VS-5584

SKU: orb1301070

Description

VS-5584 (SB2343) is a potent and selective small molecule inhibitor targeting both PI3K and mTOR kinases. It is widely used in preclinical research to investigate oncogenic signaling pathways in cancer biology, demonstrating utility in both in vitro cellular assays and in vivo tumor models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1246560-33-7
• MW: 354.41
• Purity: 99.54%
• Formula: C₁₇H₂₂N₈O
• SMILES: CC(C)n1c(C)nc2c(nc(nc12)N1CCOCC1)-c1cnc(N)nc1
• Target: mTOR,PI3K
• Solubility: DMSO:66 mg/mL (186.22 mM);Ethanol:3 mg/mL (8.46 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.64 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  PI3Kγ:3.0 nM|mTOR:3.4 nM|DNA-PK:1270 nM|PI3Kα:2.6 nM|PI3Kβ:21 nM|PI3Kδ:2.7 nM|VPS34:7470 nM
• 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. 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).
• 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. 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.
• Cell Research:
  CellTiter-Glo assay(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Mammalian target of Rapamycin, Inhibitor, inhibit, mTOR, Phosphoinositide 3-kinase, PI3Kα, PI3Kγ, PI3Kβ, PI3Kδ, PI3K, SB 2343, SB2343, SB-2343, VS 5584, VS5584, VS-5584

Compound Identifiers

PubChem CID

46912230