Cat. No.: HY-128333

PI3K/mTOR Inhibitor-4

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Based on 1 Customer Validation

PI3K/mTOR Inhibitor-4 is an orally active pan-class I PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity for PI3Kα, PI3Kγ, PI3Kδ and mTOR with IC₅₀ values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research of cancer.

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

Purity: 97.04%
CAS No.: 2361215-32-7
Formula: C₂₇H₂₂FN₃O₆S
Molecular Weight:535.54

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

PI3K/mTOR Inhibitor-4 Chemical Structure

CAS No.: 2361215-32-7

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

PI3Kα

0.63 nM (IC₅₀)

PI3Kδ

9.2 nM (IC₅₀)

mTOR

13.85 nM (IC₅₀)

PI3Kβ

94.54 nM (IC₅₀)

PI3Kγ

22 nM (IC₅₀)

All PI3K Isoforms :

All mTOR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	18.4 μM Compound: 8d-1	Antiproliferative activity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31228810]
A549	IC₅₀	1.35 μM Compound: 8d-1	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31228810]
HCT-116	IC₅₀	13.44 μM Compound: 8d-1	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31228810]
HeLa	IC₅₀	1.22 μM Compound: 8d-1	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31228810]
HepG2	IC₅₀	13.08 μM Compound: 8d-1	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31228810]
MCF7	IC₅₀	8.26 μM Compound: 8d-1	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31228810]

In Vitro

PI3K/mTOR Inhibitor-4 (compound 8d-1) has enzymatic inhibition activity for PI3Kα, PI3Kδ, mTOR, PI3Kβ and PI3Kγ with IC₅₀ values of 0.63 nM, 9.2 nM, 13.85 nM, 94.54 nM and 22 nM, respectively^[1].
PI3K/mTOR Inhibitor-4 shows potent anti-proliferation activity in A549, Hela, HCT-116, HepG2, A375 and MCF-7 cells with IC₅₀ values of 1.35 nM, 1.22 nM, 13.44 nM, 1.08 nM, 18.4 nM and 8.26 nM, respectively^[1].
PI3K/mTOR Inhibitor-4 (2.5-10 μM; 24 h) inhibits the PI3K/AKT/mTOR pathway^[1].

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

Cell Viability Assay^[1]

Cell Line:

PC12 and LO2 cells
Concentration:

0.625-20 µM
Incubation Time:

72 h
Result:

Showed low toxicity in concentrations from 0.625 µM to 20 µM.

Western Blot Analysis^[1]

Cell Line:

Hela cells
Concentration:

2.5, 5 and 10 µM
Incubation Time:

24 h
Result:

Dose-dependently decreased the level of phosphorylation of AKT and its downstream target S6 in Hela cell line.

In Vivo

PI3K/mTOR Inhibitor-4 (compound 8d-1) (i.v., oral; 1mg/kg, 10 mg/kg) displays favorable pharmacokinetic parameters in Sprague?Dawley rats^[1].
PI3K/mTOR Inhibitor-4 (oral; 10-50 mg/kg) shows significant efficiency in Hela/A549 tumor xenograft models without causing significant weight loss and toxicity^[1].

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

Animal Model:

SD rats (male; 200-220 g)^[1]
Dosage:

1, 10 mg/kg
Administration:

Intravenous, oral

Result:

IV (1 mg/kg)		PO (10 mg/kg)
CL (ml/min/kg)	Vss (ml/kg)	T_max (h)	C_max (ng/ml)	AUCinf (ng*h/ml)	t_1/2 (h)	F(%)
8.6	1199.81	2.67	886.67	4753.35	1.78	24.1

Animal Model:

BALB/c nude mice (female; 6-7 weeks; 18-22 g)^[1]
Dosage:

10, 20, 40, 50 mg/kg/d (Hela model) and 20, 40 mg/kg/d (A549 model)
Administration:

Oral
Result:

Inhibited the growth of xenograft tumors in a dose-dependent manner.

Chemical Information

CAS No. 2361215-32-7
Appearance Solid
Molecular Weight 535.54
Formula C₂₇H₂₂FN₃O₆S
Color White to off-white
SMILES

FC1=CC=C(S(NC2=CC(C3=CC=C(OCC(N4C5=CC=C(OC)C=C5)=O)C4=C3)=CN=C2OC)(=O)=O)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (466.82 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

1.8673 mL

9.3364 mL

18.6727 mL

5 mM

0.3735 mL

1.8673 mL

3.7345 mL

10 mM

0.1867 mL

0.9336 mL

1.8673 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 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]. Guoyi Yan, et al. Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. Eur J Med Chem [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8673 mL	9.3364 mL	18.6727 mL	46.6819 mL
	5 mM	0.3735 mL	1.8673 mL	3.7345 mL	9.3364 mL
	10 mM	0.1867 mL	0.9336 mL	1.8673 mL	4.6682 mL
	15 mM	0.1245 mL	0.6224 mL	1.2448 mL	3.1121 mL
	20 mM	0.0934 mL	0.4668 mL	0.9336 mL	2.3341 mL
	25 mM	0.0747 mL	0.3735 mL	0.7469 mL	1.8673 mL
	30 mM	0.0622 mL	0.3112 mL	0.6224 mL	1.5561 mL
	40 mM	0.0467 mL	0.2334 mL	0.4668 mL	1.1670 mL
	50 mM	0.0373 mL	0.1867 mL	0.3735 mL	0.9336 mL
	60 mM	0.0311 mL	0.1556 mL	0.3112 mL	0.7780 mL
	80 mM	0.0233 mL	0.1167 mL	0.2334 mL	0.5835 mL
	100 mM	0.0187 mL	0.0934 mL	0.1867 mL	0.4668 mL

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PI3K/mTOR Inhibitor-4

Bioactive Compound Library Max

Bioactive Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

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Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

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Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

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Membrane Protein-targeted Compound Library

Serine/Threonine Kinase Inhibitor Library

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Multi-Target Compound Library

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MCE Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Lactylation Compound Library

All PI3K Isoforms

All mTOR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PI3K/mTOR Inhibitor-4 Related Classifications

HY-128333 Related Classifications