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Synonyms:
BEN-28010
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | BEN-28010 is a selective, orally bioavailable CHK1 inhibitor that can cross the blood-brain barrier, featuring an IC50 of 4.0 nM. This compound acts as a radiosensitizer and demonstrates antitumor activity in glioblastoma (GBM) models. BEN-28010 is applicable for research related to glioblastoma. |
| Targets & IC50 | Chk1:4.0 nM |
| In vitro | BEN-28010 is a potent inhibitor of recombinant CHK1 kinase, with an IC50 of 4.0 nM. It inhibits CHK1 activity in SW620 cells with an IC50 of 0.45 μM. BEN-28010 also reduces the viability of p53 mutant LN-18 cells with an efficacy (IC50 0.14 ± 0.01 μM) that is 24 times greater than that for p53 wild-type A172 cells (IC50 3.3 ± 0.15 μM). Additionally, BEN-28010 enhances the cytotoxic effects of ionizing radiation on GBM stem cells, achieving an IC50 of 0.62 μM following 3 Gy IR treatment. The compound demonstrates favorable in vitro ADME properties and selectivity, including high CHK1 selectivity over the kinome and CHK2, low arrhythmia risk, minimal CYP interaction, high permeability, and low efflux mediated by MDR1 and BCRP. |
| In vivo | BEN-28010 (50-100 mg/kg; orally; administered every other day for 10 consecutive days) demonstrates statistically significant tumor growth inhibition both as a standalone treatment and in combination with IR in subcutaneous LN229 glioblastoma (GBM) xenografts. |
| Molecular Weight | 374.44 |
| Formula | C20H22N8 |
| Cas No. | 3033961-38-2 |
| Smiles | N(C1=CN(C=N1)C2=CC=C(C=C2)N3C[C@H](N(C)C)CC3)C=4C=NC(C#N)=CN4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 µL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
| Size | Quantity | Unit Price | Amount | Operation |
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