Name | Gefitinib-based PROTAC 3 |
Synonyms | NTN21277 Gefitinib-based PROTAC 3 NTN21277(Gefitinib-based PROTAC 3) |
CAS | 2230821-27-7 |
Molecular Formula | C47H57ClFN7O8S |
Molar Mass | 934.52 |
Density | 1.300±0.06 g/cm3(Predicted) |
Boling Point | 1065.6±65.0 °C(Predicted) |
Solubility | DMSO : 60 mg/mL (64.20 mM) |
pKa | 14.07±0.40(Predicted) |
Storage Condition | 2-8°C |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.07 ml | 5.35 ml | 10.701 ml |
5 mM | 0.214 ml | 1.07 ml | 2.14 ml |
10 mM | 0.107 ml | 0.535 ml | 1.07 ml |
5 mM | 0.021 ml | 0.107 ml | 0.214 ml |
biological activity | Gefitinib-based PROTAC 3 coupling EGFR binding element with VHL ligand through connector can induce degradation of EGFR and its mutants. DC50 values in HCC827 (exon 19) and H3255(L858R) are 11.7 nM and 22.3 nM respectively. |
target | TargetValue EGFR (in HCC827(Exon 19 del) cells) 11.7 nM(DC50) EGFR (in H3255 (L858R) cells) 22.3 nM(DC50) |
Target | Value |
EGFR (in HCC827(Exon 19 del) cells) | 11.7 nM(DC50) |
EGFR (in H3255 (L858R) cells) | 22.3 nM(DC50) |
use | EGFR binding element can be combined with VHL ligand through linker to act on HCC827 and H3255 cells to induce EGFR degradation. DC50 is 11.7nM and 22.3 nM respectively. |