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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3033961-38-2
- 分子式: C20H22N8
- 分子量:374.44
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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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.
化学情報
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CAS 番号 3033961-38-2
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分子量 374.44
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
BEN-28010 関連分類
HY-186085 関連分類
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