| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
| ln Vitro |
SGC-GAK-1 Strong for serine/threonin 16 (STK16), adapter protein 2-associated protein 2 (AAK1), cyclin G-associated protein (GAK), and Ki 3.1 nM, 53 μM, and 51 μM[1]. With a KD of SGCGAK-1 (0.1), 1 and 10 μM, 48 hours or 72 hours, SGC-GAK-1 binds to cyclin G-related product (GAK), coupling agent product 2 (RIPK2), AarF domain containing product 3 (ADCK3), and nemo-like product (NLK) efficiently. revealed substantial growth inhibition at 10 μM at 1.9 nM, 110 nM, 190 nM, and 520 nM on LNCaP, VCaP, and 22Rv1 cells [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: prostate cancer cells (22Rv1, LNCaP, VCaP, PC3, DU145) Tested Concentrations: 0.1, 1, and 10 µM Incubation time has an effect, but has minimal effect on PC3 and DU145 cells [1]. Incubation Duration: 48 hrs (hours) or 72 hrs (hours) Experimental Results: Displayed potent antiproliferative activity in LNCaP and 22Rv1 cells with IC50 of 0.05±0.15 µM and 0.17±0.65 µM, respectively. |
| References |
| Molecular Formula |
C18H17BRN2O3
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|---|---|
| Molecular Weight |
389.243183851242
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| Exact Mass |
388.042
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| CAS # |
2226517-76-4
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| Related CAS # |
2226517-76-4;
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| PubChem CID |
134812846
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
24
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| Complexity |
387
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| Defined Atom Stereocenter Count |
0
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| SMILES |
BrC1C=CC2C(C=1)=C(C=CN=2)NC1C=C(C(=C(C=1)OC)OC)OC
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| InChi Key |
AUOSKLDNVNGKRR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H17BrN2O3/c1-22-16-9-12(10-17(23-2)18(16)24-3)21-15-6-7-20-14-5-4-11(19)8-13(14)15/h4-10H,1-3H3,(H,20,21)
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| Chemical Name |
6-Bromo-N-(3,4,5-trimethoxyphenyl)-4-quinolinamine
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| Synonyms |
SGC-GAK-1 SGCGAK-1 SGC-GAK1 SGC GAK 1
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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 : ~41.67 mg/mL (~107.05 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.34 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), 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. Solubility in Formulation 2: 2.08 mg/mL (5.34 mM) 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; with ultrasonication. 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 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: ≥ 2.08 mg/mL (5.34 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 | 2.5691 mL | 12.8455 mL | 25.6911 mL | |
| 5 mM | 0.5138 mL | 2.5691 mL | 5.1382 mL | |
| 10 mM | 0.2569 mL | 1.2846 mL | 2.5691 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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