PH14
Based on 1 Customer Validation
PH14 is a PI3Kα/HDAC3 inhibitor, with an IC50 value of 20.3 nM against PI3Kα and 24.5 nM against HDAC3. PH14 blocks the phosphorylation of AKT, inhibits the PI3K/AKT signaling pathway, increases the level of acetylated histone H3, promotes apoptosis, and exerts antiproliferative activity against tumor cells. PH14 can be used in the research of mantle cell lymphoma, myeloma, acute promyelocytic leukemia, and breast cancer.
For research use only. We do not sell to patients.
- Purity: 99.09%
- CAS No.: 3053430-96-6
- Formula: C34H39N9O5
- Molecular Weight:653.73
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Storage:Powder -20°C, 3 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]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PI3Kα 20.3 nM (IC50) |
HDAC3 24.5 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| JeKo-1 | IC50 |
0.5 μM
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Antiproliferative activity against human mantle cell lymphoma Jeko-1 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin assay.
Antiproliferative activity against human mantle cell lymphoma Jeko-1 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin assay.
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37948955 |
| HL-60 | IC50 |
0.9 μM
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Antiproliferative activity against human acute early myeloid leukemia HL60 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin assay.
Antiproliferative activity against human acute early myeloid leukemia HL60 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin assay.
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37948955 |
| MDA-MB-231 | IC50 |
1.5 μM
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Antiproliferative activity against human breast cancer MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin assay.
Antiproliferative activity against human breast cancer MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin assay.
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37948955 |
In Vitro
PH14 is a broad-spectrum PI3K inhibitor with the strongest targeted activity against PI3Kα, with an IC50 of 20.3 nM[1].
PH14 is a selective inhibitor of HDAC1-3, with the strongest inhibitory activity against HDAC3 (IC50 = 24.5 nM)[1].
PH14 (10 μM) exhibits weak inhibitory effects on CYP1A2, CYP2B6, CYP2C9, CYP2C19 and CYP3A4, and moderate inhibitory effect on CYP2D6 in human liver microsomes[1].
PH14 (48 h) potently inhibits the proliferation of various tumor cell lines, with the strongest activity against Jeko-1 cells (IC50 = 0.5 μM), and shows no cytotoxicity against normal HL7702 hepatocytes even at a concentration as high as 100 μM[1].
PH14 (0.25-1 μM; 24 h) blocks the PI3K/AKT signaling pathway, selectively increases the level of acetylated histone H3, and induces caspase 3 cleavage in Jeko-1 cells[1].
PH14 (0.25-1 μM; 48 h) dose-dependently induces apoptosis in Jeko-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human mantle cell lymphoma Jeko-1 cells
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Concentration:0.25, 0.5, 1 μM
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Incubation Time:24 h
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Result:Reduced phosphorylated AKT (p-AKT-S473) levels without changing total AKT levels at 0.25 μM.
Dose-dependently increased acetylated histone H3 (Ac-H3) levels with no effect on acetylated tubulin (Ac-tubulin) levels.
Upregulated cleaved-caspase3 levels at tested concentrations.
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Cell Line:human mantle cell lymphoma Jeko-1 cells
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Concentration:0.25, 0.5, 1 μM
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Incubation Time:48 h
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Result:Induced Jeko-1 cell apoptosis in a dose-dependent manner, with increasing apoptotic cell populations observed at higher concentrations.
Parmacokinetics
| Species | Dose | Route | C0 | T1/2 | AUC0-t | AUC0-∞ | MRTINF_obs | Vss | CL |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 1 mg/kg | i.v. | 13733 ng/mL | 10 h | 2697 ng/mL·h | 2772 ng/mL·h | 2 h | 719 mL/kg | 361 mL/h/kg |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (male)[1]
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Dosage:1 mg/kg
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Administration:i.v.; single administration
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Result:Exhibited favorable in vivo pharmacokinetic properties in male ICR mice
Chemical Information
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CAS No. 3053430-96-6
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Appearance Solid
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Molecular Weight 653.73
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Formula C34H39N9O5
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Color White to pink
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SMILES
COC1=NC(N2CCOCC2)=NC(C3=CC=C(NC(NC4=CC=C(C(NCCCCCC(NC5=CC=CC=C5N)=O)=O)C=C4)=O)C=C3)=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (76.48 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)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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 | 1.5297 mL | 7.6484 mL | 15.2968 mL | 38.2421 mL |
| 5 mM | 0.3059 mL | 1.5297 mL | 3.0594 mL | 7.6484 mL | |
| 10 mM | 0.1530 mL | 0.7648 mL | 1.5297 mL | 3.8242 mL | |
| 15 mM | 0.1020 mL | 0.5099 mL | 1.0198 mL | 2.5495 mL | |
| 20 mM | 0.0765 mL | 0.3824 mL | 0.7648 mL | 1.9121 mL | |
| 25 mM | 0.0612 mL | 0.3059 mL | 0.6119 mL | 1.5297 mL | |
| 30 mM | 0.0510 mL | 0.2549 mL | 0.5099 mL | 1.2747 mL | |
| 40 mM | 0.0382 mL | 0.1912 mL | 0.3824 mL | 0.9561 mL | |
| 50 mM | 0.0306 mL | 0.1530 mL | 0.3059 mL | 0.7648 mL | |
| 60 mM | 0.0255 mL | 0.1275 mL | 0.2549 mL | 0.6374 mL |
PH14 Related Classifications
HY-149669 Related Classifications
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