TopBP1-IN-5
TopBP1-IN-5 is a TopBP1-BRCT7/8 inhibitor (IC50=2.47-3.8 nM). TopBP1-IN-5 selectively disrupts the interaction of TopBP1-BRCT7/8 with E2F1, mutp53, MIZ1, PLK1, CIP2A, and Top2A, without affecting BRCT1/2- and BRCT5-mediated interactions. TopBP1-IN-5 activates caspase-3/7 and caspase-8 to induce prometaphase arrest, mitotic catastrophe, and apoptosis, while inhibiting the MYC transcriptional program and enhancing the binding of MIZ1 to the p21Cip1 promoter. TopBP1-IN-5 exhibits broad-spectrum anticancer activity in triple-negative breast cancer, ovarian cancer, lung cancer, and acute myeloid leukemia models, and can be used for research on related cancers.
For research use only. We do not sell to patients.
- CAS No.: 896074-75-2
- Formula: C21H22N2O3
- Molecular Weight:350.41
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-468, MDAH-2774, AML12
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Concentration:5 μM
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Incubation Time:20 h
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Result:Induced apoptosis in MDA-MB-468 and MDAH-2774 cells as indicated by caspase-3/7 activity.
Had no effect in nontransformed AML12 mouse hepatocytes.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) (female, BCM2665 PDX model)[1]
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Dosage:40 mg/kg (efficacy); 15, 30, 45, or 60 mg/kg (dose-response)
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Administration:i.p.; twice weekly (40 mg/kg) or three times per week (dose-response); 15 days (40 mg/kg) or 3 weeks (dose-response)
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Result:Significantly suppressed tumor growth at 40 mg/kg twice weekly.
Induced apoptosis as evidenced by increased PARP1 cleavage in tumors.
Did not induce apoptosis or alter Ki-67 staining in intestinal crypts.
Increased the thermal stability (Tm) of TopBP1 protein in xenograft tumor tissues.
Showed dose-dependent in vivo antitumor activity with doses up to 60 mg/kg tolerated well and no plateau in efficacy observed.
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Animal Model:NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG)[1]
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Dosage:30 mg/kg
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Administration:i.p.; three times per week; 17 days
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Result:Significantly reduced the growth of H1975-OsiR tumors.
Did not alter Ki-67 staining or trigger apoptosis in mouse intestinal crypts.
Chemical Information
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CAS No. 896074-75-2
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Molecular Weight 350.41
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Formula C21H22N2O3
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SMILES
CN1CCN(CC1)CC2=CC(=O)OC3=C2C=C(C(=C3)C4=CC=CC=C4)O
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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)
TopBP1-IN-5 Related Classifications
HY-W320366 Related Classifications
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