DDC-01-163
Based on 1 Customer Validation
DDC-01-163 is an allosteric PROTAC degrader targeting EGFR. DDC-01-163 is dependent on the ubiquitin–proteasome system. DDC-01-163 can selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells. DDC-01-163 is effective against Osimertinib (HY-15772)-resistant cells with L/T/C797S and L/T/L718Q EGFR mutations. DDC-01-163 exhibits enhanced anti-proliferative activity against L858R/T790M EGFR-Ba/F3 cells when combined with the ATP-site EGFR inhibitor Osimertinib. DDC-01-163 can be used for the study of non-small cell lung cancer.
(Pink: EGFR ligand (HY-151048); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W008005)).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.05%
- CAS. Nr.: 2140806-84-2
- Formel: C49H51N9O9S
- Molecular Weight:942.05
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Alle PROTACs Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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EGFRL858R/T790M |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | EC50 |
<500 nM
Compound: Example I-22
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Protac activity at native cereblon/EGFR T790M/L858R mutant (unknown origin) transfected in mouse Baf3 cells assessed as reduction in cell proliferation by MTS assay
Protac activity at native cereblon/EGFR T790M/L858R mutant (unknown origin) transfected in mouse Baf3 cells assessed as reduction in cell proliferation by MTS assay
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[PMID: 31413790] |
| BaF3 | IC50 |
28 nM
Compound: Fig 1, Cpd 7
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Antiproliferative activity against mouse BaF3 harbouring EGFR L858R/T790M/L718Q mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
Antiproliferative activity against mouse BaF3 harbouring EGFR L858R/T790M/L718Q mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
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[PMID: 35691176] |
| BaF3 | IC50 |
41 nM
Compound: 5
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Antiproliferative activity against human mouse BaF3 expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell proliferation
Antiproliferative activity against human mouse BaF3 expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell proliferation
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[PMID: 35254067] |
| BaF3 | IC50 |
41 nM
Compound: Fig 1, Cpd 7
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Antiproliferative activity against mouse BaF3 harbouring EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
Antiproliferative activity against mouse BaF3 harbouring EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
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[PMID: 35691176] |
| BaF3 | IC50 |
50 nM
Compound: Fig 1, Cpd 7
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Antiproliferative activity against mouse BaF3 harbouring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
Antiproliferative activity against mouse BaF3 harbouring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
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[PMID: 35691176] |
| BaF3 | IC50 |
96 nM
Compound: 14
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Antiproliferative activity against mouse BaF3 cells transfected with EGFR L8585R/T790M mutant assessed as inhibition of cell growth
Antiproliferative activity against mouse BaF3 cells transfected with EGFR L8585R/T790M mutant assessed as inhibition of cell growth
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[PMID: 35728507] |
| BaF3 | IC50 |
96 nM
Compound: 5
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Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation
Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation
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[PMID: 35254067] |
| BaF3 | IC50 |
96 nM
Compound: DDC-01-163
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Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition incubated for 72 hrs
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition incubated for 72 hrs
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[PMID: 36274273] |
DDC-01-163 exhibits an IC50 value of 45 nM against EGFR L858R/T790M[1].
DDC-01-163 (72 h) shows an IC50 value of 45 at 72 h against EGFR L858R/T790M, and exhibits an EC50 of 0.096 μM against L858R/T790M mutant Ba/F3 cells, while the EC50 against wild-type EGFR Ba/F3 cells was >10 μM[1].
DDC-01-163 (5 h) bound CRBN more effectively than JBJ-07-038 in BRD4BD2 cells[1].
DDC-01-163 (0.01-1 μM, 6-48 h) induces dose- and time-dependent EGFR degradation in Ba/F3 L858R/T790M cells, with maximum degradation occurring at 24 hours. A hook effect was observed at higher concentrations, while no degradation was observed in wild-type Ba/F3 cells[1].
DDC-01-163 (0.1-1 μM, 0-72 h) induces time-dependent EGFR degradation in H1975 cells, with maximum degradation occurring between 24 and 48 hours[1].
DDC-01-163 (0.1 μM, 72 h), when combined with Osimertinib, enhances the anti-proliferative activity and EGFR phosphorylation inhibition in L858R/T790M Ba/F3 cells, whereas high-dose Osimertinib (0.1 μM) exerted an antagonistic effect[1].
DDC-01-163 (72 h) effectively inhibits the proliferation of Ba/F3 cells stably transfected with L858R/T790M/C797S (EC50 = 0.041 μM) or L858R/T790M/L718Q EGFR (EC50 = 0.028 μM) mutations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:L858R/T790M Ba/F3 cells
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Concentration:0.01 μM, 0.1 μM, 1 μM
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Incubation Time:6 h, 24 h, 48 h
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Result:In L858R/T790M mutant Ba/F3 cells, dose- and time-dependent EGFR degradation was induced, with maximum degradation (59-62%) occurring at 24 hours and persisting until 48 hours. A hook effect (degradation decreased) was observed at higher concentrations (1 μM).
Chemical Information
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CAS. Nr. 2140806-84-2
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Appearance Solid
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Molecular Weight 942.05
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Formel C49H51N9O9S
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Color Light yellow to yellow
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SMILES
O=C1NC(C(CC1)N2C(C3=C(C2=O)C(NCCOCCOCCOCCN4CCN(CC4)C5=CC=C(C6=CC=C7C(C(N(C(C8=CC=CC=C8)C(NC9=NC=CS9)=O)C7)=O)=C6)C=N5)=CC=C3)=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (53.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
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- Korean - KR (251 KB)
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Handling Instructions (2659 KB)
Verweise
[2]. Jaebong Jang, et al. Mutant-Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug-Resistant Mutations. Angew Chem Int Ed Engl. 2020 Aug 17;59(34):14481-14489. [Content Brief]
[3]. Surya Kant Tripathi, et al. Allosteric mutant-selective fourth-generation EGFR inhibitors as an efficient combination therapeutic in the treatment of non-small cell lung carcinoma. Drug Discov Today. 2021 Jun;26(6):1466-1472. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.0615 mL | 5.3076 mL | 10.6151 mL | 26.5379 mL |
| 5 mM | 0.2123 mL | 1.0615 mL | 2.1230 mL | 5.3076 mL | |
| 10 mM | 0.1062 mL | 0.5308 mL | 1.0615 mL | 2.6538 mL | |
| 15 mM | 0.0708 mL | 0.3538 mL | 0.7077 mL | 1.7692 mL | |
| 20 mM | 0.0531 mL | 0.2654 mL | 0.5308 mL | 1.3269 mL | |
| 25 mM | 0.0425 mL | 0.2123 mL | 0.4246 mL | 1.0615 mL | |
| 30 mM | 0.0354 mL | 0.1769 mL | 0.3538 mL | 0.8846 mL | |
| 40 mM | 0.0265 mL | 0.1327 mL | 0.2654 mL | 0.6634 mL | |
| 50 mM | 0.0212 mL | 0.1062 mL | 0.2123 mL | 0.5308 mL |
DDC-01-163 Related Classifications
HY-139997 Related Classifications
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