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UNC10217938A (UNC7938), a 3-deazapteridine analog with high oligonucleotide enhancing effects, is a destabilizer of the endosome membrane that can enhance the endosome-leakage activity of cell-penetrating peptides and facilitating the endosomal escape of macromolecules initially internalized by mammalian cells via endocytosis.
Physicochemical Properties
| Molecular Formula | C26H28N6O2 |
| Molecular Weight | 456.5395 |
| Exact Mass | 456.227 |
| CAS # | 1347749-97-6 |
| PubChem CID | 57402790 |
| Appearance | Light yellow to yellow solid powder |
| LogP | 4.1 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 7 |
| Rotatable Bond Count | 9 |
| Heavy Atom Count | 34 |
| Complexity | 622 |
| Defined Atom Stereocenter Count | 0 |
| SMILES | O(C([H])([H])C([H])([H])[H])C(N([H])C1C([H])=C(C2=C(N=1)N=C(C1C([H])=C([H])C([H])=C([H])C=1[H])C(C1C([H])=C([H])C([H])=C([H])C=1[H])=N2)N([H])C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H])=O |
| InChi Key | HHICWLZMNOCMIQ-UHFFFAOYSA-N |
| InChi Code | InChI=1S/C26H28N6O2/c1-4-34-26(33)29-21-17-20(27-15-16-32(2)3)24-25(28-21)31-23(19-13-9-6-10-14-19)22(30-24)18-11-7-5-8-12-18/h5-14,17H,4,15-16H2,1-3H3,(H2,27,28,29,31,33) |
| Chemical Name | ethyl N-[8-[2-(dimethylamino)ethylamino]-2,3-diphenylpyrido[2,3-b]pyrazin-6-yl]carbamate |
| Synonyms | UNC 7938UNC 10217938A UNC7938 UNC 10217938A UNC-7938UNC10217938AUNC-10217938-A |
| 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) |
Biological Activity
| ln Vitro | Compared to Retro-1, UNC10217938A is significantly more effective and potent as it significantly increases luciferase induction in HelaLuc705 cells within the 5-25 µM range. UNC10217938A offers a 60-fold enhancement at 10 µM and a 220-fold enhancement at 20 µM when compared to splice switching oligonucleotide (SSO) alone[1]. In contrast, 100 µM Retro-1 only delivers an 11-fold enhancement. Receptor-targeted oligonucleotide conjugates can have their effects significantly increased by UNC10217938A. UNC10217938A has the ability to amplify the effects of both negatively charged and uncharged morpholino oligonucleotides[1]. Cells exposed to UNC10217938A exhibit a significant decrease in TAMRA-oligonucleotide co-localization with the late endosome marker Rab7, but little change in co-localization with the lysosomal marker LAMP-1. UNC10217938A induces a partial release of oligonucleotides into the cytosol from late endosomes through nuclear accumulation[1]. |
| ln Vivo | In EGFP654 mice, systemic treatment with SSO623 and intravenous injection of UNC10217938A (7.5 mg/kg) result in discernible increases in EGFP fluorescence in the liver, kidney, and heart[3]. |
| References |
[1]. High-throughput screening identifies small molecules that enhance the pharmacological effects of oligonucleotides. Nucleic Acids Res. 2015 Feb 27;43(4):1987-96. |
Solubility Data
| Solubility (In Vitro) | DMSO : ~10 mg/mL (~21.90 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.19 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 + to the above solution and mix evenly; then add 450 μL of 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 | 2.1904 mL | 10.9519 mL | 21.9039 mL | |
| 5 mM | 0.4381 mL | 2.1904 mL | 4.3808 mL | |
| 10 mM | 0.2190 mL | 1.0952 mL | 2.1904 mL |