Benzeneacetamide, α-[[(2S)-2-(4-cyanophenyl)propyl]amino]-N-[5-(1-methyl-1H-pyrazol-4-yl)-2-pyridinyl]-, (αR)-
- CAS No.
- 2374971-81-8
- Chemical Name:
- Benzeneacetamide, α-[[(2S)-2-(4-cyanophenyl)propyl]amino]-N-[5-(1-methyl-1H-pyrazol-4-yl)-2-pyridinyl]-, (αR)-
- Synonyms
- CPI-1612;(R)-2-(((S)-2-(4-Cyanophenyl)propyl)amino)-N-(5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-yl)-2-phenylacetamide;Benzeneacetamide, α-[[(2S)-2-(4-cyanophenyl)propyl]amino]-N-[5-(1-methyl-1H-pyrazol-4-yl)-2-pyridinyl]-, (αR)-
- CBNumber:
- CB58096099
- Molecular Formula:
- C27H26N6O
- Molecular Weight:
- 450.55
- MDL Number:
- MFCD32899894
- MOL File:
- 2374971-81-8.mol
- MSDS File:
- SDS
- TDS File:
- TDS
Benzeneacetamide, α-[[(2S)-2-(4-cyanophenyl)propyl]amino]-N-[5-(1-methyl-1H-pyrazol-4-yl)-2-pyridinyl]-, (αR)- 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)- price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Biosynth | BC177710 | CPI-1612 | 2374971-81-8 | 1mg | $254.1 | 2026-06-04 | Buy |
| Biosynth | BC177710 | CPI-1612 | 2374971-81-8 | 5mg | $1079.95 | 2026-06-04 | Buy |
| Biosynth | BC177710 | CPI-1612 | 2374971-81-8 | 10mg | $1727.9 | 2026-06-04 | Buy |
| ChemScene | CS-0127588 | CPI-1612 99.75% | 2374971-81-8 | 5mg | $433 | 2026-06-04 | Buy |
| ChemScene | CS-0127588 | CPI-1612 99.75% | 2374971-81-8 | 10mg | $737 | 2026-06-04 | Buy |
Benzeneacetamide, α-[[(2S)-2-(4-cyanophenyl)propyl]amino]-N-[5-(1-methyl-1H-pyrazol-4-yl)-2-pyridinyl]-, (αR)- Chemical Properties, Uses, Production
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
Raw materials
Preparation Products
Benzeneacetamide, α-[[(2S)-2-(4-cyanophenyl)propyl]amino]-N-[5-(1-methyl-1H-pyrazol-4-yl)-2-pyridinyl]-, (αR)- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Beijing Solarbio Science & Tecnology Co., Ltd. | 17801761073 18101056239 | 3193328036@qq.com | China | 28150 | 68 |
| ShangHai ChuanQian Chemcial Technique Centre | 15869524721 | 3525679403@qq.com | China | 4565 | 58 |
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| Nantong QuanYi Biotechnology Co., Ltd | 0513-66337626 18051384581 | sales@chemhifuture.com | China | 5985 | 58 |
| Soochow Chirally Material Science and Technology Co.,Ltd | 0512-66834346 17751187418 | sales@krl-tech.com | China | 1284 | 58 |
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| Soochow Chirally Material Science and Technology Co.,Ltd | +86-51266834346 +86-17751128648 | sales@krl-tech.com | China | 1050 | 58 |
| TargetMol Chemicals Inc. | 13564774135 | marketing@targetmol.com | United States | 19950 | 58 |
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2374971-81-8 (Benzeneacetamide, α-[[(2S)-2-(4-cyanophenyl)propyl]amino]-N-[5-(1-methyl-1H-pyrazol-4-yl)-2-pyridinyl]-, (αR)-) Related Search:
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