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CPI-1612 - 99%, high purity , CAS No.2374971-81-8

COA COA
    Grade & Purity:
  • ≥99%
In stock
Item Number
C646560
Grouped product items
SKU Size
Availability
 Price Qty
C646560-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$780.90
C646560-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,300.90
C646560-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$2,550.90
C646560-50mg
50mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$4,200.90
C646560-100mg
100mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$6,800.90
Wish List
Bulk Order  SDS  DATASHEET  Specification Sheet
View related series
Epigenetics (1496) Histone Acetyltransferase (79) Histone Modification (1379)

Basic Description

Specifications & Purity ≥99%
Biochemical and Physiological Mechanisms 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.
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Product Description

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

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organic acids and derivatives
Class 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
Description 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

Associated Targets(Human)

EP300 Tchem Histone acetyltransferase p300 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
CREBBP Tchem CREB-binding protein (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
KCNH2 Tclin HERG (29587 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2C8 Tchem Cytochrome P450 2C8 (1492 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP1A2 Tchem Cytochrome P450 1A2 (26471 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2C19 Tchem Cytochrome P450 2C19 (29246 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2B6 Tchem Cytochrome P450 2B6 (1338 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EP300 Tchem Histone acetyltransferase p300 (1259 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KAT2B Tchem Histone acetyltransferase PCAF (884 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CREBBP Tchem CREB-binding protein (1602 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KAT5 Tchem Histone acetyltransferase KAT5 (85 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KAT6A Tchem Histone acetyltransferase KAT6A (320 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KAT7 Tbio Histone acetyltransferase KAT7 (12 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KAT6B Tchem Histone acetyltransferase KAT6B (12 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
JeKo-1 (376 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Mus musculus (284745 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GCN5 Histone acetyltransferase GCN5 (89 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

IUPAC Name (2R)-2-[[(2S)-2-(4-cyanophenyl)propyl]amino]-N-[5-(1-methylpyrazol-4-yl)pyridin-2-yl]-2-phenylacetamide
INCHI 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
InChIKey SEDFZSHSBUXKAC-NIYFSFCBSA-N
Smiles 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
Isomeric SMILES 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
Molecular Weight 450.53

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

Solubility DMSO : 100 mg/mL (221.96 mM; Need ultrasonic)

Solution Calculators

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