Antitumor agent-96
Antitumor agent-96 (Compound D34) is a potent MRE11 inhibitor. Antitumor agent-96 down-regulates the HR pathway by binding with MRE11 and suppressing its endonuclease functions. Antitumor agent-96 induces CM cells apoptosis.
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- CAS. Nr.: 3041063-90-2
- Formel: C27H32N2O2
- Molecular Weight:416.56
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
MRE11[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L02 | IC50 |
25.6 μM
Compound: D34
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Antiproliferative activity against human HL7702 cells cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human HL7702 cells cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
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[PMID: 36868105] |
Antitumor agent-96 (Compound D34; 72 h) has a particular cytotoxicity selectivity in CM cells of CM-AS16 (IC50 = 2.9±0.1 μM), CRMM2 (IC50 = 0.7 ± 0.0 μM), CM2005.1 (IC50 = 1.0 ± 0.1 μM), and CRMM1 (IC50 = 1.3 ± 0.3 μM), compared to ocular melanoma, cutaneous melanoma and normal cells[1].
Antitumor agent-96 (0.1-10 μM; 48 h) induces CRMM1 cell apoptosis[1].
Antitumor agent-96 (0.3 μM; 0-72 h) inhibits CRMM1 cell migration[1].
Antitumor agent-96 (0.3-10 μM; 48 h) augments DNA damage accumulation in CM cells and down-regulates MRN complex in HR pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CM-AS16, CRMM2 , CM2005.1, CRMM1, HL7702 and PIG1
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Concentration:
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Incubation Time:72 h
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Result:Inhibited proliferation with IC50s of 2.9 ± 0.1, 0.7 ± 0.0, 1.0 ± 0.1, 1.3 ± 0.3, 25.6 ± 0.8 and 32.9 ± 0.3 μM against CM-AS16, CRMM2, CM2005.1, CRMM1, HL7702 and PIG1, respectively.
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Cell Line:CRMM1 cells
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Concentration:0.1, 0.3, 1, 3 and 10 μM
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Incubation Time:48 h
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Result:Significantly led to CRMM1 cells death over the concentrations of 0.3 μM. The apoptotic rates rose to 80% when incubated at 3 μM.
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Cell Line:CRMM1 cells
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Concentration:0.3 μM
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Incubation Time:0, 24, 48 and 72 h
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Result:Inhibited migration rate from 70% to 45% at 72 h.
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Cell Line:CRMM1 and CRMM2
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Concentration:0.3, 1, 3 and 10 μM
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Incubation Time:48 h
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Result:Stimulated tumor suppressor p53. Induced significant accumulation of γ-H2AX. The three MRN subunits MRE11, RAD50, and NBS1, were significantly down-regulated in a dose-dependent manner. The expression of MRN downstream effectors, including BCRA1 and RAD51, were also inhibited in both CRMM1 and CRMM2 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NCG mice, CRMM1 xenograft tumor model[1]
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Dosage:10 mg/kg and 20 mg/kg
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Administration:Intraperitoneal injection, five times per week for 28 days
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Result:Suppressed tumor growth. Did not induce any conspicuous body weight loss.
Chemical Information
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CAS. Nr. 3041063-90-2
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Molecular Weight 416.56
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Formel C27H32N2O2
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SMILES
O=C(C1=C2C=CC=CC2=CC=C1OCCCN3CCNCC3)CCCC4=CC=CC=C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Antitumor agent-96 Related Classifications
HY-149972 Related Classifications
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