| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C34H39N9O5 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
PH14 is a dual PI3Kα/HDAC3 inhibitor, with IC50 values of 20.3 nM against PI3Kα and 24.5 nM against HDAC3. It blocks AKT phosphorylation, inhibits the PI3K/AKT signaling pathway, increases acetylated histone H3 levels, promotes apoptosis, and shows antiproliferative activity against tumor cells. It can be used in research on mantle cell lymphoma, myeloma, acute promyelocytic leukemia, and breast cancer[1]. It is supplied as a white to pink solid (C34H39N9O5, MW 653.73) at 99.09% purity.
Physical & Chemical Properties
| CAS Number | 3053430-96-6 |
|---|---|
| Molecular Formula | C34H39N9O5 |
| Molecular Weight | 653.73 g/mol |
| Purity | 99.09% |
| Appearance | Solid |
| Color | White to pink |
| 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 |
| Target | PI3Kα, HDAC3 |
| Signaling Pathway | PI3K/Akt/mTOR; Epigenetics; Cell Cycle/DNA Damage; Apoptosis |
| Solubility | In Vitro: DMSO: 50 mg/mL (76.48 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
PI3Kα 20.3 nM (IC50) |
HDAC3 24.5 nM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 50 mg/mL (76.48 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
PH14 is a broad-spectrum PI3K inhibitor, most strongly targeting PI3Kα (IC50 of 20.3 nM)[1]. PH14 is also a selective inhibitor of HDAC1-3, with its strongest inhibitory activity against HDAC3 (IC50 = 24.5 nM)[1]. In human liver microsomes, PH14 (10 μM) weakly inhibits CYP1A2, CYP2B6, CYP2C9, CYP2C19 and CYP3A4, and moderately inhibits CYP2D6[1]. PH14 (48 h) potently inhibits proliferation of various tumor cell lines, most strongly in Jeko-1 cells (IC50 = 0.5 μM), and is not cytotoxic to normal HL7702 hepatocytes, even at concentrations up to 100 μM[1]. In Jeko-1 cells, PH14 (0.25-1 μM; 24 h) blocks the PI3K/AKT signaling pathway, selectively raises acetylated histone H3 levels, and induces caspase 3 cleavage[1]. PH14 (0.25-1 μM; 48 h) induces apoptosis in Jeko-1 cells in a dose-dependent manner[1].
Western Blot Analysis[1]
| Cell Line | human mantle cell lymphoma Jeko-1 cells |
|---|---|
| Concentration | 0.25, 0.5, 1 μM |
| Incubation Time | 24 h |
| 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. |
Apoptosis Analysis[1]
| Cell Line | human mantle cell lymphoma Jeko-1 cells |
|---|---|
| Concentration | 0.25, 0.5, 1 μM |
| Incubation Time | 48 h |
| Result | Induced Jeko-1 cell apoptosis in a dose-dependent manner, with increasing apoptotic cell populations observed at higher concentrations. |
In Vivo
In male ICR mice, PH14 (1 mg/kg; intravenous injection; single administration) shows favorable in vivo pharmacokinetic properties[1].
| Animal Model | ICR mice (male)[1] |
|---|---|
| Dosage | 1 mg/kg |
| Administration | i.v.; single administration |
| Result | Exhibited favorable in vivo pharmacokinetic properties in male ICR mice |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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