- Min.Order :1 Gram
- Purity: >99%
- Payment Terms : T/T,
Keywords
VS-5584 1246560-33-7
Quick Details
- Appearance:white powder
- Application:for laboratory research
- PackAge:Aluminium foil bag packing
- ProductionCapacity:1|Kilogram|Day
- Storage:keep away from heat, sparks and flames
- Transportation:by air; by sea; by express
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Details:
Technical Data
| Molecular Weight (MW) | 354.41 |
|---|---|
| Formula |
C17H22N8O |
| CAS No. | 1246560-33-7 |
| Synonyms | N/A |
| Solubility (25°C) | DMSO 71 mg/mL |
|---|---|
| Water <1 mg/mL | |
| Ethanol 3 mg/mL | |
| Storage | 2 years -20℃Powder |
| 6 months-80℃in DMSO |
| Chemical Name | 2-Pyrimidinamine, 5-[8-methyl-9-(1-methylethyl)-2-(4-morpholinyl)-9H-purin-6-yl]- |
|---|
Preparing Stock Solutions
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. | |||||
|---|---|---|---|---|---|---|
| Targets | mTOR | PI3Kα | PI3Kα-H1047 | PI3Kβ | PI3Kδ | PI3Kγ |
| IC50 | 3.4 nM | 2.6 nM | 3.3 nM | 21 nM | 2.7 nM | 3.0 nM [1] |
| 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] | |||||
| Features | ||||||
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