SA-PA
SA-PA is an intracellular self-assembling CRBN-recruiting PROTAC composed of an alkynylated Sorafenib precursor (SA) and an azidated Pomalidomide precursor (PA). SA-PA promotes the ubiquitination and proteasomal degradation of VEGFR-2, EphB4, and PDGFR-β, and exhibits inhibitory activity against U87 and A549 cell proliferation. SA-PA is used in cancer-related research, such as glioblastoma and non-small cell lung cancer.
(Pink: ligand (HY-10201); Blue: Cereblon ligand (HY-10984); Black: linker).
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- CAS. Nr.: 3058085-76-7
- Formel: C40H32ClF3N10O8
- Molecular Weight:873.19
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
VEGFR-2 |
EPHB4 |
PDGFR-β |
In Vitro
SA (0.016-10 μM; 48 h) and PA (0.016-10 μM; 48 h) promote the degradation of VEGFR-2, EphB4, and PDGFR-β proteins in U87 cells; treatment with PA (10 μM) alone also induces the degradation of these target proteins in U87 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- MTT Cell Proliferation Assay
Chemical Information
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CAS. Nr. 3058085-76-7
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Molecular Weight 873.19
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Formel C40H32ClF3N10O8
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SMILES
O=C(NCC1=CN(CCCC(NC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
SA-PA Related Classifications
HY-155684 Related Classifications
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Keywords
- SA-PA
- 3058085-76-7
- PROTACs
- VEGFR
- Ephrin Receptor
- PDGFR
- copper-catalyzed azide-alkyne cycloaddition
- cell-free reaction conditions
- proteolysis targeting chimera
- bioorthogonal copper-catalyzed azide-alkyne cycloaddition
- pomalidomide-derived azide-containing precursor
- sorafenib-derived alkyne-containing precursor
- PROTAC
- Inhibitor
- inhibitor
- inhibit