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CX-6258 inhibited Flt-3 and Pim-3 (IC50=0.134 and 0.016 uM). CX-6258 is a reversible inhibitor of Pim-1 (Ki=0.005 uM). CX-6258 shows robust antiproliferative potencies against all cell lines tested derived from human solid tumors and hematological malignancies. CX-6258 shows dose-dependent efficacy in mice bearing MV-4-11 xenografts, with 45% and 75% TGI at 50 and 100 mg/kg/day, respectively.
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Source | Clin Cancer Res (2016). Figure 3. CX-6258 |
| Method | Cell-cycle analyses | |
| Cell Lines | PC3 and DU145 cells | |
| Concentrations | 0, 5, or 10 mmol/L | |
| Incubation Time | 48-hour | |
| Results | Cell-cycle analyses of LNCaP cells 48 hours following CX- 6258 treatment revealed a significant decrease in G0–G1 phase and a pronounced accumulation of cells in G2–M phase |
| Cell Experiment | |
|---|---|
| Cell lines | MV-4-11, SEM, EOL-1, MOLM-13, PL-21, THP-1, K562, MEG01, HL60 and U266 cells |
| Preparation method | Cell Viability assay. For proliferation assays, cells were plated at 5,000 to 20,000 cells per well in 96 well plates overnight before treatment for 96 hours with serially diluted compound or vehicle DMSO. Cell viability was measured after the addition of 10 μL Alamar Blue (Invitrogen) for 4 hours at 37˚C. The GI50 was determined by calculating growth at each dose relative to vehicle treated cells and cell viability at the time of treatment. |
| Concentrations | 0~10 μM |
| Incubation time | 96 h |
| Animal Experiment | |
|---|---|
| Animal models | MV-4-11 xenograft models in nude mice |
| Formulation | H2O |
| Dosages | 50 or 100 mg/kg once daily over a period of 21 days |
| Administration | PO |
| Molecular Weight | 461.94 |
| Formula | C26H24ClN3O3 |
| CAS Number | 1202916-90-2 |
| Solubility (25°C) | DMSO ≥ 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Pim Products |
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| SGI-1776
SGI-1776 is novel small molecule inhibitor of PIM kinase activity with IC50 of 7 ± 1.8, 363 ± 27.6 and 69 ± 9.2 nM for Pim-1, Pim-2, and Pim-3, respectively. |
| SMI-4a
SMI-4a is a potent inhibitor of Pim1 with IC50 of 17 nM, modest potent to Pim-2, does not significantly inhibit other serine/threonine- or tyrosine-kinases. |
| TCS PIM-1 1
TCS PIM-1 1 is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2(IC50s > 20,000 nM). |
| Hispidulin
Hispidulin is a natural flavonoid with a wide range of biological activities. Hispidulin is an inhibitor of PIM-1 with IC50 value of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. |
| AZD-1208
AZD1208 is a potent, highly selective, and orally available Pim kinase inhibitor that effectively inhibits all three isoforms at <5 nM or <150 nM in enzyme and cell assays, respectively. |
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