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.
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).
|
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. Further protocols information, click here.
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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.
Protocols
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EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
The EdU incorporation assay measures DNA synthesis by adding the thymidine analog 5-ethynyl-2′-deoxyuridine to cells or tissues, where it is incorporated into newly synthesized DNA during S phase. Incorporated EdU is detected by copper-catalyzed azide-alkyne cycloaddition, in which a fluorescent azide covalently reacts with the ethynyl group on EdU, allowing S-phase cells to be detected by fluorescence microscopy, flow cytometry, or high-content imaging. EdU detection does not require DNA denaturation or anti-BrdU antibody access, which preserves sample structure and improves compatibility with immunostaining and multiparameter cytometry compared with BrdU-based detection. EdU can be cytotoxic in a cell-type- and exposure-dependent manner, so pulse duration, concentration, and continuous-labeling designs should be validated for each cell type.
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Flow cytometric DNA-content cell-cycle staining
Flow cytometric DNA-content cell-cycle staining measures the fluorescence intensity of DNA-bound fluorochromes in single cells or nuclei to estimate DNA content distributions, allowing assignment of populations to G0/G1, S, and G2/M phases by DNA histogram deconvolution. Propidium iodide (PI) intercalates into DNA, and PI fluorescence is proportional to cellular DNA content when staining is performed under conditions that make DNA accessible and minimize non-DNA signal. Cells with G2/M DNA content are expected to show approximately twice the fluorescence intensity of G0/G1 cells, while S-phase cells occupy intermediate fluorescence values. PI-based DNA-content analysis can also detect cells with fractional DNA content, often reported as sub-G1, when DNA fragmentation and extraction during staining reduce retained DNA signal in apoptotic cells. DAPI is an alternative DNA fluorochrome for univariate DNA-content analysis, while bivariate approaches combining DNA content with proliferation
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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BrdU Incorporation Assay
Bromodeoxyuridine (BrdU) incorporation assay is based on the principle that BrdU, a thymidine analog, is incorporated into newly synthesized DNA during the S phase of the cell cycle, thereby serving as a marker of DNA replication and cellular proliferation. Incorporated BrdU can be detected using anti-BrdU antibodies following DNA denaturation, enabling visualization or quantification of proliferating cells through immunochemical detection methods such as immunofluorescence or immunohistochemistry.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)