| Identification | Back Directory | [Name]
CPI-169 | [CAS]
1450655-76-1 | [Synonyms]
CPI-169
CPI 169;CPI169
CPI-169 racemate
CPI169;CPI 169;CPI-169
1-(1-(1-(Ethylsulfonyl)piperidin-4-yl)ethyl)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1H-indole-3-carboxamide
1H-Indole-3-carboxamide, N-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-1-[1-[1-(ethylsulfonyl)-4-piperidinyl]ethyl]-2-methyl- | [Molecular Formula]
C27H36N4O5S | [MDL Number]
MFCD28167777 | [MOL File]
1450655-76-1.mol | [Molecular Weight]
528.66 |
| Chemical Properties | Back Directory | [density ]
1.31±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≥26.45 mg/mL in DMSO; insoluble in H2O; ≥2.18 mg/mL in EtOH with gentle warming and ultrasonic | [form ]
solid | [pka]
11.01±0.10(Predicted) |
| Hazard Information | Back Directory | [Uses]
CPI-169 is a heteroaryl amide that was discovered useful as modulator of Me modifying enzymes. | [Definition]
ChEBI: 1-[1-(1-ethylsulfonyl-4-piperidinyl)ethyl]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methyl-3-indolecarboxamide is an indolecarboxamide. | [Biological Activity]
cpi-169 is a novel, small molecule and potent inhibitor of enhancer of zeste homolog 2 (ezh2) with an ic50 value of <1nm for polycomb repressive complex 2 (prc2) [1].cpi-169 has been found to be a potent ezh2 inhibitor with an ic50 value of <1nm for polycomb repressive complex 2 (prc2). in addition, cpi-169 has been reported to reduce cellular levels of histone h3 on lysine 27(h3k27) with an ec50 value of 70nm. moreover, cpi-169 has been exhibited to trigger cell cycle arrest and apoptosis in cells. apart from these, treatment the inhibitor at 200mpk twice daily, cpi-169 has been noted to have a well tolerated in mice with no observed toxic effect or body weight loss [1]. | [storage]
Store at -20°C | [References]
[1] vidya balasubramanian, priya iyer, shilpi arora, patrick troyer, emmanuel normant. constellation pharmaceuticals, cambridge, ma. cpi-169, a novel and potent ezh2 inhibitor, synergizes with chop in vivo and achieves complete regression in lymphoma xenograft models |
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