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Purity: ≥98%
| Targets |
SGC GAK 1 targets cyclin G-associated kinase (GAK) with high affinity, exhibiting a Ki of 3.1 nM and a Kd of 1.9 nM. It has >30-fold selectivity over a panel of other kinases.
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| 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].
In vitro, SGC GAK 1 potently binds to GAK with a Ki of 3.1 nM and a Kd of 1.9 nM. It inhibits GAK in live cell assays with an IC50 of 110 nM. It shows strong growth inhibition in LNCaP, VCaP, and 22Rv1 prostate cancer cells at 10 μM. |
| ln Vivo |
In vivo, SGC GAK 1 has been used to study the role of GAK in intracellular membrane trafficking and related signaling pathways. Its effects on tumor growth have been evaluated in xenograft models.
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| Enzyme Assay |
In vitro enzyme assays for SGC GAK 1 involve measuring the inhibition of purified GAK kinase activity. The enzyme is incubated with a peptide substrate and ATP in the presence of varying concentrations of the compound. The phosphorylation of the substrate is measured using radioactivity (e.g., [³²P]-ATP) or by a fluorescence-based method. The IC50 or Ki is determined from the inhibition curve.
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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. In vitro cellular assays for SGC GAK 1 are performed using cancer cell lines, particularly prostate cancer cells (e.g., LNCaP, VCaP). Cells are treated with the compound for 72 hours, and cell viability is measured using CellTiter-Glo or MTT assays. The compound's effect on GAK-mediated endocytosis can be assessed by measuring the uptake of fluorescently labeled transferrin or EGF. |
| Animal Protocol |
In vivo animal studies for SGC GAK 1 are conducted in mouse xenograft models using prostate cancer cell lines. Tumor-bearing mice are treated with the compound orally or intraperitoneally, and tumor volume is measured over time. The compound's ability to inhibit tumor growth is assessed, and tumor tissue is analyzed for GAK inhibition and downstream signaling effects.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for SGC GAK 1 are not detailed in publicly available sources. As a cell-active chemical probe, its properties have been optimized for cellular and in vivo studies. Standard PK parameters would be assessed in rodent models for further development.
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| Toxicity/Toxicokinetics |
Toxicological data for SGC GAK 1 are not widely published. As a research compound, its safety profile would be evaluated in the context of specific studies. No significant toxicity has been reported in the available literature at the doses used for in vivo experiments.
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| References | |
| Additional Infomation |
SGC GAK 1 is a research-grade small molecule chemical probe for cyclin G-associated kinase (GAK). It is not an approved drug. It is used to study the role of GAK in various cellular processes, including endocytosis, vesicular transport, and cancer cell proliferation. It is a valuable tool for target validation and drug discovery.
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| 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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