PROTAC VEGFR-2 degrader-3
Based on 1 Customer Validation
VEGFR-2-IN-39 (PROTAC-5) is a PROTAC targeting VEGFR-2 (IC50: 208.6 nM). VEGFR-2-IN-39 has low toxicity.VEGFR-2-IN-39 inhibits the proliferation of EA.hy926, one of HUVECs, in a concentration-dependent manner, with an IC50 of 38.65 µM.
For research use only. We do not sell to patients.
- Purity: 99.09%
- CAS No.: 2353417-86-2
- Formula: C55H66FN9O6S
- Molecular Weight:1000.23
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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VEGFR2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| EA.hy 926 | IC50 |
38.65 μM
Compound: PROTAC-5
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Antiangiogenic activity in human EA.hy 926 cells measured after 24 hrs by MTT assay
Antiangiogenic activity in human EA.hy 926 cells measured after 24 hrs by MTT assay
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[PMID: 32750566] |
VEGFR-2-IN-39 (0-60 μM; 0-72 h) can efficiently reduce the protein levels of VEGFR-2 in a dose-dependent manner[1].
VEGFR-2-IN-39 (10-40 μM; 72 h) prolongs the S phase of the cell cycle in HUVECs[1].
VEGFR-2-IN-39 (0.1-40 μM; 72 h) induces apoptosis in HUVECs in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HUVECs
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Concentration:0-60 μM
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Incubation Time:0-72 h
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Result:VEGFR-2 levels by up to 60% at a concentration of 40 μmol/L, with rapid degradation visible as early as 24 hours and nearly complete by 48 hours.
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Cell Line:HUVECs
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Concentration:10-40 μM
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Incubation Time:0-72 h
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Result:Resulted in a significant increase in the proportion of cells in the S phase, indicating a halt or delay in the progression of the cell cycle. Correspondingly, there was a notable reduction in the number of cells in the G1 phase.
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Cell Line:HUVECs
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Concentration:0.1-40 μM
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Incubation Time:0-72 h
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Result:Resulted in a significant dose-dependent increase in the percentage of apoptotic cells. The percentage of late apoptotic cells increased as follows:
control (untreated) : 5.34%
10 μM: 6.94%
20 μM: 8.32%
30 μM: 15.6%
40 μM: 48.7%
Chemical Information
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CAS No. 2353417-86-2
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Appearance Solid
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Molecular Weight 1000.23
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Formula C55H66FN9O6S
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Color White to off-white
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SMILES
NC1=NN(C(CCCCCCCCCCC(N[C@@H](C(C)(C)C)C(N2[C@@H](C[C@H](C2)O)C(NCC3=CC=C(C4=C(N=CS4)C)C=C3)=O)=O)=O)=O)C5=CC=CC(C6=CC=C(C=C6)NC(NC7=C(C=CC(C)=C7)F)=O)=C15
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 200 mg/mL (199.95 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 (protect from light). 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 (protect from light). 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 (protect from light). 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 | 0.9998 mL | 4.9989 mL | 9.9977 mL | 24.9943 mL |
| 5 mM | 0.2000 mL | 0.9998 mL | 1.9995 mL | 4.9989 mL | |
| 10 mM | 0.1000 mL | 0.4999 mL | 0.9998 mL | 2.4994 mL | |
| 15 mM | 0.0667 mL | 0.3333 mL | 0.6665 mL | 1.6663 mL | |
| 20 mM | 0.0500 mL | 0.2499 mL | 0.4999 mL | 1.2497 mL | |
| 25 mM | 0.0400 mL | 0.2000 mL | 0.3999 mL | 0.9998 mL | |
| 30 mM | 0.0333 mL | 0.1666 mL | 0.3333 mL | 0.8331 mL | |
| 40 mM | 0.0250 mL | 0.1250 mL | 0.2499 mL | 0.6249 mL | |
| 50 mM | 0.0200 mL | 0.1000 mL | 0.2000 mL | 0.4999 mL | |
| 60 mM | 0.0167 mL | 0.0833 mL | 0.1666 mL | 0.4166 mL | |
| 80 mM | 0.0125 mL | 0.0625 mL | 0.1250 mL | 0.3124 mL | |
| 100 mM | 0.0100 mL | 0.0500 mL | 0.1000 mL | 0.2499 mL |
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