| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
AP sites can become new substrates when TH10785 (6.25 μM, 30 min) induces de novo β,δ-elimination in vitro [1]. By targeting AP sites, TH10785 (10 μM, 0–2 minutes) enables OGG1 to improve DNA repair [1]. TH10785 (0–20 μM, 72 hours) causes cells to become dependent on PNKP1 and activates OGG1 β and δ-lyase [1]. When an AP site analog containing double-stranded DNA (KD=1.3 μM) is added, the affinity of TH10785 (2 μM) for OGG1 (KD=5.5 μM) increases [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: U2OS Cell Tested Concentrations: 0-20 μM Incubation Duration: 72 hrs (hours) Experimental Results: Reduction by combination of TH10785 and PNKP1 inhibition. Western Blot Analysis[1] Cell Types: U2OS Cell Tested Concentrations: 0.65 μM; 10 μM Incubation Duration: 30 minutes; 24 hrs (hours) Experimental Results: In the presence of TH10785, combined PNKP1 inhibition and OGG1 inhibition of AP sites via β, δ-elimination APE1-independent de novo β, δ-elimination causes upregulation of DDR members. RT-PCR[1] Cell Types: U2OS Cell Tested Concentrations: 10 μM Incubation Duration: 1 hour Experimental Results: diminished oxidative damage in guanine-rich regions of the genome. Immunofluorescence[1] Cell Types: U2OS OGG1-GFP Cell Tested Concentrations: 1 μM Incubation Duration: 0-2 minutes Experimental Results: More OGG1 is recruited at the laser injury site. |
| References |
| Molecular Formula |
C17H21N3
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|---|---|
| Molecular Weight |
267.37
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| Exact Mass |
267.173
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| CAS # |
1002801-51-5
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| PubChem CID |
8078523
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| Appearance |
White to off-white solid powder
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| LogP |
4.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
322
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1=C2C(C=CC=C2)=C(NC2CCCCC2)N=C1C1CC1
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| InChi Key |
ZQMGQZOHIDOPCQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H21N3/c1-2-6-13(7-3-1)18-17-14-8-4-5-9-15(14)19-16(20-17)12-10-11-12/h4-5,8-9,12-13H,1-3,6-7,10-11H2,(H,18,19,20)
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| Chemical Name |
N-cyclohexyl-2-cyclopropylquinazolin-4-amine
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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 : ≥ 100 mg/mL (~374.01 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.35 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), suspension 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 (9.35 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 (9.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7401 mL | 18.7007 mL | 37.4014 mL | |
| 5 mM | 0.7480 mL | 3.7401 mL | 7.4803 mL | |
| 10 mM | 0.3740 mL | 1.8701 mL | 3.7401 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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