ANTXR1-IN-1
ANTXR1-IN-1 is a ANTXR1 inhibitor with a Ka of 2.88 μM for hANTXR1, and exhibits anti-tumor cell activity. ANTXR1-IN-1 undergoes acylation with Ser229 of ANTXR1, thereby inhibiting tumor cell proliferation. ANTXR1-IN-1 induces G2/M phase arrest and apoptosis in tumor cells. ANTXR1-IN-1 can be used for research on melanoma, non-small cell lung cancer, hepatocellular carcinoma, and colorectal cancer.
For research use only. We do not sell to patients.
- CAS No.: 2222728-15-4
- Formula: C33H32ClNO5
- Molecular Weight:558.06
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
ANTXR1-IN-1 (Compound 8a) (0.625-10 μM; 24-72 h) potently and selectively inhibits the proliferation of A375, NCI-H460, HepG2, HCT116, and CX-1 tumor cells with IC50 values ranging from 1.91-5.09 μM, while showing minimal cytotoxicity to normal VERO and HEK-293 cells, with anti-tumor activity increasing in a time-dependent manner over 24, 48, and 72 h[1].
ANTXR1-IN-1 (2 μM; 0-24 h) induces G2/M phase arrest in HCT116 cells[1].
ANTXR1-IN-1 (2-10 μM; 3-24 h) promotes concentration-dependent apoptosis in HCT116 cells[1].
ANTXR1-IN-1 (5 μM; 0-120 min) shows moderate stability in human plasma with a half-life of 23.58 min when incubated at 5 μM and 37°C[1].
ANTXR1-IN-1 (20 μM; 8 h) enhances the thermal stability of proteins in HCT116 cell lysates[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human melanoma A375 cells, human non-small cell lung cancer NCI-H460 cells, human hepatoma HepG2 cells, human colorectal cancer HCT116 and CX-1 cells, normal monkey kidney VERO cells, human embryonic kidney HEK-293 cells
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Concentration:0.625-10 μM (tumor cell lines); 0-100 μM (normal cell lines)
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Incubation Time:24, 48, 72 h
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Result:Inhibited proliferation of A375 cells with an IC50 of 1.91 μM.
Exhibited broad-spectrum anti-tumor activity with IC50 values of 4.86 μM in NCI-H460 cells, 5.09 μM in HepG2 cells, 3.80 μM in HCT116 cells, and 4.30 μM in CX-1 cells.
Increased anti-tumor activity progressively over 24, 48, and 72 h in a time-dependent manner across 5 tumor cell lines.
Showed minimal cytotoxicity in normal VERO and HEK-293 cells with CC50 values exceeding 20 μM.
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Cell Line:human colorectal cancer HCT116 cells
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Concentration:2 μM
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Incubation Time:0, 3, 8, 24 h
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Result:Induced G2/M phase arrest in HCT116 cells, with the proportion of cells in G2/M phase increasing from 4% at 0 h to 64% at 24 h.
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Cell Line:human colorectal cancer HCT116 cells
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Concentration:2-10 μM
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Incubation Time:3, 8, 24 h
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Result:Induced marked early and late apoptosis in HCT116 cells.
Contributed to apoptotic rates ranging from 44.57% to 60.67% in a concentration-dependent manner when tested alongside compounds 7d and 8b.
Chemical Information
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CAS No. 2222728-15-4
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Molecular Weight 558.06
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Formula C33H32ClNO5
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SMILES
O=C(CC1(C[C@H]2C3)C[C@H]3C[C@H](C2)C1)OC4=C(OC)C=CC5=C4C=[N+](CC6)C7=C5C=CC8=C7C6=CC9=C8OCO9.[Cl-]
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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)
ANTXR1-IN-1 Related Classifications
HY-183806 Related Classifications
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