CBP-93872
CBP-93872 is a G2 checkpoint inhibitor and a chemosensitizer. CBP-93872 specifically inhibits DNA double-strand break (DSB)-dependent, Nbs1-mediated ATR activation, without directly inhibiting ATR kinase activity or affecting ATR activation induced by other types of DNA damage; meanwhile, it suppresses the pathway between ATM and ATR activation, thereby reducing the autophosphorylation of ATR and the subsequent phosphorylation of Chk1. CBP-93872 does not inhibit DNA end resection at DSB sites. CBP-93872 induces cell death and enhances the cytotoxic effects of platinum-containing compounds and pyrimidine antimetabolites on cancer cells. CBP-93872 can be used in related research on p53-mutant cancers, colorectal cancer, and pancreatic cancer.
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- CAS No.: 67427-51-4
- 화학식: C10H15BrN2O
- 분자량:259.15
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
Chk1 |
In Vitro
CBP-93872 (>50 μM; 72 h) inhibits the proliferation of colorectal cancer HT29 cells at concentrations above 50 μM after 72 h of treatment[2].
CBP-93872 (>200 μM; 72 h) inhibits the proliferation of Panc-1 pancreatic cancer cells at a concentration higher than 200 μM after 72 h of treatment[2].
CBP-93872 (50 μM; 48 h) abrogates the G2 checkpoint activation induced by Cisplatin (HY-17394) in HT29 colorectal cancer cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-29 cells
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Concentration:20 μM
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Incubation Time:2 h post-IR/UV/MMS treatment; 4 h post-HU treatment; 4, 8 h post-10 Gy IR treatment
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Result:Strongly compromised IR-induced phosphorylation of Chk1 at serines 317 and 345, as well as ATR autophosphorylation at threonine 1989, but did not affect ATM autophosphorylation at serine 1981 or Chk2 phosphorylation.
Did not alter Chk1 phosphorylation induced by UV, MMS, or HU.
Reduced H3 pS10 levels at 4 hours post-IR, then elevated H3 pS10 levels at 8 hours post-IR.
Inhibited IR-induced phosphorylation of Nbs1 at serine 343 and RPA2 at serine 33, but did not affect UV-induced Nbs1 phosphorylation or the formation of Nbs1-Mre11-Rad50 complexes.
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Cell Line:HT29 human colorectal cancer cells
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Concentration:10-200 μM
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Incubation Time:72 h
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Result:Suppressed HT29 cell proliferation at concentrations greater than 50 μM after 72 h.
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Cell Line:Panc-1 human pancreatic cancer cells
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Concentration:50-500 μM
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Incubation Time:72 h
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Result:Suppressed Panc-1 cell proliferation at concentrations greater than 200 μM after 72 h.
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Cell Line:HT29 human colorectal cancer cells
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Concentration:50 μM (in combination with 30 μM oxaliplatin)
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Incubation Time:72 h (flow cytometry); 16, 24, 48, 72 h (immunoblotting)
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Result:Increased the sub-G1 cell population in HT29 cells from 6.1% to 24.3% after 72 h.
Detected abundant cleaved caspase 3 and elevated γH2AX in cells receiving combined treatment.
Chemical Information
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CAS No. 67427-51-4
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분자량 259.15
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화학식 C10H15BrN2O
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SMILES
BrC1=CC(=CC=C1NCC(O)CN)C
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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)
CBP-93872 Related Classifications
HY-119225 Related Classifications
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