Benzeneacetamide, α-[[(2S)-2-(4-cyanophenyl)propyl]amino]-N-[5-(1-methyl-1H-pyrazol-4-yl)-2-pyridinyl]-, (αR)- manufacturers
- CPI-1612
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- $2110.00
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2026-04-22
- CAS:2374971-81-8
- Purity:
- Supply Ability: 10g
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| | Benzeneacetamide, α-[[(2S)-2-(4-cyanophenyl)propyl]amino]-N-[5-(1-methyl-1H-pyrazol-4-yl)-2-pyridinyl]-, (αR)- Basic information |
| | Benzeneacetamide, α-[[(2S)-2-(4-cyanophenyl)propyl]amino]-N-[5-(1-methyl-1H-pyrazol-4-yl)-2-pyridinyl]-, (αR)- Chemical Properties |
| Boiling point | 719.1±60.0 °C(Predicted) | | density | 1.20±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 100 mg/mL (221.96 mM; Need ultrasonic) | | form | Solid | | pka | 12.12±0.70(Predicted) | | color | White to off-white |
| | Benzeneacetamide, α-[[(2S)-2-(4-cyanophenyl)propyl]amino]-N-[5-(1-methyl-1H-pyrazol-4-yl)-2-pyridinyl]-, (αR)- Usage And Synthesis |
| Uses | CPI-1612 is a highly potent, orally active EP300/CBP histone acetyltransferase (HAT) inhibitor with an IC50 of 8.1 nM for EP300 HAT. CPI-1612 has an anticancer activity[1]. | | in vivo | CPI-1612 (compound 17; 0.5 mg/kg; oral administration; twice a day; for 4 weeks) treatment shows 67% tumor growth inhibition (TGI) with concomitant reduction of H3K27Ac in plasma and reduction of H3K18Ac in the tumor[1].
While the oral exposure of CPI-1612 (compound 17) in dogs (0.5 mg/kg IV; 1.0 mg/kg PO; clearance = 0.42 L/h/kg, Vss = 3.7 L/kg, T1/2 = 5.5 h, F% = 71; AUC/dose = 1691 h·mg/mL) and mice (1 mg/kg IV; 5 mg/kg PO; clearance = 3.8 L/h/kg, Vss = 2.0 L/kg, T1/2 = 0.98 h, F% = 79; AUC/dose = 211 h·mg/mL) is good, the exposure in rats is limited by poor bioavailability (1.0 mg/kg IV; 5.0 mg/kg PO; clearance = 2.6 L/h/kg, Vss = 1.8 L/kg, T1/2 = 1.2 h, F% = 9; AUC/dose = 35.6 h·mg/mL)[1].
A single dose of CPI-1612 is administered orally to CD-1 mice and brain and plasma exposures of CPI-1612 are measured at 0.25, 0.5, 1.0, 2.0, 4.0, and 8.0 h. CPI-1612 is highly brain-penetrant, showing a brain-to-plasma ratio of 0.35 after a single oral dose[1]. | Animal Model: | C57B6 mice injected with JEKO-1 cells[1] | | Dosage: | 0.5 mg/kg | | Administration: | Oral administration; twice a day; for 4 weeks | | Result: | Showed 67% tumor growth inhibition (TGI) at a dose of 0.5 mg/kg. |
| | IC 50 | CBP/p300 | | References | [1] Jonathan E Wilson, et al. Discovery of CPI-1612: A Potent, Selective, and Orally Bioavailable EP300/CBP Histone Acetyltransferase Inhibitor. ACS Med Chem Lett. 2020 Apr 23;11(6):1324-1329. DOI:10.1021/acsmedchemlett.0c00155 |
| | Benzeneacetamide, α-[[(2S)-2-(4-cyanophenyl)propyl]amino]-N-[5-(1-methyl-1H-pyrazol-4-yl)-2-pyridinyl]-, (αR)- Preparation Products And Raw materials |
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