2. Disease Areas
  3. Cancer Respiratory Disease Digestive System Disease
  4. Lung Cancer Respiratory Cancer Colorectal Cancer Digestive System Cancer
  5. Non-Small Cell Lung Cancer
  6. 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.

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ANTXR1-IN-1

ANTXR1-IN-1 Chemical Structure

CAS No. : 2222728-15-4

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ANTXR1-IN-1 Related Antibodies

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Description

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[1].

In Vitro

ANTXR1-IN-1 (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.

ANTXR1-IN-1 Related Antibodies

Cell Proliferation Assay[1]

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
Concentration: 0.625-10 μM (tumor cell lines); 0-100 μM (normal cell lines)
Incubation Time: 24, 48, 72 h
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.

Cell Cycle Analysis[1]

Cell Line: human colorectal cancer HCT116 cells
Concentration: 2 μM
Incubation Time: 0, 3, 8, 24 h
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.

Apoptosis Analysis[1]

Cell Line: human colorectal cancer HCT116 cells
Concentration: 2-10 μM
Incubation Time: 3, 8, 24 h
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.
Molecular Weight

558.06

Formula

C33H32ClNO5
CAS No.
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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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ANTXR1-IN-1 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:

ANTXR1-IN-12222728-15-4Othersmelanomacolorectal cancerhepatocellular carcinomanon-small cell lung cancerNCI-H460Ser229HCT116HepG2A375ANTXR1Inhibitorinhibitorinhibit

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