PROTAC EGFR degrader 11
Based on 1 Customer Validation
PROTAC EGFR degrader 11 (Compound B71) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC50 <100 nM. PROTAC EGFR degrader 11 binds CRBN-DDB1 with a Ki of 36 nM. PROTAC EGFR degrader 11 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC50 <100 nM.
For research use only. We do not sell to patients.
- Purity : 99.20%
- CAS No.: 3034244-71-5
- Formula: C49H64ClFN10O7S
- Molecular Weight:991.61
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Description
IC50 & Target
|
CRBN-DDB1 36 nM (Ki) |
Chemical Information
-
CAS No. 3034244-71-5
-
Appearance Solid
-
Molecular Weight 991.61
-
Formula C49H64ClFN10O7S
-
Color White to off-white
-
SMILES
O=C1C(C2=C(F)C=C(N3CCC(OCCN(CC4)CCN4C(CC5)CCN5C(C(CC)=C6)=CC(OC)=C6NC7=NC=C(Cl)C(NC8=CC=C(OC)C=C8N(S(=O)(C)=O)C)=N7)CC3)C=C2)CCC(N1)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : ≥ 100 mg/mL (100.85 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
-
Data Sheet (270 KB)
-
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)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
References
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 | 1.0085 mL | 5.0423 mL | 10.0846 mL | 25.2115 mL |
| 5 mM | 0.2017 mL | 1.0085 mL | 2.0169 mL | 5.0423 mL | |
| 10 mM | 0.1008 mL | 0.5042 mL | 1.0085 mL | 2.5212 mL | |
| 15 mM | 0.0672 mL | 0.3362 mL | 0.6723 mL | 1.6808 mL | |
| 20 mM | 0.0504 mL | 0.2521 mL | 0.5042 mL | 1.2606 mL | |
| 25 mM | 0.0403 mL | 0.2017 mL | 0.4034 mL | 1.0085 mL | |
| 30 mM | 0.0336 mL | 0.1681 mL | 0.3362 mL | 0.8404 mL | |
| 40 mM | 0.0252 mL | 0.1261 mL | 0.2521 mL | 0.6303 mL | |
| 50 mM | 0.0202 mL | 0.1008 mL | 0.2017 mL | 0.5042 mL | |
| 60 mM | 0.0168 mL | 0.0840 mL | 0.1681 mL | 0.4202 mL | |
| 80 mM | 0.0126 mL | 0.0630 mL | 0.1261 mL | 0.3151 mL | |
| 100 mM | 0.0101 mL | 0.0504 mL | 0.1008 mL | 0.2521 mL |