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VS-5584

Catalog No. T6103 CAS 1246560-33-7

Synonyms: SB2343, VS 5584, VS5584

VS-5584 (SB2343) is a pan-PI3K/mTOR kinase inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

VS-5584, CAS 1246560-33-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
2 mg	In stock	$ 48.00
5 mg	In stock	$ 77.00
10 mg	In stock	$ 101.00
25 mg	In stock	$ 181.00
50 mg	In stock	$ 328.00
100 mg	In stock	$ 531.00
1 mL * 10 mM (in DMSO)	In stock	$ 84.00

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Purity: 98.41%

Purity: 97.82%

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Description	VS-5584 (SB2343) is a pan-PI3K/mTOR kinase inhibitor.
Targets&IC50	mTOR:3.4 nM, PI3Kγ:3.0 nM, PI3Kα:2.6 nM, PI3Kβ:21 nM, PI3Kδ:2.7 nM
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 is approximately 10-fold selective for cancer stem cells with an EC50 of 15 nM in HMLE breast cancer cells. VS-5584 preferentially decreases CD44Hi/CD24Lo cells in an HMLER immortalized mammary cancer cell line. In SUM159 cells, VS-5584 effectively eliminates the cancer stem cell side population. [1] A large human cancer cell line panel screen (436 lines) reveals broad antiproliferative sensitivity and that cells harboring mutations in PI3KCA are generally more sensitive toward VS-5584 treatment. In the FLT3-ITD harboring MV4-11 cells, VS-5584 blocks pAkt (S473) and pAkt (T308) with IC50 of 12 and 13 nM, respectively. The IC50 of VS-5584 for pS6 (S240/244), pAkt (S473), and pAkt (T308) are 20, 23, and 15 nM, respectively. [2]
In vivo	In mice bearing triple negative breast cancer tumors, oral dosing of VS-5584 decreases tumor cancer stem cells and induces tumor regression in taxane-resistant models. [1] In a PTENnull human prostate PC3 xenograft model, treatment with VS-5584 leads to significant tumor growth inhibition (TGI) of 79% and 113% for 11 and 25 mg/kg, respectively. In a FLT3-ITD AML xenograft model, VS-5584 treatment induces dose-dependent inhibition of tumor growth (28% for 3.7 mg/kg and 76% for 11 mg/kg). [2]
Kinase Assay	In vitro mTOR kinase assays : The reaction mixture consisted of the following components in 10 μL assay buffer (50 mM Hepes pH 7.5, 10 mM MgCl 2, 3 mM MnCl 2, 1 mM EGTA, 2 mM DTT, 0.01%Tween-20): 0.10 μg/mL of in-house generated mTOR enzyme, 0.05 μM ULight-eIF4E-binding protein 1 (Thr37/46) peptide and 10 μM ATP. The mixture is incubated for 60 min at room temperature. 10 μL of Detection mixture consisted of 16 mM EDTA, 0.004 mM Eu-W1024-labeled Anti-Phospho-eIF4E-binding protein 1-(Thr37/46) antibody and 1X LANCE? Detection Buffer is then added and incubated for 60 min.
Cell Research	CellTiter-Glo assay(Only for Reference)

Synonyms	SB2343, VS 5584, VS5584
Molecular Weight	354.41
Formula	C17H22N8O
CAS No.	1246560-33-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 3 mg/mL (8.46 mM)

DMSO: 66 mg/mL (186.2 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. JA Pachter, et al. Molecular Targets and Cancer Therapeutics, 2012, abstract 405. 2. Hart S, et al. Mol Cancer Ther, 2013, 12(2), 151-161.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Inhibitor Library Anti-Cancer Drug Library Drug Repurposing Compound Library Kinase Inhibitor Library Anti-Colorectal Cancer Compound Library Metabolism Compound Library Anti-Ovarian Cancer Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

VS-5584 1246560-33-7 PI3K/Akt/mTOR signaling PI3K mTOR Phosphoinositide 3-kinase inhibit SB2343 SB-2343 Inhibitor SB 2343 VS 5584 VS5584 Mammalian target of Rapamycin inhibitor

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