SML3281

GSK215 hydrochloride

≥98% (HPLC)

• Synonym(s): (2S,4R)-4-hydroxy-1-((S)-2-(2-(4-(3-methoxy-4-(4-(2-(methylcarbamoyl)phenylamino)-5-(trifluoromethyl)pyridin-2-ylamino)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide hydrochloride, GSK 215 hydrochloride, GSK-215 hydrochloride
• Empirical Formula (Hill Notation): C₅₀H₅₉F₃N₁₀O₆S · xHCl
• Molecular Weight: 985.13 (free base basis)
• UNSPSC Code: 51111800
• NACRES: NA.21
• MDL number: MFCD34574613
• Assay: ≥98% (HPLC)
• Form: powder
• Storage condition: desiccated

Properties

• 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

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.

Disclaimer

Hygroscopic

Safety Information

• Storage Class: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable