SPP-037
SPP-037 is an orally active and selective inhibitor of ST6GAL1 (IC50 = 3.59 μM). SPP-037 inhibits integrin α2,6-sialylation and integrin-FAK-paxillin pathway. SPP-037 inhibits cancer cell proliferation, migration and exhibits antiangiogenic activity. SPP-037 has anti-tumor activity in MDA-MB-231 xenograft mouse model. SPP-037 can be used for the research of triple-negative breast cancer.
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- Formule: C36H50ClN3O9S
- Masse moléculaire:736.31
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Stockage:
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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Activité biologique
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Chemical Information
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Activité biologique
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ST6GAL1 3.59 μM (IC50) |
SPP-037 potently and selectively inhibits ST6GAL1 (IC50 = 3.59 ± 0.09 μM) and weaker inhibition of ST3GAL3 (IC50 = 14 μM)[1].
SPP-037 (20-80 μM; 48 h) reduces the viability of MDA-MB-231 triple-negative breast cancer cells in a dose-dependent manner[1].
SPP-037 (10-20 μM; 16 h) inhibits the migration of MDA-MB-231 triple-negative breast cancer cells[1].
SPP-037 (5-10 μM; 18 h) inhibits tube formation by HUVECs[1].
SPP-037 (5-20 μM) dose-dependently decreases α2,6-sialylation of integrins β1, β3, and β4 in MDA-MB-231 triple-negative breast cancer cells[1].
SPP-037 (10-20 μM; 2 h) dose-dependently inhibits phosphorylation of FAKTyr397, Tyr576/577 and paxillinTyr118 in MDA-MB-231 triple-negative breast cancer cells at 10, 15, and 20 μM, with effects visible within 2 h, without changing total protein levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 triple-negative breast cancer cells
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Concentration:0.5, 1, 5, 10, 20, 40, 80 μM
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Incubation Time:48 h
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Result:Exhibits cytotoxicity in MDA-MB-231 cells, with >50% cell death observed at 40 and 80 μM.
Showed low cytotoxicity at 0.5-10 μM.
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Cell Line:MDA-MB-231 triple-negative breast cancer cells
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Concentration:10, 15, 20 μM
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Incubation Time:2 h
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Result:Dose-dependently inhibits phosphorylation of FAK (Tyr397, Tyr576/577) and paxillin (Tyr118) in MDA-MB-231 cells without altering total FAK or paxillin protein levels.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/cAnN.Cg-Foxn1nu/CrlNarl (female, 4-5 weeks old, breast cancer MDA-
MB-231 xenograft model)[1] -
Dosage:20 mg/kg
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Administration:i.p.; twice weekly; until day 38; p.o.; twice weekly; until day 38
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Result:Achieved 27% tumor growth inhibition (TGI) with intraperitoneal administration by day 38.
Achieved 33% tumor growth inhibition (TGI) with oral administration by day 38.
Significantly delayed the onset of lung metastasis, comparable to Paclitaxel (HY-B0015).
Caused no significant loss in body weight or other overt signs of toxicity.
Chemical Information
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Masse moléculaire 736.31
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Formule C36H50ClN3O9S
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SMILES
[H][C@]12CC[C@@]3([C@H](CC[C@]3([C@@]1(CC[C@@]4(C[C@@H](CC[C@]24C)OC([C@@H](NS(=O)(C5=CC=C(C6=NON=C56)Cl)=O)CC(O)=O)=O)[H])[H])[H])[C@@H](CCCCC(O)=O)C)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SPP-037 Related Classifications
HY-172888 Related Classifications
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