1. Epigenetics
  2. Histone Acetyltransferase
  3. CPI-1612

CPI-1612 

Cat. No.: HY-136285
Handling Instructions

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.

For research use only. We do not sell to patients.

CPI-1612 Chemical Structure

CPI-1612 Chemical Structure

CAS No. : 2374971-81-8

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Description

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].

IC50 & Target

IC50: 8.1 nM (EP300 HAT)[1]

In Vitro

CPI-1612 inhibits full length EP300 and full length CBP with IC50 values <0.5 nM and 2.9 nM, respectively[1].
CPI-1612 inhibits H3K18Ac MSD (H3K18 = histone 3 lysine 18, MSD = meso scale discovery) and JEKO-1 cell proliferation with with IC50 values 14 nM and <7.9 nM, respectively[1].
CPI-1612 (compound 17) shows weak activity in a hERG binding assay (IC50 = 10.4 μM) and displayed moderate inhibition of CYP2C8 (IC50 = 1.9 μM) and CYP2C19 (IC50 = 2.7 μM)[1].

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[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

450.53

Formula

C₂₇H₂₆N₆O

CAS No.

2374971-81-8

SMILES

O=C(NC1=NC=C(C2=CN(C)N=C2)C=C1)[[email protected]](NC[[email protected]](C3=CC=C(C#N)C=C3)C)C4=CC=CC=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

CPI-1612CPI1612CPI 1612Histone AcetyltransferaseHATsHATP300CBPacetylationCREBHDACInhibitorinhibitorinhibit

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