DGY-09-192 is a selective PROTAC degrader designed to target fibroblast growth factor receptors FGFR1 and FGFR2 for proteasomal degradation. According to published data (Xie et al., J Med Chem 2022, 65(21):14544–14558), DGY-09-192 effectively induces degradation of FGFR1 and FGFR2 in cancer cell lines, with DC₅₀ values (half-maximal degradation concentration) of approximately 50–150 nM for FGFR1 and 30–70 nM for FGFR2 in FGFR-driven cell lines like KATO III and NCI-H1581. The compound showed potent antiproliferative activity, with GI₅₀ values (growth inhibition) of around 40–90 nM in FGFR-amplified cancer cells. Mechanistically, it demonstrated robust target engagement, inducing ubiquitination and subsequent proteasomal degradation, outperforming the parent FGFR kinase inhibitor in sustained pathway suppression.
MedKoo Cat#: 123534
Name: DGY-09-192
CAS#: 2504949-52-2
Chemical Formula: C49H59Cl2N11O7S
Exact Mass: 1015.3700
Molecular Weight: 1017.04
Elemental Analysis: C, 57.87; H, 5.85; Cl, 6.97; N, 15.15; O, 11.01; S, 3.15
The following data is based on the product molecular weight 1,017.04 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |