2. Apoptosis
  3. Apoptosis
  4. 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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Antitumor agent-96

Antitumor agent-96 Chemical Structure

CAS No. : 3041063-90-2

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Antitumor agent-96 Related Antibodies

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Description

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[1].

IC50 & Target

MRE11[1]
Cellular Effect
Cell Line Type Value Description References
L02 IC50
25.6 μM
Compound: D34
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
[PMID: 36868105]
In Vitro

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.

Antitumor agent-96 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: CM-AS16, CRMM2 , CM2005.1, CRMM1, HL7702 and PIG1
Concentration:
Incubation Time: 72 h
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.

Apoptosis Analysis[1]

Cell Line: CRMM1 cells
Concentration: 0.1, 0.3, 1, 3 and 10 μM
Incubation Time: 48 h
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.

Cell Migration Assay [1]

Cell Line: CRMM1 cells
Concentration: 0.3 μM
Incubation Time: 0, 24, 48 and 72 h
Result: Inhibited migration rate from 70% to 45% at 72 h.

Western Blot Analysis[1]

Cell Line: CRMM1 and CRMM2
Concentration: 0.3, 1, 3 and 10 μM
Incubation Time: 48 h
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.
In Vivo

Antitumor agent-96 dihydrochloride (Compound D34 dihydrochloride; 10 and 20 mg/kg; i.p.; five times per week for 28 days) shows anti-tumor effect in mice[1].

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

Animal Model: NCG mice, CRMM1 xenograft tumor model[1]
Dosage: 10 mg/kg and 20 mg/kg
Administration: Intraperitoneal injection, five times per week for 28 days
Result: Suppressed tumor growth. Did not induce any conspicuous body weight loss.
Molecular Weight

416.56

Formula

C27H32N2O2
CAS No.
SMILES

O=C(C1=C2C=CC=CC2=CC=C1OCCCN3CCNCC3)CCCC4=CC=CC=C4
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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Antitumor agent-96 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:

Antitumor agent-963041063-90-2Antitumor agent96Antitumor agent 96ApoptosisCM-AS16CRMM2 CM2005.1CRMM1MRE11RAD50NBS1γ-H2AXInhibitorinhibitorinhibit

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