CPI-1612
Based on 1 Customer Validation
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.
- Purity: 99.75%
- CAS No.: 2374971-81-8
- Formula: C27H26N6O
- Molecular Weight:450.53
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Epigenetics Compound Library
HY-L005
-
Histone Modification Research Compound Library
HY-L024
-
Anti-Cancer Compound Library
HY-L025
-
Orally Active Compound Library
HY-L061
-
Chemical Probe Library
HY-L063
-
Anti-Pulmonary Fibrosis Compound Library
HY-L125
-
Heterocyclic Compound Library
HY-L138
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Lactylation Compound Library
HY-L249
Biological Activity
|
CBP/p300 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | EC50 |
0.014 μM
Compound: 17; CPI-1612
|
Inhibition of EP300/CBP HAT domain in human HCT116 cells assessed as reduction in H3K18 acetylation incubated for 2 hrs by meso scale discovery
Inhibition of EP300/CBP HAT domain in human HCT116 cells assessed as reduction in H3K18 acetylation incubated for 2 hrs by meso scale discovery
|
[PMID: 32551019] |
| JeKo-1 | GI50 |
<0.0079 μM
Compound: 17; CPI-1612
|
Growth inhibition of human JeKo1 cells incubated for 72 hrs by Cell Titer-Glo luminescent cell viability assay
Growth inhibition of human JeKo1 cells incubated for 72 hrs by Cell Titer-Glo luminescent cell viability assay
|
[PMID: 32551019] |
| LP-1 | GI50 |
0.005 μM
Compound: CPI-1612
|
Antiproliferative activity against human LP-1 cells assessed as growth inhibition incubated for 3 days by fluorescence based assay
Antiproliferative activity against human LP-1 cells assessed as growth inhibition incubated for 3 days by fluorescence based assay
|
[PMID: 38505842] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (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.
Chemical Information
-
CAS No. 2374971-81-8
-
Appearance Solid
-
Molecular Weight 450.53
-
Formula C27H26N6O
-
Color White to off-white
-
SMILES
O=C(NC1=NC=C(C2=CN(C)N=C2)C=C1)[C@H](NC[C@H](C3=CC=C(C#N)C=C3)C)C4=CC=CC=C4
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 230 mg/mL (510.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 5 mg/mL (11.10 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (272 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2196 mL | 11.0980 mL | 22.1961 mL | 55.4902 mL |
| 5 mM | 0.4439 mL | 2.2196 mL | 4.4392 mL | 11.0980 mL | |
| 10 mM | 0.2220 mL | 1.1098 mL | 2.2196 mL | 5.5490 mL | |
| 15 mM | 0.1480 mL | 0.7399 mL | 1.4797 mL | 3.6993 mL | |
| 20 mM | 0.1110 mL | 0.5549 mL | 1.1098 mL | 2.7745 mL | |
| 25 mM | 0.0888 mL | 0.4439 mL | 0.8878 mL | 2.2196 mL | |
| 30 mM | 0.0740 mL | 0.3699 mL | 0.7399 mL | 1.8497 mL | |
| 40 mM | 0.0555 mL | 0.2775 mL | 0.5549 mL | 1.3873 mL | |
| 50 mM | 0.0444 mL | 0.2220 mL | 0.4439 mL | 1.1098 mL | |
| 60 mM | 0.0370 mL | 0.1850 mL | 0.3699 mL | 0.9248 mL | |
| 80 mM | 0.0277 mL | 0.1387 mL | 0.2775 mL | 0.6936 mL | |
| 100 mM | 0.0222 mL | 0.1110 mL | 0.2220 mL | 0.5549 mL |
CPI-1612 Related Classifications
HY-136285 Related Classifications
Powered by Bioz