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: VEGFR-2 and EPHB4 and PDGFRβ ligand (HY-10201); Blue: Cereblon ligand (HY-10984); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3058085-76-7
- Formula: C40H32ClF3N10O8
- Molecular Weight:873.19
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
VEGFR-2 |
EPHB4 |
PDGFR-β |
In Vitro
SA-PA exhibits antiproliferative activity against U87 cells (IC50 = 5.684 μM) and A549 cells (IC50 = 1.157 μM); treatment with PA alone shows little to no antiproliferative activity against U87 and A549 cells[1].
SA-PA (2-10 μM; 48 h) promotes the degradation of VEGFR-2, EphB4, and PDGFR-β proteins in U87 cells at a concentration of 10 μM; treatment with PA alone (10 μM) 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.
Chemical Information
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CAS No. 3058085-76-7
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Molecular Weight 873.19
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Formula 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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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-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