[CAS NO. 2226517-76-4] SGC-GAK-1
PRODUCTS SPECIFICATIONS [2226517-76-4]
DESCRIPTION [2226517-76-4]
Overview
| MDL | MFCD31689258 |
|---|---|
| Molecular Weight | 389.24 |
| Molecular Formula | C18H17BrN2O3 |
| SMILES | COC1=C(C(OC)=CC(NC2=CC=NC3=CC=C(C=C23)Br)=C1)OC |
1 Publications Citing Use of MCE
Summary
SGC-GAK-1 is a potent, selective cyclin G-associated kinase ( GAK ) inhibitor with a K i of 3.1 nM. SGC-GAK-1 is a chemical probe for GAK [1] .
IC50 & Target
Ki: 3.1 nM (GAK) [1]
In Vitro
SGC-GAK-1 potently binds cyclin G-associated kinase (GAK), adaptor protein 2-associated kinase (AAK1), serine/threonine kinase 16 (STK16) with K
i
s of 3.1 nM, 53 µM, 51 µM, respectively
[1]
.
SGC-GAK-1 potently binds cyclin G-associated kinase (GAK), receptor-interacting protein kinase 2 (RIPK2), AarF domain containing kinase 3 (ADCK3), and nemo-like kinase (NLK) with K
D
s of 1.9 nM, 110 nM, 190 nM, and 520 nM, respectively
[1]
.
SGCGAK-1 (0.1, 1, and 10 µM, 48 hours or 72 hours) shows strong growth inhibition in LNCaP, VCaP, and 22Rv1 cells at 10 µM, but minimal effect in PC3 and DU145 cells
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | Prostate cancer cells (22Rv1, LNCaP, VCaP, PC3, DU145) |
| Concentration: | 0.1, 1, and 10 µM |
| Incubation Time: | 48 hours or 72 hours |
| Result: | Showed potent antiproliferative activity in LNCaP and 22Rv1 cells with IC 50 s of 0.05±0.15 µM and 0.17±0.65 µM, respectively. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 41.67 mg/mL ( 107.05 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |