| Identification | Back Directory | [Name]
CX6258 | [CAS]
1202916-90-2 | [Synonyms]
CX6258
CS-1091
CX-6258/CX6258
CX-6258, >=98%
CX-6258;CX6258;CX 6258
(E)-5-Chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2
(Z)-5-CHLORO-3-((5-(3-(4-METHYL-1,4-DIAZEPANE-1-CARBONYL)PHENYL)FURAN-2-YL)METHYLENE)INDOLIN-2-ONE.HCL
(3E)-5-Chloro-3-[(5-{3-[(4-methyl-1,4-diazepan-1-yl)carbonyl]phen yl}-2-furyl)methylene]-1,3-dihydro-2H-indol-2-one
(3E)-5-Chloro-3-[[5-[3-[(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)carbonyl]phenyl]-2-furanyl]methylene]-1,3-dihydro-2H-indol-2-one
2H-indol-2-one 5-chloro-3-[[5-[3-[(hexahydro-4-methyl-1h-14-diazepin-1-yl)carbonyl]phenyl]-2-furanyl]methylene]-1,3-dihydro- (3e)-
(3E)-5-Chloro-3-[[5-[3-[(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)carbonyl]phenyl]-2-furanyl]methylene]-1,3-dihydro-2H-indol-2-one CX-6258
CX6258 (3E)-5-Chloro-3-[[5-[3-[(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)carbonyl]phenyl]-2-furanyl]methylene]-1,3-dihydro-2H-indol-2-one | [Molecular Formula]
C26H24ClN3O3 | [MDL Number]
MFCD28142834 | [MOL File]
1202916-90-2.mol | [Molecular Weight]
461.94 |
| Chemical Properties | Back Directory | [Boiling point ]
697.8±55.0 °C(Predicted) | [density ]
1.309±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in EtOH; ≥11.15 mg/mL in DMSO; ≥2.575 mg/mL in H2O with gentle warming | [form ]
solid | [pka]
11.38±0.20(Predicted) | [color ]
Yellow to orange |
| Hazard Information | Back Directory | [Uses]
CX-6258 is a potent, selective, and orally efficacious pan-Pim kinases inhibitor. | [Biological Activity]
pim kinases (provirus integration site for moloney murine leukemia virus) are a family of serine/threonine kinases that regulate cell survival. this family of kinases is composed of three different isoforms (pim-1, pim-2, and pim-3). the simultaneous inhibition of pim-1, pim-2, and pim-3 kinases is emerging as a promising strategy for anticancer drug development. cx-6258 is a potent, selective, and orally efficacious pan-pim kinases inhibitor. | [in vitro]
cx-6258 exhibited in vitro synergy with chemotherapeutics. the antiproliferative activity of cx-6258 was examined against a panel of cell lines derived from human solid tumors and hematological malignancies. cx-6258 demonstrated robust antiproliferative potencies against all cell lines tested [1]. | [in vivo]
cx-6258 was evaluated in two human tumor xenograft growth efficacy models, acute myeloid leukemia mv-4-11, and prostate adenocarcinoma pc3. the drug exhibited dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (tgi) and a 100 mg/kg dose producing 75% tgi. in addition, cx-6258 displayed significant efficacy in vivo in two xenograft models representing the diseases where pim kinases had been shown to play an important role [1]. | [target]
Pim1 | [storage]
Store at -20°C | [References]
[1] haddach m, michaux j, schwaebe mk, et al. discovery of cx-6258. a potent, selective, and orally efficacious pan-pim kinases inhibitor. acs med chem lett. 2011;3(2):135-9. |
|
|