MYC-IN-4
MYC-IN-4 is a MYC inhibitor. MYC-IN-4 impairs MYC/MAX protein-protein interaction (IC50 = 3.06 μM). MYC-IN-4 inhibits MYC-aberrant PC-3 prostate cancer cells with an IC50 of 0.440 μM. MYC-IN-4 demonstrates potent antitumor efficacy in FVB mice bearing Myc-CaP prostate tumor allografts. MYC-IN-4 can be used for the study of prostate cancer.
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- CAS No.: 3109265-41-7
- 화학식: C19H10F6N2O2
- 분자량:412.29
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
MYC-IN-4 (Compound 15) exhibits potent antiproliferative activity against PC-3 cells (MYC-aberrant prostate cancer cells), with an IC50 value of 0.440 μM[1].
MYC-IN-4 (68 h) shows broad-spectrum antiproliferative activity against 14 other neoplastic cell lines, including MDA-MB-231, HCT-116, Myc-CaP, LN-CaP, NCI-H1581, A549, SK-N-BE, SK-OV-3, HepG-2, A-204, A-431, MG-63, LP-1, and MV4-11 cells, with IC50 values ranging from 0.331 μM to 2.60 μM[1].
MYC-IN-4 (10 μM, 1 h) significantly impairs MYC/MAX protein-protein interaction (PPI) in PC-3 cells via Co-IP assay[1].
MYC-IN-4 (0.1-100 μM, 2 h) inhibits MYC/MAX PPI in a cell-free AlphaLISA assay, with an IC50 value of 3.06 μM[1].
MYC-IN-4 (10 μM, 1 h) reduces the thermal stability of endogenous MYC in PC-3 cells[1].
MYC-IN-4 (1-10 μM, 24 h) induces concentration-dependent MYC degradation in PC-3 cells[1].
MYC-IN-4 suppresses MYC transcriptional activity in HEK293T cells transfected with E-box luciferase reporter plasmid, with an IC50 value of 0.739 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Myc-CaP cells (1 × 106 in 100 µL total volume) were subcutaneously implanted into the right flanks of 6-week-old male FVB mice to establish MYC-driven prostate tumor allograft models[1]
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Dosage:10, 30, 50 mg/kg
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Administration:i.p., QOD for 16 days
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Result:Achieved tumor growth inhibition (TGI) rates of 57% and 70% at doses of 30 mg/kg and 50 mg/kg.
Showed no significant changes in body weight.
Reduced the Ki67 expression.
Combined with INCB086550 (HY-134884) increased the infiltration of CD8⁺ T cells and CD45⁺ leukocytes in the tumor microenvironment.
Chemical Information
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CAS No. 3109265-41-7
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분자량 412.29
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화학식 C19H10F6N2O2
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SMILES
OC1=C2C(OC(C3=CC=C(C=C3)C(F)(F)F)=C2)=CC=C1C4=CC(C(F)(F)F)=NN4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)