5-[8-Methyl-9-(1-methylethyl)-2-(4-morpholinyl)-9H-purin-6-yl]-2-pyrimidinamine VS-5584
VS-5584 (SB2343)
CAS: 1246560-33-7
Molecular Formula: C17H22N8O
5-[8-Methyl-9-(1-methylethyl)-2-(4-morpholinyl)-9H-purin-6-yl]-2-pyrimidinamine VS-5584 - Names and Identifiers
5-[8-Methyl-9-(1-methylethyl)-2-(4-morpholinyl)-9H-purin-6-yl]-2-pyrimidinamine VS-5584 - Physico-chemical Properties
| Molecular Formula | C17H22N8O |
| Molar Mass | 354.41 |
| Density | 1.48±0.1 g/cm3(Predicted) |
| Boling Point | 687.2±65.0 °C(Predicted) |
| pKa | 4.53±0.10(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | VS-5584 is an ATP-competitive inhibitor that selectively inhibits the PI3K/mTOR signaling pathway with comparable effects and inhibition of all human PI3K subtypes and mTOR kinases. VS-5584 was about 10-fold more selective for HMLE breast cancer cells than for cancer stem cells, with an EC50 value of 15 nM. VS-5584 preferentially reduced CD44 in HMLER immortalized breast cancer cell lines a large number of human cancer cell lines (436 strains) showed extensive anti-proliferative sensitivity, and cells containing the PI3KCA mutation were generally more sensitive to VS-5584 treatment. In FLT3-ITD cells mutated in MV4-11, VS-5584 inhibited pAkt(S473) and pAKT(T308) with IC50 of 12 nM and 13 nM, respectively. VS-5584 inhibited pS6 (S240/244), pAkt (S473) and pAkt (T308) with IC50 of 20 nM,23 nM, and 15 nM, respectively. |
| In vivo study | In mice with triple-negative breast cancer, oral doses of VS-5584 reduced tumor stem cells and induced tumor regression in a taxane-resistant model. PTEN |
5-[8-Methyl-9-(1-methylethyl)-2-(4-morpholinyl)-9H-purin-6-yl]-2-pyrimidinamine VS-5584 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.822 ml | 14.108 ml | 28.216 ml |
| 5 mM | 0.564 ml | 2.822 ml | 5.643 ml |
| 10 mM | 0.282 ml | 1.411 ml | 2.822 ml |
| 5 mM | 0.056 ml | 0.282 ml | 0.564 ml |
Last Update：2024-01-02 23:10:35
5-[8-Methyl-9-(1-methylethyl)-2-(4-morpholinyl)-9H-purin-6-yl]-2-pyrimidinamine VS-5584 - Reference Information
| biological activity | VS-5584 (SB2343) is an effective, selective, PI3K/mTOR dual inhibitor, inhibiting mTOR and PI3Kα/β/δ/γ,IC50 is 3.4 nM and 2.6-21 nM respectively. Phase 1. |
| target | TargetValue PI3Kα (Cell-free say) 2.6 nM PI3Kδ (Cell-free say) 2.7 nM PI3Kγ (Cell-free say) 3.0 nM mTOR (Cell-free say) 3.4 nM PI3Kβ (Cell-free say) 21 nM |
| Target | Value |
| PI3Kα (Cell-free assay) | 2.6 nM |
| PI3Kδ (Cell-free assay) | 2.7 nM |
| PI3Kγ (Cell-free assay) | 3.0 nM |
| mTOR (Cell-free assay) | 3.4 nM |
| PI3Kβ (Cell-free assay) | 21 nM |
| in vitro study | VS-5584 is a competitive inhibitor of ATP, selectively inhibiting PI3K/mTOR signaling pathway, and its effect is equivalent to inhibiting all PI3K subtypes and mTOR kinase. The selectivity of VS-5584 for HMLE breast cancer cells is about 10 times higher than that of cancer stem cells, and the EC50 value is 15 nM. VS-5584 preferentially reduces CD44 in HMLER immortalized breast cancer cell lines. A large number of human cancer cell lines (436 strains) show extensive antiproliferative sensitivity. Cells containing PI3KCA mutations are usually more sensitive to VS-5584 therapy. In FLT3-ITD mutated MV4-11 cells, VS-5584 inhibited pAkt(S473) and pAKT(T308) with IC50 of 12 nM and 13 nM, respectively. VS-5584 inhibits pS6 (S240/244), pAkt (S473) and pAkt (T308),IC50 is 20 nM,23 nM, and 15 nM respectively. |
| in vivo study | in mice with triple negative breast cancer, the oral dose of VS-5584 reduces tumor stem cells and induces tumor regression in a model of taxane resistance. In PTEN |
Last Update：2024-04-09 21:04:16
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Product Name: VS-5584 (SB2343) Visit Supplier Webpage Request for quotationCAS: 1246560-33-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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