2. Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK Cytoskeleton
  3. Sialyltransferase Endogenous Metabolite FAK Integrin
  4. 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.

For research use only. We do not sell to patients.

SPP-037

SPP-037 Chemical Structure

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Based on 1 publication(s) in Google Scholar

SPP-037 Related Antibodies

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αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

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Description

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[1].

IC50 & Target[1]

ST6GAL1

3.59 μM (IC50)

In Vitro

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.

SPP-037 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: MDA-MB-231 triple-negative breast cancer cells
Concentration: 0.5, 1, 5, 10, 20, 40, 80 μM
Incubation Time: 48 h
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.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 triple-negative breast cancer cells
Concentration: 10, 15, 20 μM
Incubation Time: 2 h
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.
In Vivo

SPP-037 (20 mg/kg; i.p. or p.o.; twice weekly; until day 38) delivers significant antitumor efficacy, with 27% tumor growth inhibition via intraperitoneal administration and 33% inhibition via oral administration, while also delaying lung metastasis in a breast cancer xenograft mouse model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/cAnN.Cg-Foxn1nu/CrlNarl (female, 4-5 weeks old, breast cancer MDA-
MB-231 xenograft model)[1]
Dosage: 20 mg/kg
Administration: i.p.; twice weekly; until day 38; p.o.; twice weekly; until day 38
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.
Molecular Weight

736.31

Formula

C36H50ClN3O9S
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SPP-037 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SPP-037SPP037SPP 037SialyltransferaseEndogenous MetaboliteFAKIntegrinPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseST6GAL1focal adhesion kinase (FAK)HUVECsxenograft mouse modelST3GAL1paxillinMDA-MB-231triple-negative breast cancerST3GAL3integrin α2,6-sialylationInhibitorinhibitorinhibit

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