PROTAC BCR-ABL1 ligand 1
Based on 1 Customer Validation
PROTAC BCR-ABL1 ligand 1, compound GMB-475, is the ligand of PROTAC that allosterically targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel-Lindau, resulting in ubiquitination and subsequent degradation of BCR-ABL1.
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- Purity: 99.17%
- CAS No.: 2489876-34-6
- 화학식: C17H12F3N3O2
- 분자량:347.29
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
GMB-475 (0-10 μM) exhibits cell proferation with IC50 values of 1.11,1.98,0.37 μM for BCR-ABL1 WT, T315I, G250E cells, respectively[1]. GMB-475 (0-30 μM) induces the degradation of BCR-ABL1 and c-ABL1 with concomitant inhibition of downstream signaling via the STAT5 pathway, in a dose- and time-dependent fashion in the context of both K562 and Ba/F3 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562 and Ba/F3 cells
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Concentration:0-30 μM
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Incubation Time:
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Result:Decreased p-STAT5 expression.
Chemical Information
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CAS No. 2489876-34-6
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Appearance Solid
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분자량 347.29
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화학식 C17H12F3N3O2
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Color Light brown to gray
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SMILES
OC1=CC=C(C2=NC=NC(NC3=CC=C(OC(F)(F)F)C=C3)=C2)C=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 125 mg/mL (359.93 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
순도&문서
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Data Sheet (271 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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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 | 2.8794 mL | 14.3972 mL | 28.7944 mL | 71.9859 mL |
| 5 mM | 0.5759 mL | 2.8794 mL | 5.7589 mL | 14.3972 mL | |
| 10 mM | 0.2879 mL | 1.4397 mL | 2.8794 mL | 7.1986 mL | |
| 15 mM | 0.1920 mL | 0.9598 mL | 1.9196 mL | 4.7991 mL | |
| 20 mM | 0.1440 mL | 0.7199 mL | 1.4397 mL | 3.5993 mL | |
| 25 mM | 0.1152 mL | 0.5759 mL | 1.1518 mL | 2.8794 mL | |
| 30 mM | 0.0960 mL | 0.4799 mL | 0.9598 mL | 2.3995 mL | |
| 40 mM | 0.0720 mL | 0.3599 mL | 0.7199 mL | 1.7996 mL | |
| 50 mM | 0.0576 mL | 0.2879 mL | 0.5759 mL | 1.4397 mL | |
| 60 mM | 0.0480 mL | 0.2400 mL | 0.4799 mL | 1.1998 mL | |
| 80 mM | 0.0360 mL | 0.1800 mL | 0.3599 mL | 0.8998 mL | |
| 100 mM | 0.0288 mL | 0.1440 mL | 0.2879 mL | 0.7199 mL |