1802175-07-0
1802175-07-0 structure
- Name: CPI-169
- Chemical Name: 1-[(1R)-1-(1-ethylsulfonyl-4-piperidinyl)ethyl]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methyl-3-indolecarboxamide
- CAS Number: 1802175-07-0
- Molecular Formula: C27H36N4O5S
- Molecular Weight: 528.664
- Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
- Create Date: 2018-06-09 05:06:15
- Modify Date: 2024-01-10 18:16:55
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CPI-169 is a novel and potent EZH2 inhibitor, with IC50s of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.
| Name | 1-[(1R)-1-(1-ethylsulfonyl-4-piperidinyl)ethyl]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methyl-3-indolecarboxamide |
|---|---|
| Synonyms |
1-{(1R)-1-[1-(Ethylsulfonyl)-4-piperidinyl]ethyl}-N-[(4-methoxy-6-methyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-2-methyl-1H-indole-3-carboxamide
1-[(1R)-1-(1-ethylsulfonyl-4-piperidinyl)ethyl]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methyl-3-indolecarboxamide 1H-Indole-3-carboxamide, N-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-1-[(1R)-1-[1-(ethylsulfonyl)-4-piperidinyl]ethyl]-2-methyl- CPI-169 |
| Description | CPI-169 is a novel and potent EZH2 inhibitor, with IC50s of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively. |
|---|---|
| Related Catalog | |
| Target |
IC50: 0.24 nM (EZH2 WT), 0.51 nM (EZH2 Y641N), 6.1 nM (EZH1) |
| In Vitro | CPI-169 inhibits the catalytic activity of PRC2 with an IC50 of < 1nM, decreases cellular levels of H3K27me3 with an EC50 of 70 nM, and triggers cell cycle arrest and apoptosis in a variety of cell lines[1]. In KARPAS-422 cells, CPI-169 shows a dose-dependent inhibitory effect on cell viability, and produces synergy anti-proliferative activity when used in combination with ABT-199. In 16 out of 25 NHL cell lines, CPI-169 also suppresses cell growth with GI50 of <5 μM[2]. |
| In Vivo | CPI-169 (200 mpk, s.c. BID) is well tolerated in mice with no observed toxic effect or body weight loss. CPI-169 treatment leads to tumor growth inhibition (TGI) of an EZH2 mutant KARPAS-422 DLBCL xenograft. CPI-169 (100 mpk, BID) with a single dose of CHOP leads tumors to rapidly regress and become unpalpable[1]. In mice bearing KARPAS-422 xenografts, CPI-169 (200 mg/kg, s.c.) effectively suppresses H3K27me3 levels and results in lymphoma tumor regression without affecting body weight or causing any overt adverse effects[2]. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Molecular Formula | C27H36N4O5S |
| Molecular Weight | 528.664 |
| Exact Mass | 528.240662 |
| LogP | 2.67 |
| Index of Refraction | 1.631 |
| Storage condition | 2-8℃ |