产品介绍
Product Description
Biochem/physiol Actions
GSK215 is a potent and selective focal adhesion kinase (FAK) degrader (DC50 = 1.3 nM; A549 cells) composed of the FAK inhibitor VS-4718 and the VHL E3 ligase binder VHL-021. GSK215 shows cell type-dependent growth inhibition, where it inhibits A549 (IC50 <1 µM) and MCF-7 (IC50 <0.1 µM), but not BT474, in 2D cultures, while the growth of BT47 (IC50 <0.1 µM) and MCF-7 (IC50 ~0.1 µM), but not A5494, are inhibited by GSK215 in 3D cultures.
Potent and selective focal adhesion kinase (FAK) degrader composed of the FAK inhibitor VS-4718 and the VHL E3 ligase binder VHL-021.
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Hygroscopic
技术参数
Specifications
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| composition | , 0-8 (H2O),, 1.8-3.3 mol (HCl) |
| storage condition | desiccated |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear (warmed) |
| storage temp. | 2-8°C |
| SMILES string | FC(F)(F)c1cnc(cc1Nc7c(cccc7)C(=O)NC)Nc2c(cc(cc2)N3CCN(CC3)CC(=O)N[C@@H](C(C)(C)C)C(=O)N4[C@@H](C[C@H](C4)O)C(=O)N[C@@H](C)c5ccc(cc5)c6[s]cnc6C)OC |
| InChI key | ZGSWGXNEXAXEGV-XFCHVEHOSA-N |
