms |
GDP 366; GDP366; GDP-366
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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 |
| 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) |
DMSO: ~62.5 mg/mL (~166.5 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.54 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 20.8 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6635 mL | 13.3174 mL | 26.6347 mL | |
| 5 mM | 0.5327 mL | 2.6635 mL | 5.3269 mL | |
| 10 mM | 0.2663 mL | 1.3317 mL | 2.6635 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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