VS-5584 is a pan-PI3K/mTOR kinase inhibitor.
| Pack Size | Availability | Price/USD | Quantity |
|---|---|---|---|
| 1 mg | In stock | $ 88 | |
| 2 mg | In stock | $ 149 | |
| 4 mg | In stock | $ 238 | |
| 10 mg | In stock | $ 449 | |
| 20 mg | In stock | $ 686 |
| Description | VS-5584 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. 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. |
| 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). |
| Synonyms | VS5584, VS 5584, SB2343 |
| CAS No. | 1246560-33-7 |
| Chemical Formula | C17H22N8O |
| Molecular Weight | 354.418 |
| Solubility | Ethanol: 3 mg/mL (8.46 mM) DMSO: 66 mg/mL (186.2 mM); H2O: <1 mg/mL |
| Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
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