SA-VA
SA-VA is a heterobifunctional PROTAC molecule generated in situ via click chemistry, and acts as a degrader for VEGFR-2 and EphB4. SA-VA is self-assembled from the alkynyl precursor SA and the azide precursor VA through a copper ion-mediated intracellular click chemistry reaction, recruits the E3 ubiquitin ligase VHL to mediate the ubiquitination of target proteins, and triggers degradation via the proteasome pathway. SA-VA induces cell cycle arrest and apoptosis in U87 glioma cells. SA-VA can be used in cancer-related research.
(Pink: VEGFR and Ephrin Receptor Target protein ligand; Blue: VHL ligand (HY-125845); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3058085-77-8
- Formula: C50H53ClF3N11O7S
- Molecular Weight:1044.54
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
VEGFR-2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
1.060 μM
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SA + VA exhibits anti-proliferative activity against U87 cells (IC50 = 16.024 μM) and A549 cells (IC50 = 1.060 μM).
SA + VA exhibits anti-proliferative activity against U87 cells (IC50 = 16.024 μM) and A549 cells (IC50 = 1.060 μM).
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37216813 |
In Vitro
SA‑VA (SA + VA) exhibits anti-proliferative activity against U87 cells (IC50 = 16.024 μM) and A549 cells (IC50 = 1.060 μM)[1].
SA-VA (0-1 μM; 48 h) arrests the cell cycle of U87 cells in the S phase in a concentration-dependent manner[1].
SA‑VA (2 μM; 48 h) significantly induces the degradation of VEGFR‑2 and EphB4 proteins in U87 cells[1].
SA‑VA barely induces the degradation of VEGFR‑2 and EphB4 proteins in A549 cells, and the basal expression level of VEGFR‑2 protein in A549 cells is relatively low[1].
SA-VA (0-20 μM; 48 h) induces apoptosis in U87 cells in a concentration-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:U87, A549 cells
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Concentration:2 μM
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Incubation Time:48 h
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Result:Induced obvious degradation of VEGFR‑2 and EphB4 proteins; hardly induced degradation of VEGFR‑2 and EphB4 proteins, VEGFR‑2 protein level is inherently low in A549 cells.
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Cell Line:U87 cells
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Concentration:0, 0.1, 1 μM
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Incubation Time:48 h
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Result:Arrested cell cycle at S phase in a concentration‑dependent manner.
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Cell Line:U87 cells
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Concentration:0.1, 1, 5, 10, 20 μM
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Incubation Time:48 h
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Result:Induced concentration‑dependent apoptosis.
Chemical Information
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CAS No. 3058085-77-8
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Molecular Weight 1044.54
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Formula C50H53ClF3N11O7S
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SMILES
O=C(NCC1=CN(CCCCC(N[C@@H](C(C)(C)C)C(N2[C@H](C(NCC3=CC=C(C4=C(C)N=CS4)C=C3)=O)C[C@@H](O)C2)=O)=O)N=N1)C5=NC=CC(OC6=CC=C(NC(NC7=CC=C(Cl)C(C(F)(F)F)=C7)=O)C=C6)=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SA-VA Related Classifications
HY-155685 Related Classifications
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