- 貨號 Cat. No.
- S7016
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
VS-5584 (SB2343)
Catalog No.S7016
VS-5584 (SB2343) is a potent and selective dual PI3K/mTOR inhibitor for mTOR, PI3Kα/β/δ/γ with IC50 of 3.4 nM and 2.6-21 nM, respectively.
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10mg |
USD 248 |
In stock |
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50mg |
USD 844 |
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
Description |
VS-5584 (SB2343) is a potent and selective dual PI3K/mTOR inhibitor for mTOR, PI3Kα/β/δ/γ with IC50 of 3.4 nM and 2.6-21 nM, respectively. |
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Targets |
mTOR |
PI3Kα |
PI3Kα-H1047 |
PI3Kβ |
PI3Kδ |
PI3Kγ |
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IC50 |
3.4 nM |
2.6 nM |
3.3 nM |
21 nM |
2.7 nM |
3.0 nM [1] |
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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] |
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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] |
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Features |
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Protocol(Only for Reference)
Kinase Assay: [2]
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. |
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Cell Assay: [2]
Cell lines |
SNU-478, SNU-1196, SNU-245, SNU-1079, SNU-308, and SNU-869 |
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Concentrations |
~10 μM |
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Incubation Time |
48 h |
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Method |
CellTiter-Glo assay |
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Animal Study: [2]
Animal Models |
Male (PC3 and COLO 205) or female (MV4-11 and HuH7) BALB/c nude mice or female SCID mice (NCI-N87) |
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Dosages |
11 mg/kg, 25 mg/kg once daily |
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Administration |
orally |
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Solubility |
0.5% methylcellulose/0.2% Tween 80, 30 mg/mL |
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1
References
Molecular Weight (MW) |
354.41 |
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Formula |
C17H22N8O
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CAS No. |
1246560-33-7 |
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Storage |
2 years -20℃Powder |
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6 months-80℃in DMSO |
Syonnyms |
N/A |
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Solubility (25°C) * |
In vitro |
DMSO |
71 mg/mL (200 mM) |
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Water |
<1 mg/mL (<1 mM) |
Ethanol |
3 mg/mL (8 mM) |
In vivo |
0.5% methylcellulose/0.2% Tween 80, |
30 mg/mL |
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
Chemical Name |
2-Pyrimidinamine, 5-[8-methyl-9-(1-methylethyl)-2-(4-morpholinyl)-9H-purin-6-yl]- |
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