(2S,4R)-1-((S)-2-(3-(2-((5-((4-((3-氯-4-氟苯基)氨基)-7-甲氧基喹唑啉-6-基)氧基)戊基)氧基)乙氧基)丙酰胺基)-3,3-二甲基丁酰基)-4-羟基-N-(4-(4-甲基噻唑-5-基)苄基)吡咯烷-2-甲酰胺
Gefitinib-based PROTAC 3
CAS: 2230821-27-7
Molecular Formula: C47H57ClFN7O8S
(2S,4R)-1-((S)-2-(3-(2-((5-((4-((3-氯-4-氟苯基)氨基)-7-甲氧基喹唑啉-6-基)氧基)戊基)氧基)乙氧基)丙酰胺基)-3,3-二甲基丁酰基)-4-羟基-N-(4-(4-甲基噻唑-5-基)苄基)吡咯烷-2-甲酰胺 - Names and Identifiers
| Name | Gefitinib-based PROTAC 3 |
| Synonyms | NTN21277 Gefitinib-based PROTAC 3 NTN21277(Gefitinib-based PROTAC 3) |
| CAS | 2230821-27-7 |
(2S,4R)-1-((S)-2-(3-(2-((5-((4-((3-氯-4-氟苯基)氨基)-7-甲氧基喹唑啉-6-基)氧基)戊基)氧基)乙氧基)丙酰胺基)-3,3-二甲基丁酰基)-4-羟基-N-(4-(4-甲基噻唑-5-基)苄基)吡咯烷-2-甲酰胺 - Physico-chemical Properties
| 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 |
(2S,4R)-1-((S)-2-(3-(2-((5-((4-((3-氯-4-氟苯基)氨基)-7-甲氧基喹唑啉-6-基)氧基)戊基)氧基)乙氧基)丙酰胺基)-3,3-二甲基丁酰基)-4-羟基-N-(4-(4-甲基噻唑-5-基)苄基)吡咯烷-2-甲酰胺 - Preparation solution concentration reference
| 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 |
Last Update：2024-01-02 23:10:35
(2S,4R)-1-((S)-2-(3-(2-((5-((4-((3-氯-4-氟苯基)氨基)-7-甲氧基喹唑啉-6-基)氧基)戊基)氧基)乙氧基)丙酰胺基)-3,3-二甲基丁酰基)-4-羟基-N-(4-(4-甲基噻唑-5-基)苄基)吡咯烷-2-甲酰胺 - Reference Information
| 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. |
Last Update：2024-04-09 21:31:57
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View History
(2S,4R)-1-((S)-2-(3-(2-((5-((4-((3-氯-4-氟苯基)氨基)-7-甲氧基喹唑啉-6-基)氧基)戊基)氧基)乙氧基)丙酰胺基)-3,3-二甲基丁酰基)-4-羟基-N-(4-(4-甲基噻唑-5-基)苄基)吡咯烷-2-甲酰胺
2-AMINO-3-HYDROXY-2-METHYL-3-(4-NITRO-PHENYL)-PROPIONIC ACID
3-AMINO-2-HYDROXY-4-PHENYLBUTYRIC ACID
异乌药内酯
Benzoic acid, 3-aMino-5-b...
1,1-二(对甲苯基)乙烷
4-β-羟基胆固醇
MMPP HEXAHYDRATE
氯化铌(V)
Methyl 5-aMinopyriMidine-2-carboxylate hydrochloride
2-AMINO-3-HYDROXY-2-METHYL-3-(4-NITRO-PHENYL)-PROPIONIC ACID
3-AMINO-2-HYDROXY-4-PHENYLBUTYRIC ACID
异乌药内酯
Benzoic acid, 3-aMino-5-b...
1,1-二(对甲苯基)乙烷
4-β-羟基胆固醇
MMPP HEXAHYDRATE
氯化铌(V)
Methyl 5-aMinopyriMidine-2-carboxylate hydrochloride