PROTAC BRAF-V600E degrader-1
Based on 1 Customer Validation
PROTAC BRAF-V600E degrader-1 (compound 23) is a potent PROTAC BRAF-V600E degrader whlie no degradation activity against BRAF-WT. PROTAC BRAF-V600E degrader-1 exhibits Kd values of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS) and inhibits the growth of melanoma cells.
(Pink: BRafV600E ligand (HY-107779); Blue: IKZF1 and IKZF3 ligand (HY-10984); Black: linker (HY-124380)).
For research use only. We do not sell to patients.
- Purity: 98.04%
- CAS No.: 2417296-84-3
- Formula: C48H54F2N10O10S
- Molecular Weight:1001.07
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Storage:Powder -20°C, 3 years , 4°C, 2 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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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BRAF-V600E 2 nM (Kd) |
Braf 2.4 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
46.5 nM
Compound: 23
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Cytotoxicity in human A375 cells assessed as reduction in cell viability by Cell-titer-Lumi assay
Cytotoxicity in human A375 cells assessed as reduction in cell viability by Cell-titer-Lumi assay
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[PMID: 32223235] |
| HT-29 | IC50 |
51 nM
Compound: 23
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Cytotoxicity in human HT-29 cells assessed as reduction in cell viability by Cell-titer-Lumi assay
Cytotoxicity in human HT-29 cells assessed as reduction in cell viability by Cell-titer-Lumi assay
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[PMID: 32223235] |
PROTAC BRAF-V600E degrader-1 (compound 23) (1 nM-10 μM; 72 h) inhibits the cell viability of A375 and HT-29[1].
PROTAC BRAF-V600E degrader-1 (1-1000 nM; 16 h or 0-24 h) inhibits p-ERK and BRAF-V600E protein in A375 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A375 and HT-29
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Concentration:1 nM-10 μM
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Incubation Time:72 h
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Result:Inhibited the cell viability of A375 and HT-29 with IC50s of 46.5 nM and 51 nM.
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Cell Line:A375
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Concentration:1, 4, 12, 37, 111, 333 and 1000 nM
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Incubation Time:16 h or 0-24 h
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Result:Induced the reduction in the phosphorylation of ERK.
Inhibited p-ERK and BRAF-V600E in a dose- and time-dependent manner.
Chemical Information
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CAS No. 2417296-84-3
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Appearance Solid
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Molecular Weight 1001.07
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Formula C48H54F2N10O10S
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Color Light yellow to yellow
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SMILES
CCCS(=O)(NC1=CC=C(F)C(N2C=C(C3=CN=CN=C3)C4=NC(N(C5CCN(C(CCOCCOCCOCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O)CC5)C)=CC=C42)=C1F)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 170 mg/mL (169.82 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)
Purity & Documentation
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Data Sheet (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 0.9989 mL | 4.9947 mL | 9.9893 mL | 24.9733 mL |
| 5 mM | 0.1998 mL | 0.9989 mL | 1.9979 mL | 4.9947 mL | |
| 10 mM | 0.0999 mL | 0.4995 mL | 0.9989 mL | 2.4973 mL | |
| 15 mM | 0.0666 mL | 0.3330 mL | 0.6660 mL | 1.6649 mL | |
| 20 mM | 0.0499 mL | 0.2497 mL | 0.4995 mL | 1.2487 mL | |
| 25 mM | 0.0400 mL | 0.1998 mL | 0.3996 mL | 0.9989 mL | |
| 30 mM | 0.0333 mL | 0.1665 mL | 0.3330 mL | 0.8324 mL | |
| 40 mM | 0.0250 mL | 0.1249 mL | 0.2497 mL | 0.6243 mL | |
| 50 mM | 0.0200 mL | 0.0999 mL | 0.1998 mL | 0.4995 mL | |
| 60 mM | 0.0166 mL | 0.0832 mL | 0.1665 mL | 0.4162 mL | |
| 80 mM | 0.0125 mL | 0.0624 mL | 0.1249 mL | 0.3122 mL | |
| 100 mM | 0.0100 mL | 0.0499 mL | 0.0999 mL | 0.2497 mL |
PROTAC BRAF-V600E degrader-1 Related Classifications
HY-137487 Related Classifications
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