BEN-28010
BEN-28010 is a selective, orally active, blood-brain barrier permeable CHK1 inhibitor with an IC50 of 4.0 nM. BEN-28010 functions as a radiosensitizer, exhibits antitumor efficacy in GBM models. BEN-28010 can be used for the research of glioblastoma.
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- CAS No.: 3033961-38-2
- Formule: C20H22N8
- Masse moléculaire:374.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
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Chk1 4.0 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| A 172 | IC50 |
3.3 μM
Compound: Example 38; BEN-28010
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Cytotoxicity against human A-172 cells harboring wild type p53 assessed as reduction in cell viability incubated for 72 hrs by CellTiterGlo-2.0 reagent based Cell Viability assay
Cytotoxicity against human A-172 cells harboring wild type p53 assessed as reduction in cell viability incubated for 72 hrs by CellTiterGlo-2.0 reagent based Cell Viability assay
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[PMID: 40273287] |
BEN-28010 potently inhibits recombinant human CHK1 kinase with an IC50 of 4.0 ± 0.9 nM[1].
BEN-28010 inhibits CHK1 activity in SW620 cells with an IC50 of 0.45 ± 0.08 μM[1].
BEN-28010 inhibits p53 mutant LN-18 cell viability, with 24-fold greater potency in p53 mutant LN-18 cells (IC50 0.14 ± 0.01 μM) than p53 wild-type A172 cells (IC50 3.3 ± 0.15 μM); it also shows enhanced activity in p53-deficient GBM cell lines overall, and has an IC50 of 99 ± 4 nM in LN229 cells[1].
BEN-28010 potentiates the cytotoxic effects of ionizing radiation in patient-derived GBM stem cells, with an IC50 of 0.62 μM post-3 Gy IR and a therapeutic interaction (RIR > 1)[1].
BEN-28010 has a favorable in vitro ADME and selectivity profile, including high CHK1 selectivity over the kinome and CHK2, low cardiac arrhythmia risk, minimal CYP interactions, high permeability, and low efflux by MDR1 and BCRP[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:NOD/SCID (female)[1]
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Dosage:15 mg/kg; 50 mg/kg; 100 mg/kg
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Administration:p.o.; every other day for 10 days
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Result:Resulted in statistically significant reductions in mean tumor volumes compared to vehicle control on day 18 at 50 mg/kg (p=0.0005) and 100 mg/kg (p<0.0001) as monotherapy.
Resulted in statistically significant reductions in average tumor volumes compared to radiotherapy alone on day 21 at 50 mg/kg (p=0.0006) and 100 mg/kg (p<0.0001) in combination with IR.
Chemical Information
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CAS No. 3033961-38-2
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Masse moléculaire 374.44
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Formule C20H22N8
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SMILES
CN(C)[C@H](CC1)CN1C(C=C2)=CC=C2N(C=N3)C=C3NC4=NC=C(C#N)N=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BEN-28010 Related Classifications
HY-186085 Related Classifications
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