Cat. No.: HY-149669

PH14

Name: PH14
Brand: MedChemExpress
SKU: HY-149669
Price: 400.00 USD
Availability: InStock
Rating: 5 (1 reviews)

고객리뷰

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.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity : 99.09%
CAS No.: 3053430-96-6
화학식: C₃₄H₃₉N₉O₅
분자량:653.73

보관:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

PH14 Chemical Structure

CAS No.: 3053430-96-6

사이즈

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
용액&용해도
- In Vitro
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

PI3Kα

20.3 nM (IC₅₀)

HDAC3

24.5 nM (IC₅₀)

All PI3K Isoforms :

All HDAC Isoforms :

All Akt Isoforms :

All Histone Acetyltransferase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
JeKo-1	IC₅₀	0.5 μM	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.	37948955
HL-60	IC₅₀	0.9 μM	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.	37948955
MDA-MB-231	IC₅₀	1.5 μM	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.	37948955

In Vitro

Anti-cancerApoptosisOthers

Anti-cancer

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].

Anti-cancer

Apoptosis

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].

Others

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].

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

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.

Parmacokinetics

Species	Dose	Route	C₀	T_1/2	AUC_0-t	AUC_0-∞	MRT_{INF_obs}	V_ss	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

PH14 (1 mg/kg; intravenous injection; single administration) exhibits favorable in vivo pharmacokinetic properties in male ICR mice^[1].

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

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

Related Protocols :

Chemical Information

CAS No. 3053430-96-6
Appearance Solid
분자량 653.73
화학식 C₃₄H₃₉N₉O₅
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
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

용액&용해도

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5297 mL

7.6484 mL

15.2968 mL

5 mM

0.3059 mL

1.5297 mL

3.0594 mL

10 mM

0.1530 mL

0.7648 mL

1.5297 mL

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.

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Deng J, et al. Discovery of benzamide-based PI3K/HDAC dual inhibitors with marked pro-apoptosis activity in lymphoma cells. European journal of medicinal chemistry. 2023 Dec 15;262:115915. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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PH14

All PI3K Isoforms

All HDAC Isoforms

All Akt Isoforms

All Histone Acetyltransferase Isoforms