2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs VEGFR
  4. VEGFR-2-IN-39

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.

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VEGFR-2-IN-39 Chemical Structure

VEGFR-2-IN-39 Chemical Structure

CAS No. : 2353417-86-2

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Based on 1 publication(s) in Google Scholar

VEGFR-2-IN-39 Related Antibodies

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Description

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[1].

IC50 & Target

VEGFR2

 

Cellular Effect
Cell Line Type Value Description References
EA.hy 926 IC50
38.65 μM
Compound: PROTAC-5
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
[PMID: 32750566]
In Vitro

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.

VEGFR-2-IN-39 Related Antibodies

Western Blot Analysis[1]

Cell Line: HUVECs
Concentration: 0-60 μM
Incubation Time: 0-72 h
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.

Cell Cycle Analysis[1]

Cell Line: HUVECs
Concentration: 10-40 μM
Incubation Time: 0-72 h
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.

Apoptosis Analysis[1]

Cell Line: HUVECs
Concentration: 0.1-40 μM
Incubation Time: 0-72 h
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%
Molecular Weight

1000.23

Formula

C55H66FN9O6S
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9998 mL 4.9989 mL 9.9977 mL
5 mM 0.2000 mL 0.9998 mL 1.9995 mL
View the 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.

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Purity & Documentation
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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VEGFR-2-IN-39 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VEGFR-2-IN-392353417-86-2PROTACsVEGFRVascular endothelial growth factor receptorVEGFR-2PROTACinhibitorHUVECsInhibitorinhibit

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