CAS No. 2230821-27-7
| IUPAC Name | (2S,4R)-1-[(2S)-2-[3-[2-[5-[4-(3-chloro-4-fluoroanilino)-7-methoxyquinazolin-6-yl]oxypentoxy]ethoxy]propanoylamino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide | |
|---|---|---|
| CAS Number | 2230821-27-7 | |
| Molecular Formula |
C47H57ClFN7O8S
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|
| Molecular Weight (MW) | 934.51 | |
| SMILES | CC1=C(SC=N1)C2=CC=C(C=C2)CNC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)CCOCCOCCCCCOC4=C(C=C5C(=C4)C(=NC=N5)NC6=CC(=C(C=C6)F)Cl)OC)O | |
| InChIKey | NICKHWYZMNLEPJ-TZSMONEZSA-N |
Gefitinib-based PROTAC 3 is a VHL-recruiting proteolysis targeting chimera (PROTAC) that targets epidermal growth factor receptor (EGFR) for proteasomal degradation. By linking an EGFR-binding moiety to a VHL ligand, it selectively degrades mutant EGFR variants, including Exon 19 deletion and L858R mutants, in non-small cell lung cancer cells. This targeted degradation impairs downstream receptor tyrosine kinase signaling, leading to inhibition of cancer cell proliferation and survival. [1]
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Concentration
Volume
Mass
|
|---|
| Solvent | Solubility & Note |
|---|---|
| DMSO |
100 mg/mL
(107.0 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.) |
| Ethanol | 100 mg/mL |
| Water | Insoluble |
| DMSO |
100 mg/mL
(107.0 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.) |
| Ethanol | 100 mg/mL |
| Water | Insoluble |
| DMSO |
100 mg/mL
(107.0 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.) |
| Ethanol | 12 mg/mL |
| Water | Insoluble |
- Preheat media/saline to 37°C.
- Mix rapidly (pipette/vortex) upon addition.
- For complex mixes, always add the aqueous phase last.
- Re-dissolve minor precipitates with a 37°C water bath and sonication (≤30 min).
Pre-aliquoted for Longevity: Solid-state aliquots offer significantly longer shelf life compared to stock solutions, ensuring maximum stability for every use.
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- Gefitinib-based PROTAC 3 Clinical Trials
- Gefitinib-based PROTAC 3 Solubility in DMSO
- Gefitinib-based PROTAC 3 Stock Solution
- Gefitinib-based PROTAC 3 Storage
- Gefitinib-based PROTAC 3 Stability
- Gefitinib-based PROTAC 3 Molecular Weight
- Gefitinib-based PROTAC 3 SMILES
- Gefitinib-based PROTAC 3 Chemical Structure (2D and 3D)
- Gefitinib-based PROTAC 3 SDS｜MSDS