1395347-24-6
1395347-24-6 structure
- Name: ISA-2011B
- Chemical Name: ISA-2011B
- CAS Number: 1395347-24-6
- Molecular Formula: C22H18ClN3O4
- Molecular Weight: 423.849
- Catalog: Research Areas Cancer
- Create Date: 2018-05-27 10:35:39
- Modify Date: 2025-08-26 11:16:24
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ISA-2011B is a PIP5Kα inhibitor with promising anticancer effects .
| Name | ISA-2011B |
|---|---|
| Synonyms |
5H-1,3-Dioxolo[4,5-g]pyrazino[1,2-b]isoquinoline-7,10-dione, 5-(5-chloro-1H-indol-3-yl)-8,9,10a,11-tetrahydro-9-methyl-, (5S,10aS)-
(5S,10aS)-5-(5-Chloro-1H-indol-3-yl)-9-methyl-8,9,10a,11-tetrahydro-5H-[1,3]dioxolo[4,5-g]pyrazino[1,2-b]isoquinoline-7,10-dione |
| Description | ISA-2011B is a PIP5Kα inhibitor with promising anticancer effects . |
|---|---|
| Related Catalog | |
| In Vitro | The proliferation rate of PC-3 cells after treatment with ISA-2011B at 10, 20, and 50 μM is significantly reduced to 58.77%, 48.65%, and 21.62% of vehicle-treated controls, respectively. ISA-2011B exhibits the highest binding affinity to PIP5K1α, and to MAP/microtubule affinity-regulating kinase 1 and 4 (MARK1 and MARK4) across 460 kinases. ISA-2011B treatment inhibits PIP5K1α expression by 78.6% in PC-3 cells[1]. ISA-2011B leads to a remarkable reduction in AR-V7 and CDK1 in both nucleus and cytoplasm of 22Rv1 cells. ISA-2011B treatment also abolishes AR expression in the nucleus, without depleting the cytoplasmic AR[2]. |
| In Vivo | ISA-2011B significantly inhibits growth of tumor cells in xenograft mice, and is mediated by targeting PIP5K1α-associated PI3K/AKT and the downstream survival, proliferation, and invasion pathways[1]. Overexpression of AR-V7 increases PIP5K1α, promotes rapid growth of PCa in xenograft mice, whereas inhibition of PIP5K1α by its inhibitor ISA-2011B suppresses the growth and invasiveness of xenograft tumors overexpressing AR-V7. ISA-2011B disrupts protein stabilization of AR-V7 which is dependent on PIP5K1α, leading to suppression of invasive growth of AR-V7-high tumors in xenograft mice[2]. |
| Cell Assay | Cells are grown in phenol red-free RPMI-1640 medium 24 hours and then are treated with drugs alone or in combination for 24 hours or 48 hours. Enzalutamide at 5 μM or ISA-2011B at 20 μM or 50 μM final concentrations or solvent DMSO 1% is used. For treatment of 22Rv1 cells with MG132, a proteasome inhibitor, cells are treated with MG132 at 1 μM. For combination treatment of MG132 and ISA-2011B, cells are pre-treated with MG132 for 30 min at 1 μM prior to treatment of ISA-2011B[2]. |
| Animal Admin | Mice: BALB/c nude mice aged 8 to 12 wk are used in the experiments. Tumor cells are implanted into the mice. Tumor xenografts are treated with vehicle (control), docetaxel (10 mg/kg), ISA-2011B (40 mg/kg), and docetaxel (10 mg/kg) in combination with ISA-2011B (40 mg/kg) every second day[1]. |
| References |
| Density | 1.6±0.1 g/cm3 |
|---|---|
| Boiling Point | 714.9±60.0 °C at 760 mmHg |
| Molecular Formula | C22H18ClN3O4 |
| Molecular Weight | 423.849 |
| Flash Point | 386.1±32.9 °C |
| Exact Mass | 423.098572 |
| LogP | 2.23 |
| Vapour Pressure | 0.0±2.3 mmHg at 25°C |
| Index of Refraction | 1.762 |
| Storage condition | 2-8℃ |