≥99% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -20°C Ships Ice chest + Ice pads Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
CPI-1612 is a highly potent, orally active EP300/CBP histone acetyltransferase (HAT) inhibitor with an IC 50 of 8.1 nM for EP300 HAT . CPI-1612 has an anticancer activity
In Vitro
CPI-1612 inhibits full length EP300 and full length CBP with IC 50 values <0.5 nM and 2.9 nM, respectively. ?\nCPI-1612 inhibits H3K18Ac MSD (H3K18 = histone 3 lysine 18, MSD = meso scale discovery) and JEKO-1 cell proliferation with with IC 50 values 14 nM and <7.9 nM, respectively. ?\nCPI-1612 (compound 17) shows weak activity in a hERG binding assay (IC 50 = 10.4 μM) and displayed moderate inhibition of CYP2C8 (IC 50 = 1.9 μM) and CYP2C19 (IC 50 = 2.7 μM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 . ?\nWhile 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, V ss = 3.7 L/kg, T 1/2 = 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, V ss = 2.0 L/kg, T 1/2 = 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, V ss = 1.8 L/kg, T 1/2 = 1.2 h, F% = 9; AUC/dose = 35.6 h·mg/mL) . ?\nA 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57B6 mice injected with JEKO-1 cells 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.
Form:Solid
IC50& Target:CBP/p300
| Sorrisos canónicos | CC(CNC(C1=CC=CC=C1)C(=O)NC2=NC=C(C=C2)C3=CN(N=C3)C)C4=CC=C(C=C4)C#N |
|---|---|
| IUPAC Name | (2R)-2-[[(2S)-2-(4-cyanophenyl)propyl]amino]-N-[5-(1-methylpyrazol-4-yl)pyridin-2-yl]-2-phenylacetamide |
| InChIKey | SEDFZSHSBUXKAC-NIYFSFCBSA-N |
| INCHI | 1S/C27H26N6O/c1-19(21-10-8-20(14-28)9-11-21)15-30-26(22-6-4-3-5-7-22)27(34)32-25-13-12-23(16-29-25)24-17-31-33(2)18-24/h3-13,16-19,26,30H,15H2,1-2H3,(H,29,32,34)/t19-,26-/m1/s1 |
| SMILES isoméricas | C[C@H](CN[C@H](C1=CC=CC=C1)C(=O)NC2=NC=C(C=C2)C3=CN(N=C3)C)C4=CC=C(C=C4)C#N |
| PubChem CID | 146014965 |
| Peso molecular | 450.53 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
Download SDS →Lot-specific quality data. Enter your lot number to retrieve the exact COA.
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View spec sheet →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organic acids and derivatives |
| Classe | Carboxylic acids and derivatives |
| Subclass | Amino acids, peptides, and analogues |
| Intermediate Tree Nodes | Amino acids and derivatives - Alpha amino acids and derivatives |
| Direct Parent | Alpha amino acid amides |
| Alternative Parents | Pyrazolylpyridines Phenylpropylamines Phenylacetamides Monocyclic monoterpenoids Aromatic monoterpenoids N-arylamides Benzonitriles Aralkylamines Imidolactams Pyrazoles Heteroaromatic compounds Secondary carboxylic acid amides Nitriles Dialkylamines Azacyclic compounds Organopnictogen compounds Organic oxides Hydrocarbon derivatives Carbonyl compounds |
| Molecular Framework | Aromatic heteromonocyclic compounds |
| Substituents | Alpha-amino acid amide - 3-pyrazolylpyridine - Phenylacetamide - Phenylpropylamine - Monoterpenoid - Monocyclic monoterpenoid - Aromatic monoterpenoid - P-cymene - N-arylamide - Benzonitrile - Aralkylamine - Imidolactam - Benzenoid - Pyridine - Monocyclic benzene moiety - Heteroaromatic compound - Pyrazole - Azole - Secondary carboxylic acid amide - Carboxamide group - Azacycle - Organoheterocyclic compound - Secondary amine - Nitrile - Carbonitrile - Secondary aliphatic amine - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Organooxygen compound - Organonitrogen compound - Carbonyl group - Amine - Aromatic heteromonocyclic compound |
| Descrição | This compound belongs to the class of organic compounds known as alpha amino acid amides. These are amide derivatives of alpha amino acids. |
| External Descriptors | Not available |
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| Solubilidade | DMSO : 100 mg/mL (221.96 mM; Need ultrasonic) |
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