Cat. No.: HY-16585

VS-5584

(Synonyms: SB2343)

5 Cited Publications

고객리뷰

Based on 5 publication(s) in Google Scholar

VS-5584 is a pan-PI3K/mTOR kinase inhibitor with IC₅₀s of 16 nM, 68 nM, 42 nM, 25 nM, and 37 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively. VS-5584 simultaneously blocks mTORC2 as well as mTORC1.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 98.71%
CAS No.: 1246560-33-7
화학식: C₁₇H₂₂N₈O
분자량:354.41

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

VS-5584 Chemical Structure

CAS No.: 1246560-33-7

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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
- In Vivo
- Clinical Trial
Chemical Information
Publications (5)
용액&용해도
- In Vitro
- In Vivo
Protocol
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

PI3Kα

16 nM (IC₅₀)

PI3Kγ

25 nM (IC₅₀)

PI3Kδ

42 nM (IC₅₀)

PI3Kβ

68 nM (IC₅₀)

Vps34

7470 nM (IC₅₀)

mTOR

37 nM (IC₅₀)

mTORC1

mTORC2

DNA-PK

1270 nM (IC₅₀)

All PI3K Isoforms :

All mTOR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	IC₅₀	0.13 μM Compound: 1; SB2343, VS-5584	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay	[PMID: 29360358]
MV4-11	IC₅₀	0.2 μM Compound: 1; SB2343, VS-5584	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay	[PMID: 29360358]
PC-3	IC₅₀	0.18 μM Compound: 1; SB2343, VS-5584	Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay	[PMID: 29360358]

In Vitro

VS-5584 is an ATP-competitive inhibitor which selectively inhibits PI3K/mTOR signaling with equivalent low nanomolar potency against all human Class I PI3K isoforms and mTOR kinase. VS-5584 (0.001, 0.01, 0.1,1,10 and 100 μM) preferentially inhibits cancer stem cells in HMLE breast cancer cells while Paclitaxel increases the percentage of cancer stem cells. VS-5584 (0.1, 1, 10, 100 and 1000 nM) reduces the number of Aldefluor-positive cancer stem cells while Paclitaxel increases the percentage of cancer stem cells. VS-5584 (10, 30, 100, 300 nM) reduces the percentage of cancer stem cells (side population) in a Hoechst dye exclusion assay^[1]. VS-5584 is a potent inhibitor of mTOR (IC₅₀=37 nM) as well as class I PI3K isoforms (IC₅₀: PI3Kα=16 nM; PI3Kβ=68 nM; PI3Kγ=25 nM; PI3Kδ=42 nM). All other evaluated kinases show negligible binding when tested up to 10 μM VS-5584^[1].

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

In Vivo

Nude mice bearing MDA-MB-231 human breast cancer tumors are treated for 5 days with once daily oral VS-5584 (25 mg/kg). Oral treatment of tumor bearing mice with VS-5584 reduces cancer atem cells analyzed from extracted tumors. Mice are implanted with tumor fragments from a docetaxel-resistant patient-derived triple negative breast cancer. Mice are treated with VS-5584 (20 mg/kg, po, qd) or Docetaxel (20 mg/kg, i.v.). Oral VS-5584 induces tumor regression in a Docetaxel-resistant patient-derived breast cancer model^[1]. A single oral dose of VS-5584 is rapidly absorbed with a t_max of 0.9 hours and an elimination half-life of 10 hours. To determine the pharmacokinetic and pharmacodynamic relationship in tumors, PC3-tumor–bearing mice are treated with a single dose of VS-5584 and plasma and tumors are harvested after 6 hours and analyzed for concentrations of VS-5584 and effects on target efficacy biomarkers. Plasma levels of VS-5584 increase dose-dependently. For evaluation of efficacy in a Rapamycin-sensitive PC3 engraftment model, tumor-bearing mice are treated with VS-5584 for 28 days in comparison with the rapalog Everolimus. VS-5584 is well tolerated at both doses tested (11 and 25 mg/kg) with minimal weight loss (mean 4.7% on day 27). Treatment with VS-5584 leads to significant tumor growth inhibition (TGI) of 79% and 113% for 11 and 25 mg/kg, respectively^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1246560-33-7
Appearance Solid
분자량 354.41
화학식 C₁₇H₂₂N₈O
Color Light yellow to yellow
SMILES

NC1=NC=C(C2=C3N=C(C)N(C(C)C)C3=NC(N4CCOCC4)=N2)C=N1
Synonyms

SB2343
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (5)

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Br J Cancer

Thermal stress involved in TRPV2 promotes tumorigenesis through the pathways of HSP70/27 and PI3K/Akt/mTOR in esophageal squamous cell carcinoma. [Abstract]

2022 Nov;127(8):1424-1439. PMID: 35896815
Front Pharmacol

CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]

2020 Nov 11:11:580407. PMID: 33343350
Sci Rep

QSAR analysis on a large and diverse set of potent phosphoinositide 3-kinase gamma (PI3Kγ) inhibitors using MLR and ANN methods. [Abstract]

2022 Apr 12;12(1):6090. PMID: 35414065
Research Square Print

2023 Mar 9.
Research Square Preprint

2020 Sep.

용액&용해도

In Vitro:

DMSO : 33.33 mg/mL (94.04 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

2.8216 mL

14.1080 mL

28.2159 mL

5 mM

0.5643 mL

2.8216 mL

5.6432 mL

10 mM

0.2822 mL

1.4108 mL

2.8216 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (7.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Cell Assay^[1]

For proliferation assays in 96-well plates, SET-2, SNU-478, SNU-1196, SNU-245, SNU-1079, SNU-308, SNU-869, and MKN7 cells are used. The multiple myeloma cells (H929, MM1.S, MM1.R, R8226, U266) and nasopharyngeal cells (CNE-1, CNE-2, HONE1, HK1) are used. Cells are seeded at 30% to 50% confluency for adherent cells, or 2,000 to 6,000 cells for suspension cells and treated the following day with VS-5584 (in triplicates) at concentrations up to 10 μM for 48 hours. Cell viability is monitored using the CellTiter-Glo assay. Dose-response curves were plotted to determine IC₅₀ values for the compounds using the XL-fit software^[1].

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

Animal Administration^[1]

Mice^[1]
Athymic BALB/c nude mice (BALB/cOlaHsd-Foxn1nu) are used. Fox-Chase severe combined immunodeficient (SCID) mice (CB17/Icr-Prkdc^scid/CrlBltw) are used. Male (PC3 and COLO 205) or female (MV4-11 and HuH7) BALB/c nude mice or female SCID mice (NCI-N87) are implanted intradermally in the right flank with 5×10⁶ (PC3, COLO205, HuH7, NCI-N87) or 1×10⁷ (MV4-11) cells. Cells are resuspended in 70% (v/v; COLO205 and HuH7 only) or 50% (v/v) serum-free growth medium/Matrigel and injected in a total volume of 100 μL, using a 27.5-gauge needle. Dosing started 7 to 14 days after tumor implantation. VS-5584 (11 and 25 mg/kg) is dosed daily orally^[1].

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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Hart S, et al. VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. Mol Cancer Ther, 2013, 12(2), 151-161. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8216 mL	14.1080 mL	28.2159 mL	70.5398 mL
	5 mM	0.5643 mL	2.8216 mL	5.6432 mL	14.1080 mL
	10 mM	0.2822 mL	1.4108 mL	2.8216 mL	7.0540 mL
	15 mM	0.1881 mL	0.9405 mL	1.8811 mL	4.7027 mL
	20 mM	0.1411 mL	0.7054 mL	1.4108 mL	3.5270 mL
	25 mM	0.1129 mL	0.5643 mL	1.1286 mL	2.8216 mL
	30 mM	0.0941 mL	0.4703 mL	0.9405 mL	2.3513 mL
	40 mM	0.0705 mL	0.3527 mL	0.7054 mL	1.7635 mL
	50 mM	0.0564 mL	0.2822 mL	0.5643 mL	1.4108 mL
	60 mM	0.0470 mL	0.2351 mL	0.4703 mL	1.1757 mL
	80 mM	0.0353 mL	0.1763 mL	0.3527 mL	0.8817 mL

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VS-5584

Antioxidant Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Lipid Metabolism Compound Library

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

Pain-Related Compound Library

Mitochondrial Protection Compound Library

Membrane Protein-targeted Compound Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

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

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) VS-5584

All PI3K Isoforms

All mTOR Isoforms

Biological Activity

Chemical Information

Publications (5)

용액&용해도

Protocol

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

VS-5584 Related Classifications

HY-16585 Related Classifications