ChemicalBook > CAS DataBase List > VS-5584

VS-5584

Product Name: VS-5584
CAS No.: 1246560-33-7
Chemical Name: VS-5584
Synonyms: SB-2343;VS-5584 (SB2343);SB2343;CS-875;SB 2343;VS-5584;VS-5584, >=98%;VS-5584 VS5584;VS-5584 USP/EP/BP;VS-5584, 10 mM in DMSO
CBNumber: CB42666411
Molecular Formula: C17H22N8O
Formula Weight: 354.41
MOL File: 1246560-33-7.mol

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VS-5584 Property

Boiling point:: 687.2±65.0 °C(Predicted)
Density: 1.48±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: insoluble in H2O; ≥17.7 mg/mL in DMSO; ≥4.71 mg/mL in EtOH with ultrasonic
form: solid
pka: 4.53±0.10(Predicted)
color: Light yellow to yellow
InChI: InChI=1S/C17H22N8O/c1-10(2)25-11(3)21-14-13(12-8-19-16(18)20-9-12)22-17(23-15(14)25)24-4-6-26-7-5-24/h8-10H,4-7H2,1-3H3,(H2,18,19,20)
InChIKey: QYBGBLQCOOISAR-UHFFFAOYSA-N
SMILES: C1(N)=NC=C(C2=C3C(=NC(N4CCOCC4)=N2)N(C(C)C)C(C)=N3)C=N1

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H302Harmful if swallowed

H372Causes damage to organs through prolonged or repeated exposure

H410Very toxic to aquatic life with long lasting effects

Precautionary statements

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P273Avoid release to the environment.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 16294
Product name: VS-5584
Purity: ≥98%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 16294
Product name: VS-5584
Purity: ≥98%
Packaging: 5mg
Price: $139
Updated: 2024/03/01

Cayman Chemical

Product number: 16294
Product name: VS-5584
Purity: ≥98%
Packaging: 10mg
Price: $230
Updated: 2024/03/01

ChemScene

Product number: CS-1202
Product name: VS-5584
Purity: 98.15%
Packaging: 5mg
Price: $90
Updated: 2021/12/16

ChemScene

Product number: CS-1202
Product name: VS-5584
Purity: 98.15%
Packaging: 10mg
Price: $120
Updated: 2021/12/16

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VS-5584 Chemical Properties,Usage,Production

Description

Phosphatidylinositol 3-kinase (PI3K) signaling through Akt/PKB and the mammalian target of rapamycin (mTOR) controls gene expression related to cell proliferation, differentiation, and apoptosis. Increased activity of this pathway is important in many types of cancer. VS-5584 is a purine analog that inhibits mTOR (IC₅₀ = 37 nM) and PI3K (IC₅₀s = 16, 68, 25, and 42 nM for the α, β, γ, and δ isoforms, respectively) without relevant activity against more than 400 additional lipid and protein kinases. By inhibiting the phosphorylation of substrates downstream of PI3K and mTOR, VS-5584 demonstrates broad anti-proliferative sensitivity leading to tumor growth inhibition in human tumor models.

Uses

VS-5584 is a pan-PI3K/mTOR kinase inhibitor with IC50s of 16 nM, 68 nM, 42 nM, 25 nM, and 37 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively. VS-5584 simultaneously blocks mTORC2 as well as mTORC1.

in vivo

Nude mice bearing MDA-MB-231 human breast cancer tumors are treated for 5 days with once daily oral VS-5584 (25 mg/kg). Oral treatment of tumor bearing mice with VS-5584 reduces cancer atem cells analyzed from extracted tumors. Mice are implanted with tumor fragments from a docetaxel-resistant patient-derived triple negative breast cancer. Mice are treated with VS-5584 (20 mg/kg, po, qd) or Docetaxel (20 mg/kg, i.v.). Oral VS-5584 induces tumor regression in a Docetaxel-resistant patient-derived breast cancer model^[1]. A single oral dose of VS-5584 is rapidly absorbed with a t_max of 0.9 hours and an elimination half-life of 10 hours. To determine the pharmacokinetic and pharmacodynamic relationship in tumors, PC3-tumor–bearing mice are treated with a single dose of VS-5584 and plasma and tumors are harvested after 6 hours and analyzed for concentrations of VS-5584 and effects on target efficacy biomarkers. Plasma levels of VS-5584 increase dose-dependently. For evaluation of efficacy in a Rapamycin-sensitive PC3 engraftment model, tumor-bearing mice are treated with VS-5584 for 28 days in comparison with the rapalog Everolimus. VS-5584 is well tolerated at both doses tested (11 and 25 mg/kg) with minimal weight loss (mean 4.7% on day 27). Treatment with VS-5584 leads to significant tumor growth inhibition (TGI) of 79% and 113% for 11 and 25 mg/kg, respectively^[1].

target

mTOR

IC 50

PI3Kα: 16 nM (IC₅₀); PI3Kγ: 25 nM (IC₅₀); PI3Kδ: 42 nM (IC₅₀); PI3Kβ: 68 nM (IC₅₀); Vps34: 7470 nM (IC₅₀); mTOR: 37 nM (IC₅₀); mTORC1; mTORC2; DNA-PK: 1270 nM (IC₅₀)

References

[1] Hart S, et al. VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. Mol Cancer Ther, 2013, 12(2), 151-161. DOI:10.1158/1535-7163.MCT-12-0466

VS-5584 Preparation Products And Raw materials

Raw materials

Preparation Products

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VS-5584 Suppliers

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View Lastest Price from VS-5584 manufacturers

Career Henan Chemical Co

Product: VS-5584 1246560-33-7
Price: US $2.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 100kg
Release date: 2018-12-23

1246560-33-7, VS-5584Related Search:

VX-745 USP/EP/BP VX 702 Vps VR23 VRT752271 Defactinib BKM120 (NVP-BKM120, Buparlisib) ABT 737 IPI 145 IC-87114 XL147

2-Pyrimidinamine, 5-[8-methyl-9-(1-methylethyl)-2-(4-morpholinyl)-9H-purin-6-yl]-

5-[8-Methyl-9-(1-methylethyl)-2-(4-morpholinyl)-9H-purin-6-yl]-2-pyrimidinamine VS-5584

VS-5584, >=98%

VS-5584

SB 2343

SB2343

SB-2343

VS-5584 (SB2343)

5-(9-Isopropyl-8-Methyl-2-Morpholin-4-yl-9H-purin-6-yl)-pyriMidin-2-ylaMine

5-(9-ISOPROPYL-8-METHYL-2-MORPHOLINO-9H-PURIN-6-YL)PYRIMIDIN-2-AMINE

5-[8-Methyl-9-(1-methylethyl)-2-(4-morpholinyl)-9H-purin-6-yl]-2-pyrimidinamine

VS-5584 (SB2343);VS-5584;VS5584;VS 5584

SB-2343; VS5584; VS 5584; SB2343; SB 2343

CS-875

5-[9-Isopropyl-8-methyl-2-(morpholin-4-yl)purin-6-yl]pyrimidin-2-amine

VS-5584 USP/EP/BP

VS-5584 VS5584

VS-5584, 10 mM in DMSO

VS-5584 (SB2343) ，S7016

1246560-33-7

C17H22N8O

Akt

mTOR

PI3K

PI3K/Akt/mTOR

Inhibitors