1353859-00-3
1353859-00-3 structure
- Name: CX-6258 hydrochloride
- Chemical Name: 2H-Indol-2-one, 5-chloro-3-[[5-[3-[(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)carbonyl]phenyl]-2-furanyl]methylene]-1,3-dihydro-, hydrochloride (1:1), (3E)
- CAS Number: 1353859-00-3
- Molecular Formula: C26H25Cl2N3O3
- Molecular Weight: 498.401
- Catalog: Biochemical Inhibitor Tyrosine protein kinase/signal transducer and transcriptional activator inhibitor (JAK/STAT) Pim inhibitor
- Create Date: 2017-05-30 06:37:32
- Modify Date: 2024-01-14 11:25:56
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CX-6258 hydrochloride is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively[1].
| Name | 2H-Indol-2-one, 5-chloro-3-[[5-[3-[(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)carbonyl]phenyl]-2-furanyl]methylene]-1,3-dihydro-, hydrochloride (1:1), (3E) |
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| Synonyms |
2H-Indol-2-one, 5-chloro-3-[[5-[3-[(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)carbonyl]phenyl]-2-furanyl]methylene]-1,3-dihydro-, (3E)-, hydrochloride (1:1)
(3E)-5-Chloro-3-[(5-{3-[(4-methyl-1,4-diazepan-1-yl)carbonyl]phenyl}-2-furyl)methylene]-1,3-dihydro-2H-indol-2-one hydrochloride (1:1) CX-6258 HCl |
| Description | CX-6258 hydrochloride is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively[1]. |
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| Related Catalog | |
| Target |
IC50: 5 nM (Pim-1), 25 nM (Pim-2), 16 nM (Pim-3)[1]. |
| In Vitro | CX-6258 causes dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively[1]. CX-6258 treatment (12 mM, 3 h) treatment diminishes steady-state levels of ectopic NKX3.1 in PC3 cells[2]. CX-6258 treatment results in a significant reduction in NKX3.1 half-life[2]. Western Blot Analysis[1] Cell Line: MV-4-11 human AML cells. Concentration: 0.1 μM, 1 μM, 10 μM. Incubation Time: 2 hours. Result: Caused dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively. |
| In Vivo | CX-6258 (50-100 mg/kg; p.o; daily; over a period of 21 days) exhibits robust in vivo efficacy in two Pim kinases driven tumor models[1]. Animal Model: Nude mice, MV-4-11 xenograft models[1] Dosage: 50 mg/kg, 100 mg/kg. Administration: Oral administration; once daily; over a period of 21 days. Result: Exhibitd dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI. |
| References |
| Molecular Formula | C26H25Cl2N3O3 |
|---|---|
| Molecular Weight | 498.401 |
| Exact Mass | 497.127289 |
| PSA | 65.79000 |
| LogP | 5.68620 |
| Storage condition | -20℃ |