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Gefitinib-based PROTAC 3
🥰Excellent
Catalog No. T5437Cas No. 2230821-27-7
Gefitinib-based PROTAC 3, which connects an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827 (exon 19 del) and H3255 (L858R mutation) cells, respectively[1].
Gefitinib-based PROTAC 3
🥰Excellent
Purity: 98.25%
Catalog No. T5437Cas No. 2230821-27-7
Gefitinib-based PROTAC 3, which connects an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827 (exon 19 del) and H3255 (L858R mutation) cells, respectively[1].
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $38 | In Stock | |
| 5 mg | $58 | In Stock | |
| 10 mg | $107 | In Stock | |
| 25 mg | $178 | In Stock | |
| 50 mg | $272 | In Stock | |
| 100 mg | $393 | In Stock |
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Purity:98.25%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Gefitinib-based PROTAC 3, which connects an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827 (exon 19 del) and H3255 (L858R mutation) cells, respectively[1]. |
| Targets&IC50 | EGFR:11.7 nM (DC50, HCC827(exon 19 del) cells), EGFR:22.3 nM (DC50, H3255 (L858R mutantion) cells) |
| In vitro | H3255 cells expressing L858R EGFR treated with Gefitinib-based PROTAC 3 (25 nM-10 μM; 24 hours), HCC827 cells expressing exon 19 del EGFR treated with Gefitinib-based PROTAC 3 (100 nM-10 μM; 24 hours), which enables the degradation of both exon-19 deletion EGFR as well as the mutant isoform containing the L858R activating point mutation, while sparing the WT EGFR[1]. |
| Molecular Weight | 934.51 |
| Formula | C47H57ClFN7O8S |
| Cas No. | 2230821-27-7 |
| Smiles | N(C=1C2=C(C=C(OC)C(OCCCCCOCCOCCC(N[C@H](C(=O)N3[C@H](C(NCC4=CC=C(C=C4)C=5SC=NC5C)=O)C[C@@H](O)C3)[C@](C)(C)C)=O)=C2)N=CN1)C6=CC(Cl)=C(F)C=C6 |
| Relative Density. | 1.300 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
| Solubility Information | DMSO: 10 mM | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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