PI3K/mTOR Inhibitor-4

Name: PI3K/mTOR Inhibitor-4
Brand: MedChemExpress
SKU: HY-128333
Rating: 4.5 (1 reviews)

Cat. No.: HY-128333 Purity: 97.00%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

PI3K/mTOR Inhibitor-4 Chemical Structure

CAS No. : 2361215-32-7

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 850	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1350	In-stock	Estimated Time of Arrival: December 31
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500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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•Related Screening Libraries:

•Related Small Molecules:

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View All PI3K Isoform Specific Products:

View All Isoforms

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

View All mTOR Isoform Specific Products:

View All Isoforms

mTOR mTORC1 mTORC2

Biological Activity
Purity & Documentation
References
Customer Review

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)

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.

Molecular Weight

535.54

Formula

C₂₇H₂₂FN₃O₆S

CAS No.

2361215-32-7

Appearance

Solid

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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 (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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

μL

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 97.00%

Select Batch:

Data Sheet (282 KB) SDS (251 KB)

COA (255 KB) HNMR (274 KB) RP-HPLC (206 KB) LCMS (103 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]

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